Antibacterial Proteins/Peptides

Corona is an avian and mammalian Ribovirus which generally evade host immune mechanism hampering respiratory tract of the host. Structurally it has an envelope of protein enclosing a single-stranded positively coiled RNA genome. Coronavirus uses around 4-5 different classes of protein for its replication in the host cell. Due to the high mutation rate of the viral genome development of a vaccine against corona has been a difficult task. In the current scenario, the world is facing a problem with CoViD-19 as the biggest pandemic. Several combinations of drugs like Hydroxychloroquine, Plaquine, Chloroquine, etc. targeting viral protein have been utilized for controlling viral infection. The possibility of insect brain proteins was checked against the selected non-structural proteins of CoViD-19 that take an active role in the replication of the virus in the host. Molecular docking methodology plays an important role in predicting interaction between the insect proteins with non-structural protein (nsp) of coronavirus. The results predict good bonding affinity with possible interaction as hydrogen bond and salt bridge between antibacterial protein and nsp of CoViD-19 indicating as afuture alternative medications.

Pharmacologically active phytochemicals isolated from different parts of L. speciosa have revealed antibacterial, hypoglycemic, anti-inflammatory, hepatoprotective and antioxidant properties . This experimental study was designed to evaluate the effect of LSE in the prevention of hepatotoxicity from oxidative damage induced with MSG administration in Sprague Dawley rats and its possible mechanism of action.

On the basis of the inductive QSAR descriptors we have created a neural network-based solution enabling quantification of antibacterial activity in the series of 101 synthetic cationic polypeptides (CAMEL-s). The developed QSAR model allowed 80% correct categorical classification of antibacterial potencies of the CAMEL-s both in the training and the validation sets. The accuracy of the activity predictions demonstrates that a narrow set of 3D sensitive 'inductive' descriptors can adequately describe the aspects of intra-and intermolecular interactions that are relevant for antibacterial activity of the cationic polypeptides. The developed approach can be further expanded for the larger sets of biologically active peptides and can serve as a useful quantitative tool for rational antibiotic design and discovery.

Activation of the contact system has two classical consequences: initiation of the intrinsic pathway of coagulation, and cleavage of high molecular weight kininogen (HK) leading to the release of bradykinin, a potent proinflammatory peptide. In human plasma, activation of the contact system at the surface of significant bacterial pathogens was found to result in further HK processing and bacterial killing. A fragment comprising the D3 domain of HK is generated, and within this fragment a sequence of 26 amino acids is mainly responsible for the antibacterial activity. A synthetic peptide covering this sequence kills several bacterial species, also at physiological salt concentration, as effectively as the classical human antibacterial peptide LL-37. Moreover, in an animal model of infection, inhibition of the contact system promotes bacterial dissemination and growth. These data identify a novel and important role for the contact system in the defence against invasive bacterial infection.

Leaves of Clerodendron serratum were investigated for their phytochemical constituents like phenolic compounds, flavonoids, tannins, terpenoids, steroids and screened for in vitro antioxidant activity against 2,2-diphenyl-2-picrylhydrazyl (DPPH), superoxide anion, hydroxyl radical, nitric oxide radical, total antioxidant capacity and reducing power. Estimation of total phenolic compounds by Folin-Ciocalteu reagent indicated that the extract (1 mg) contained 130 µg of gallic acid equivalents and that of total flavonoids demonstrated 7 µg of quercetin equivalents in 1mg of the extract. DPPH radical, hydroxyl radical, nitric oxide radical and superoxide radical scavenging activities were found to be 211, 138.35, 171.54 and 177.93 µg/mL, respectively. The extract showed significant activities in all antioxidant assays and the reducing power of the extract was found to be significantly higher than ascorbic acid. The results obtained indicate that in vitro antioxidant property of Clerodendron serratum leaf extract may be due to high content of phenolic compounds and justify the therapeutic applications of the plant in the indigenous and traditional system of medicine for the treatment of inflammatory and neurological disorders.

Although regular exercise-training improves immune/inflammatory status, the influence of air pollutants exposure during outdoor endurance training compared to a sedentary lifestyle has not yet been clarified. This study aimed to compare the immune/inflammatory responses in the airways of street runners and sedentary people after acute and chronic particulate matter (PM) exposure. Forty volunteers (street runners (RUN, n = 20); sedentary people (SED, n = 20)) were evaluated 1 (acute) and 10 (chronic) weeks after PM exposure. Cytokines [interferon (IFN)-γ, tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-10, IL-13, and IL-17A] in nasal lavage fluid, salivary antibacterial peptides (lactoferrin (LTF), cathelicidin (LL-37), defensin-α 1–3), and secretory immunoglobulin A (SIgA), plasma club cell protein (CC16), and fractional exhaled nitric oxide (FeNO) were analyzed. After acute exposure, the RUN group showed lower levels of IL-13, IL-10, and FeNO, but higher defensin-α than the S...

Recently antioxidant properties of plants have been found to be correlated with the defense of oxidative stress. In this respect flavonoids and other phenolic compounds have gained considerable attention. Calotropis gigantea has been widely used for its various pharmacological activities including cancer studies. In this study, the evaluation of antioxidant activity of methanolic extract of the flowers of C. gigantea has been done by in vitro method. The antioxidant activity of flower extract was evaluated by determining lipid peroxidation method, total phenolics contents was determined according to the Folin-Ciocalteu method and total flavonoid content by aluminium chloride colorimetric method. The results of the study showed that the methanolic extract of flowers of C. gigantea possesses antioxidant activity and it can be known by the protection of the cells. The total phenolic and flavonoid content was determined and expressed in term of gallic acid equivalent and quercetin equivalent, respectively. The results of the present study clearly showed that the flower extract of C. gigantea demonstrated antioxidant activities and it may act as potential antioxidant sources for human biological system.

Although regular exercise-training improves immune/inflammatory status, the influence of air pollutants exposure during outdoor endurance training compared to a sedentary lifestyle has not yet been clarified. This study aimed to compare the immune/inflammatory responses in the airways of street runners and sedentary people after acute and chronic particulate matter (PM) exposure. Forty volunteers (street runners (RUN, n = 20); sedentary people (SED, n = 20)) were evaluated 1 (acute) and 10 (chronic) weeks after PM exposure. Cytokines [interferon (IFN)-γ, tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-10, IL-13, and IL-17A] in nasal lavage fluid, salivary antibacterial peptides (lactoferrin (LTF), cathelicidin (LL-37), defensin-α 1–3), and secretory immunoglobulin A (SIgA), plasma club cell protein (CC16), and fractional exhaled nitric oxide (FeNO) were analyzed. After acute exposure, the RUN group showed lower levels of IL-13, IL-10, and FeNO, but higher defensin-α than the S...

Although regular exercise-training improves immune/inflammatory status, the influence of air pollutants exposure during outdoor endurance training compared to a sedentary lifestyle has not yet been clarified. This study aimed to compare the immune/inflammatory responses in the airways of street runners and sedentary people after acute and chronic particulate matter (PM) exposure. Forty volunteers (street runners (RUN, n = 20); sedentary people (SED, n = 20)) were evaluated 1 (acute) and 10 (chronic) weeks after PM exposure. Cytokines [interferon (IFN)-γ, tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-10, IL-13, and IL-17A] in nasal lavage fluid, salivary antibacterial peptides (lactoferrin (LTF), cathelicidin (LL-37), defensin-α 1–3), and secretory immunoglobulin A (SIgA), plasma club cell protein (CC16), and fractional exhaled nitric oxide (FeNO) were analyzed. After acute exposure, the RUN group showed lower levels of IL-13, IL-10, and FeNO, but higher defensin-α than the S...

Abstract: Medicinal plants play an important role in folk medicine, and different plant species have been used in the treatment of many diseases. The plant species Plumbago zeylanica (known vernacularly as chitarak) of the family Plumbaginaceae is distributed as a perennial herb ...

Chemerin-derived peptide Val 66-Pro 85 (p4) restricts the growth of a variety of skinassociated bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). To better understand the antimicrobial potential of chemerin peptide, we compared p4 activity against MRSA in vitro to cathelicidin LL-37, one of the key endogenous peptides implicated in controlling the growth of S. aureus. The efficacy of p4 was also validated in relevant experimental models of skin pathology, such as topical skin infection with community-acquired MRSA, and in the context of skin inflammatory diseases commonly associated with colonization with S. aureus, such as atopic dermatitis (AD). We showed that p4 collaborates additively with LL-37 in inhibiting the growth of S. aureus, including MRSA, and that p4 was effective in vivo in reducing MRSA burden. p4 was also effective in reducing levels of skin-infiltrating leukocytes in S. aureus-infected AD-like skin. Taken together, our data suggest that p4 is effective in limiting S. aureus and, in particular, MRSA skin infection.

Marine gastropod, Peronia peronei, from north of the Persian Gulf, protein extraction was investigated using ultrafiltration, reversed-phase high-performance liquid chromatography and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF/TOF). The mass spectra showed that, the isolated peptide is most probably Dolabellanin B2 that has been extracted before from other marine mollusk, Dolabella auricularia. The antibacterial activity of purified peptide was assessed against seven bacterial strains (Staphylococcus aureus, Bacillus subtilis, Serratia marcescens, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Proteus mirabilis). Broth micro-dilution method, standard disk diffusion assay and bioautography were used for this aim. According to the results the identified peptide showed strong antibacterial activity against all mentioned bacterial strains. Computational studies through peptide modeling servers followed by 50 ns molecular dynamics simulation and surface electrostatic calculations indicates that this sequence could be most probably related to alpha helical cationic antimicrobial peptides (alpha-CAMPs) with overall charge of +1 at pH 7.

In the present study, the leaf of Cassia roxburghii and its powder were subjected to pharmacognostic evaluation in terms of macroscopic and microscopic evaluation. The powdered drug was subjected to extraction with various solvents such as petroleum ether, chloroform, ethyl acetate, methanol and aqueous extract by successive maceration. The methanolic and aqueous leaf extracts exhibited reducing power compared with ascorbic acid at similar concentrations. Based on the biochemical estimation of serum marker enzymes and histological study, all the extracts showed hepato protective activity and the maximum activity was seen in methanol extract at 200 mg/kg. The order of activity Me200>aq200>Me400>Aq400.

In the present study, the leaf of Cassia roxburghii and its powder were subjected to pharmacognostic evaluation in terms of macroscopic and microscopic evaluation. The powdered drug was subjected to extraction with various solvents such as petroleum ether, chloroform, ethyl acetate, methanol and aqueous extract by successive maceration. The methanolic and aqueous leaf extracts exhibited reducing power compared with ascorbic acid at similar concentrations. Based on the biochemical estimation of serum marker enzymes and histological study, all the extracts showed hepato protective activity and the maximum activity was seen in methanol extract at 200 mg/kg. The order of activity Me200>aq200>Me400>Aq400.

Bakuchi (Psoralea corylifolia Linn.) is one of the important endangered medicinal plants used in Ayurveda and other Traditional systems. Its cultivation and propagation is difficult due to its low germination rate (5-7%) and prolonged seed dormancy. Bakuchi seeds made into 5 groups, the experiment was conducted in a complete randomized block design with 5 treatments and 5 replications totally 500 seeds in each group) and observed for 50 days. Control Group 1 no-seed treatment, Group 2-Standard treated with 1% concentrated H2SO4, Group 3 Vrikshayurvedic treatment done by soaking in milk subsequently fumigation of Vidanga and ghee, Group 4-treated with paste of Brihati, Tila, Kamalanaala, Ghee and Group 5 treated by soaking in milk subsequently Cow dung, Vidanga and honey applied. Number of seeds germinated, germination percentage, emergence index and relative seed germination parameters were observed. HPLC studies carried out of post harvested Bakuchi seeds of all 5 groups to know the effect of seed treatments on Psoralen content quantitatively. Overall results indicates that Group 4 (8.000 ± 0.8367) seeds soaked in 12hrs milk followed by application of Brihati, Tila, Kamalanaala and Ghee paste for 12hrs treatment is statistically significant (P value>0.05) in comparison with group 2 (4.600 ± 0.6782) Sulphuric acid treatment and Group 3 (4.200± 0.9165) fumigation with Honey and Vidanga. Rest of the groups shown insignificant changes on germination parameters. HPLC results found that generally seed treatments may reduce the content of Psoralen as in control (Group 1) maximum percentage (0.04%w/w) of Psoralen is noticed. Among treatment groups Group 4 contains maximum (0.027%w/w) Psoralen next to control (0.039%w/w). Psoralen content is very less in standard Group 2 (0.022%w/w), Group 3 (0.023%w/w) & Group 4 (0.024%w/w). Maximum germination percentage was observed in Group 4 in comparison with the Group 2 conventional method of treating with sulphuric acid. Estimation of Psoralen contents in the seeds from the plants grown by various treated seeds reveled that Group 4 is qualitatively better than standard, but inferior to the control, standard and other Vrikshayurveda seed treatment techniques used in the current experiment.

In the study of designing pharmacophore models for analgesic, a series of 4-[4-chloro-3-(tri uoromethyl)-phenyl]-4-piperidinol (TFMP) derivatives were synthesized and characterized by physical and spectral method (HR-EIMS, HR-FABMS, 1 H-NMR, 13 C-NMR, UV, and FT-IR). The analgesic action of the synthesized derivatives was estimated by means of Hot Plate Method. Most of the compounds displayed potent analgesic e cacy and an ultrashort to long duration of action. The results indicate that these compounds are useful as analgesics. Qualitatively nine compounds resemble morphine in pharmacological action, whereas three derivatives are devoid of any signi cant analgesic potential. In conclusion, among active compounds (188%), 5 (137%), 6 (162%), and 8 (107%) respectively emerged as most effective analgesic and they depressed peripheral and centrally mediated pain by opioid dependent and independent systems.

Background: Antimicrobial peptides attract considerable interest as novel agents to combat infections. Their long-time potency across bacteria, viruses and fungi as part of diverse innate immune systems offers a solution to overcome the rising concerns from antibiotic resistance. With the rapid increase of antimicrobial peptides reported in the databases, peptide selection becomes a challenge. We propose similarity analyses to describe key properties that distinguish between active and non-active peptide sequences building upon the physicochemical properties of antimicrobial peptides. We used an iterative supervised machine learning approach to classify active peptides from inactive peptides with low false discovery rates in a relatively short computational search time. Results: By generating explicit boundaries, our method defines new categories of active and inactive peptides based on their physicochemical properties. Consequently, it describes physicochemical characteristics of similarity among active peptides and the physicochemical boundaries between active and inactive peptides in a single process. To build the similarity boundaries, we used the rough set theory approach; to our knowledge, this is the first time that this approach has been used to classify peptides. The modified rough set theory method limits the number of values describing a boundary to a user-defined limit. Our method is optimized for specificity over selectivity. Noting that false positives increase activity assays while false negatives only increase computational search time, our method provided a low false discovery rate. Published datasets were used to compare our rough set theory method to other published classification methods and based on this comparison, we achieved high selectivity and comparable sensitivity to currently available methods. Conclusions: We developed rule sets that define physicochemical boundaries which allow us to directly classify the active sequences from inactive peptides. Existing classification methods are either sequence-order insensitive or length-dependent, whereas our method generates the rule sets that combine order-sensitive descriptors with length-independent descriptors. The method provides comparable or improved performance to currently available methods. Discovering the boundaries of physicochemical properties may lead to a new understanding of peptide similarity.

Psoralea corylifolia Linn. (Leguminoseae) known as "Babchi" is a medicinal plant for the treatment of skin disorders. In the present investigation babchi oil has been evaluated for phytochemical constituents, antibacterial activity (agar well diffusion) and TLC bioautography assay. Phytochemical analysis demonstrated the presence of flavonoids, tannins, steroids, terpenoids, glycosides and saponins. Antibacterial activity of babchi oil was assessed on eight multi-drug resistant (MDR) clinical isolates from both Gram-positive and Gram-negative bacteria and two standard strains. It showed broad antibacterial activity against both Gram-positive bacteria such as Staphylococcus aureus, S. aureus MRSA, Enterococcus sp. and Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae. The highest in vitro inhibitory activity was observed for MDR Enterococcus sp. with wide inhibition zone diameters (21±0.16 mm) followed by standard S. aureus ATCC 25923 (16±0.11 mm) and K. pneumoniae (15±0.056 mm). Thin layer chromatography and bioautography assay demonstrated well-defined growth inhibition zones against Enterococcus sp. in correspondence with tannins observed at Rf values of 0.10-0.15 and 0.70-0.83. This established a good support to the use of this essential oil in herbal medicine and as a base for the development of novel potent drugs and phytomedicine. To the best of our knowledge, this is the first report that documents the antibacterial efficacy of tannins found in babchi oil against MDR bacteria from clinical isolates.

Batubara R, Hanum TI, Affandi O, Wahyuni HS. 2020. Chemical compounds contained in young and mature leaves of agarwood species Wikstroemia tenuiramis and its antioxidant properties. Biodiversitas 21: 4616-4622. The genus Wikstroemia is one of the genus of agarwood producing trees which has not been widely researched and published. One type of this genus is Wikstroemia tenuiramis Miq, which grows naturally in North Sumatra, the leaves are like other types of agarwood leaves can be used as raw material for agarwood leaves tea. A research has been conducted to determine the chemical contents contained in the young and mature leaves of agarwood plants species W. Tenuiramis. This research methods applied qualitative analysis using phytochemical screening, quantitative analysis to determine tannin content using titration method, antioxidant activity analysis using 2,2-diphenil-1-picrylhydrazil (DPPH) method, and compound tracing using Py-gas chromatography-mass spectrometry (Py-GC-MS) instruments. The qualitative phytochemical analysis results showed no difference in chemical compounds contained in both the young and mature leaves. Both the young and mature leaves contained flavonoids, triterpenoids, and tannins, and did not contain alkaloids, steroids and saponins. The young contained tannins of 1.079 ± 0.001% and the mature contained tannins of 4.645 ± 0.021%, not significant statistically. Py-GC-MS analysis showed the presence of various 30 bioactive compounds contained in both young and mature leaves. The analysis results also showed that both the young and mature leaves had very strong antioxidant activity. Our findings suggest that the two types of leaves have equal utility value of in term of chemical contents and antioxidant potentials.

This study evaluates the synergistic antioxidants effects of extracts of Massularia acuminata and ascorbic acid in aluminum chloride-treated oxidative stress in wistar albino rats with a view to investigate the preventive potential of co-administration of Massularia acuminata and ascorbic acids. The in vivo antioxidant properties of the extract were evaluated using in vivo catalase activity, superoxide dismutase activity and thiobarbituric acid reactive substances assay by standard methods via spectrophotometry. The in vivo studies were carried out on rats, grouped majorly into positive control, negative control and the treated groups. The positive control group was administered with normal saline (distilled water) orally, while the negative control group was orally induced with the toxicant (aluminium chloride). The treated group was orally administered with the extract after toxicant administration. Ascorbic acid was used as standard antioxidant in the study. The effects on enzyma...

Objective: The target of this current research work sought to analyze the antioxidant and antimicrobial activities of ethyl acetate and hydroalcoholic extracts of Momordica cymbalaria leaves through various in vitro assays. Methods: The antioxidant capability of the extracts to quench free radical was explored spectrophotometrically against DPPH, nitric oxide, superoxide anion, hydroxyl radicals and ferric reducing power. Metal chelating effect was also carried out by measuring the ferrous ion chelating property. The total phenolic and flavonoid contents were assessed by Folin-Ciocalteau and aluminium chloride reagents. The antimicrobial activity of ethyl acetate and hydro-alcoholic extracts of Momordica cymbalaria leaves was screened by agar diffusion method using Klebsiella pneumoniae (Gram positive bacteria), Escherichia coli (Gram negative bacteria) and Aspergillus niger (Fungi) as test microbes. Results: The ethyl acetate and hydro-alcoholic extracts yielded 0.5551±0.78µgmL-1 , 0.2035±0.35µgmL-1 gallic acid equivalent phenolic content and 0.6666±0.24µgmL-1 ,0.1154±0.62µgmL-1 quercetin equivalent flavonoid content per 1 mg of plant extracts respectively. Overall, both extracts showed better antioxidant activity in a concentration-dependent manner due to better oxidative stability. Amongst the extracts, ethyl acetate extract exhibited a higher percentage of free radical scavenging effects, increment of phenolic and flavonoid contents, maximum reducing power and metal chelating property. The quantitative determination of the detected phytoconstituents in the ethyl acetate extract also indicated the dominant presence of alkaloid, phenolic, flavonoid and steroid contents. The antimicrobial study reveals that the Momordica cymbalaria leaves extracts exhibited significant inhibitory activity against the test pathogens when compared with the standard. Conclusion: The output of overall results evokes that ethyl acetate extract of Momordica cymbalaria leaves can be utilized as a potential source of antioxidants. Moreover, both the extracts can also be effectively used as an antimicrobial agent to fight against harmful pathogens.

The development of bacterial resistance toward antibiotics has been led to pay attention to the antimicrobial peptides (AMPs). The common mechanism of AMPs is disrupting the integrity of the bacterial membrane. One of the most accessible targets for a-defensins human neutrophil peptide-1 (HNP-1) is lipid II. In the present study, we performed homology modeling and geometrical validation of human neutrophil defensin 1. Then, the conformational and physicochemical properties of HNP-1 derived peptides 2Abz 14 S 29 , 2Abz 23 S 29 , and HNP1DC18A, as well as their interaction with lipid II were studied computationally. The overall quality of the predicted model of full protein was À5.14, where over 90% of residues were in the most favored and allowed regions in the Ramachandran plot. Although HNP-1 and HNP1DC18A were classified as unstable peptides, 2Abz 14 S 29 and 2Abz 23 S 29 were stable, based on the instability index values. Molecular docking showed similar interaction pattern of peptides and HNP-1 to lipid II. Molecular dynamic simulations revealed the overall stability of conformations, though the fluctuations of amino acids in the modified peptides were relatively higher than HNP-1. Further, the binding affinity constant (Kd) of HNP-1 and 2Abz 23 S 29 in complex with lipid II was 10 times stronger than 2Abz 14 S 29 and HNP1DC18A. Overall, computational studies of conformational and interaction patterns have signified how derived peptides could have displayed relatively similar antimicrobial results compared to HNP-1 in the reported experimental studies. Chemical modifications not only have improved the physicochemical properties of derived peptides compared to HNP-1, but also they have retained the similar pattern and binding affinity of peptides.

Activation of the contact system has two classical consequences: initiation of the intrinsic pathway of coagulation, and cleavage of high molecular weight kininogen (HK) leading to the release of bradykinin, a potent proinflammatory peptide. In human plasma, activation of the contact system at the surface of significant bacterial pathogens was found to result in further HK processing and bacterial killing. A fragment comprising the D3 domain of HK is generated, and within this fragment a sequence of 26 amino acids is mainly responsible for the antibacterial activity. A synthetic peptide covering this sequence kills several bacterial species, also at physiological salt concentration, as effectively as the classical human antibacterial peptide LL-37. Moreover, in an animal model of infection, inhibition of the contact system promotes bacterial dissemination and growth. These data identify a novel and important role for the contact system in the defence against invasive bacterial infection.

Objective: Plant parts have been useful for food and remedies to various disease conditions for man long ago, but few have been studied for their toxicological effects. The aim of this study was to evaluate the phytochemical constituents and toxicological impacts of aqueous extract (AqE) Ziziphus mauritiana leaves on Wistar rats. Material-Method: The plant material was identified and authenticated at the harberium of Bayero University Kano and extraction were carried out by maceration. Phytochemical screening was carried-out using standard methods while administration of the extract was orally. Liver and kidney functional parameters were evaluated using standard kits and the histopathological evaluation were carried out according to the standard method. Results: Qualitative phytoconstituents screening revealed the presence of all Alkaloids, Saponin. Glycosides, tannin, flavonoids and others except anthraquinones while the quantitative screen showed phenol having the highest concentr...

The present study investigates the antibacterial activity of zebra blenny (Salaria basilisca) protein hydrolysates obtained by fermentation with a proteolytic bacterium, Bacillus mojavensis A21. The hydrolysate exhibited nutritional as well as antibacterial properties. The fermentative zebra blenny protein hydrolysate (FZPH) was fractionated by size exclusion chromatography on a Sephadex G-25 into six major fractions (F1-F6). Fraction F2, which exhibited the highest antibacterial activity against several Gram-positive and Gramnegative bacteria, was further fractionated by reversed-phase high performance liquid chromatography (RP-HPLC). The most active fractions named A and B which exhibited antibacterial activity, were analysed using nano ESI-LC-MS/MS to identify the sequences of the peptides. A total of 28 and 41 peptides, containing 8 to 31 amino acid residues, were identified in sub-fractions A and B, respectively. Further, identified peptides sharing sequences with previously identified peptides were reported. The results of this study suggest that FZPH are good source of natural antimicrobial peptides. Therefore, ZPH could be a beneficial ingredient for nutraceuticals.

Sida corymbosa plant is one of medicinal plants used in many parts of Africa, including Nigeria for the treatment of human diseases. The purpose of this work was to investigate the antioxidant effects of Sida corymbosa ethanolic leaf extract on rats administered carbon tetrachloride (CCl 4). One hundred and sixty male-rats between 170-180 g were used. They were grouped into 8 major groups (groups A-H) and 4 subgroups (A 1-H 4) in each group making it 32 subgroups of 5 rats each. The major groups comprise A (positive control-normal rats giving feed and water only and left for 7-28 d), B (negative control-those administered CCl 4 only at 0.4 ml/kgbw and left for 7-28 d), C-H (treatment groups-those administered extract before and after CCl 4 administration at 5,000, 3,000 and 1,000 mg/kgbw for 7-28 d). Antioxidant assays were determined using UV-VIS spectrophotometer (model 752g, China). Results of serum antioxidant assays done revealed that levels of serum reduced glutathione (GSH), glutathione peroxidase (GPx), catalase (CAT), supraoxide dismutase (SOD) and total antioxidant capacity (TAC) increased significantly (P<0.05) in the treatment groups from 7-28 d, when compared with the negative control. Oxidative assay carried out showed that serum malondialdehyde (MDA) levels were significantly lower (P<0.05) in treatment groups than in negative control groups. These may be suggesting that the extract may have improved the antioxidant levels of the rats. Sida corymbosa ethanolic leaf extract may, therefore, have positive effects on antioxidant status of rats administered CCl 4 .

The development of bacterial resistance toward antibiotics has been led to pay attention to the antimicrobial peptides (AMPs). The common mechanism of AMPs is disrupting the integrity of the bacterial membrane. One of the most accessible targets for a-defensins human neutrophil peptide-1 (HNP-1) is lipid II. In the present study, we performed homology modeling and geometrical validation of human neutrophil defensin 1. Then, the conformational and physicochemical properties of HNP-1 derived peptides 2Abz 14 S 29 , 2Abz 23 S 29 , and HNP1DC18A, as well as their interaction with lipid II were studied computationally. The overall quality of the predicted model of full protein was À5.14, where over 90% of residues were in the most favored and allowed regions in the Ramachandran plot. Although HNP-1 and HNP1DC18A were classified as unstable peptides, 2Abz 14 S 29 and 2Abz 23 S 29 were stable, based on the instability index values. Molecular docking showed similar interaction pattern of peptides and HNP-1 to lipid II. Molecular dynamic simulations revealed the overall stability of conformations, though the fluctuations of amino acids in the modified peptides were relatively higher than HNP-1. Further, the binding affinity constant (Kd) of HNP-1 and 2Abz 23 S 29 in complex with lipid II was 10 times stronger than 2Abz 14 S 29 and HNP1DC18A. Overall, computational studies of conformational and interaction patterns have signified how derived peptides could have displayed relatively similar antimicrobial results compared to HNP-1 in the reported experimental studies. Chemical modifications not only have improved the physicochemical properties of derived peptides compared to HNP-1, but also they have retained the similar pattern and binding affinity of peptides.

The idea of this study is based on the marvelous fact of nojirimycin and deoxy nojirimycin, naturally occurring from piperidine class and having their role as alpha glucosidase inhibitors. In the present work some hydroxyl piperidine analogues have been synthesized and analysed for their hypoglycemic effect through glucosidase inhibition owing to the structural resemblance with nojirimycin. The activity was done by spectral absorbance analysis using acarbose as standard. Two analogues (I & IV) were found to pose excellent activity having 87.4 and 54.7% inhibition respectively, hence strengthening the idea of studying piperidine analogiues as glucosidase inhibitors due to structural similarity with nojirimycin.

Food safety remains a significant challenge despite the growth and development in agricultural research and the advent of modern biotechnological and agricultural tools. Though the agriculturist struggles to aid the growing population&#39;s needs, many pathogen-based plant diseases by their direct impact on cell division and tissue development have led to the loss of tons of food crops every year. Though there are many conventional and traditional methods to overcome this issue, the amount and time spend are huge. Scientists have developed systems biology tools to study the root cause of the problem and rectify it. Host-pathogen protein interactions (HPIs) have a promising role in identifying the pathogens&#39; strategy to conquer the host organism. In this paper, the interactions between the host Rhynchophorus ferrugineus (an invasive wood-boring pest that destroys palm) and the pathogens Proteus mirabilis, Serratia marcescens, and Klebsiella pneumoniae are comprehensively studied ...

Six novel analogues were prepared by reacting benzimidazole molecules (BM and CMB) propiophenone and benzoyl chlorides respectively. The structures of newly synthesized compounds were determined with the help of spectroscopic techniques. The compounds were subjected to in-vitro screening for their activity against nematodes. It was observed that the benzimidazole (BM) derivatives possessed more nematicidal activity as compared to that of cyanomethyl-benzimidazole (CMB) for Meloidogyne incognita. Among them, the propiophenone substituted benzimidazole derivative B3 was found to be the most active compound and can be further studied as lead molecule for development of anthelmintic drugs.

Recent studies have highlighted the necessity to thoroughly evaluate medicinal plants due to their therapeutic potential. The current study delves into the phytochemical profile, antioxidant capacity, and hepatoprotective effect of Andrographis paniculata. The investigation specifically targets its effectiveness in mitigating liver dysfunction induced by carbon tetrachloride (CCl4) in Wistar albino rats, aiming to uncover its promising role as a natural remedy for liver-related ailments. A. paniculata leaf extract was screened for phytoconstituents and antioxidant and hepatoprotective effects in Wistar albino rats against CCl4-induced liver dysfunction. Phytochemical analysis revealed the presence of flavonoids, alkaloids, and phenolic compounds in all extracts. The phenolic concentration ranged from 10.23 to 19.52 mg gallic acid per gram of the sample, while the highest flavonoid concentration was found in the ethanol fraction (8.27 mg rutin equivalents per gram). The antioxidant a...

The development of bacterial resistance toward antibiotics has been led to pay attention to the antimicrobial peptides (AMPs). The common mechanism of AMPs is disrupting the integrity of the bacterial membrane. One of the most accessible targets for a-defensins human neutrophil peptide-1 (HNP-1) is lipid II. In the present study, we performed homology modeling and geometrical validation of human neutrophil defensin 1. Then, the conformational and physicochemical properties of HNP-1 derived peptides 2Abz 14 S 29 , 2Abz 23 S 29 , and HNP1DC18A, as well as their interaction with lipid II were studied computationally. The overall quality of the predicted model of full protein was À5.14, where over 90% of residues were in the most favored and allowed regions in the Ramachandran plot. Although HNP-1 and HNP1DC18A were classified as unstable peptides, 2Abz 14 S 29 and 2Abz 23 S 29 were stable, based on the instability index values. Molecular docking showed similar interaction pattern of peptides and HNP-1 to lipid II. Molecular dynamic simulations revealed the overall stability of conformations, though the fluctuations of amino acids in the modified peptides were relatively higher than HNP-1. Further, the binding affinity constant (Kd) of HNP-1 and 2Abz 23 S 29 in complex with lipid II was 10 times stronger than 2Abz 14 S 29 and HNP1DC18A. Overall, computational studies of conformational and interaction patterns have signified how derived peptides could have displayed relatively similar antimicrobial results compared to HNP-1 in the reported experimental studies. Chemical modifications not only have improved the physicochemical properties of derived peptides compared to HNP-1, but also they have retained the similar pattern and binding affinity of peptides.

Background: The current study focuses on the preliminary phytochemical analysis, antioxidant potential and identification of phytochemicals in Ardissia solanacea leaves extract using chromatography and HR-MS. Materials and Methods: The occurrence of phytoconstituents in different extracts of Ardissia solanacea were assessed by standard procedures. In vitro antioxidant potential was determined by Hydrogen peroxide and DPPH method. The extract was fractionated by Flash Chromatography. The fractions were analysed using HPTLC and further analyzed by HR-MS method to detect and characterize the active phytoconstituents present in it. Results: The highest concentration of flavonoids (371.91± 0.167 mg/g of Quercetin Equivalent), phenolics (10.138±0.010 mg/g of Gallic acid Equivalent) and tannins (148.23±0.510 mg/g of Tannic acid Equivalent) was observed in the ethanol extract. The antioxidant activity by DPPH and H 2 O 2 assay demonstrated that the ethanolic extract (AsEt) showed highest anti-oxidant potential (74.21% and 83.16% respectively). The ASEt was fractionated by using Flash chromatography. As a result, Out of 11 fractions, one fraction namely AsEt3 was selected further based on HPTLC results. The HR-MS analysis of ASEt3 indicated presence of thirteen compounds wherein bergapten was predominantly identified. Conclusion: It was revealed that the leaves of Ardissia solanacea possesses high antioxidant potential. The known phytoconstituents namely quercetin and taxifolin along with one unknown compound were identified through the HR-MS study. Using mass library data, we report herein 2 flavonoids and 1 phenolic in the AsEt extract.

Collagen-derived cryptic peptides (cryptides) are biologically active peptides derived from the proteolytic digestion of collagen protein. These cryptides possess a multitude of activities, including antihypertensive, antiproliferative, and antibacterial. The latter, however, has not been extensively studied. The cryptides are mainly obtained from the protein hydrolysate, followed by characterizations to elucidate the function, limiting the number of cryptides investigated within a short period. The recent threat of antimicrobial resistance microorganisms (AMR) to global health requires the rapid development of new therapeutic drugs. The current study aims to predict antimicrobial peptides (AMP) from collagen-derived cryptides, followed by elucidating their potential to inhibit biofilm-related precursors in Klebsiella pneumoniae using in silico approach. Therefore, cryptides derived from collagen amino acid sequences of various types and species were subjected to online machine-learning platforms (i.e., CAMPr3, DBAASP, dPABBs, Hemopred, and ToxinPred). The peptide-protein interaction was elucidated using molecular docking, molecular dynamics, and MM-PBSA analysis against MrkH, a K. pneumoniae's transcriptional regulator of type 3 fimbriae that promote biofilm formation. As a result, six potential antibiofilm inhibitory cryptides were screened and docked against MrkH. All six peptides bind stronger than the MrkH ligand (c-di-GMP; C2E).

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Cassia fistula L. (Caesalpinioideae), a very common plant known for its medicinal properties is a semi wild Indian Labernum Known as the golden shower tree [1]. It has great therapeutic implication in India system of medicine. The extracts derived from different parts of this plant have anti-bacterial, antipyretics, analgesic, anti-inflammatory and hypoglycemic properties and are used in the treatment of various disorders such as haematemesis, rheumatism, skin diseases , eye and liver ailments 2-4. It is also one of the ingredients of the preparations known as pilex, Purian for piles and detoxifier respectively 5. Phytochemical investigation of crude plant extracts shown the presences of bioactive principles in the plant parts like flowers, roots, fruits, seeds, leaves and barks etc. Phytochemical are non-nutritive plant chemicals that have protective or disease preventive properties. Various parts of this plants are known to be important sources of secondary metabolites mainly phenolic compounds such as epicatechin, procyanidin, biflavonoids, rhein glycosides, from the leaves 6-7 kaempferol, alkaloids, triterpenes from the flower 8 and lupeol, Beta-sitosterol,

Recent studies have highlighted the necessity to thoroughly evaluate medicinal plants due to their therapeutic potential. The current study delves into the phytochemical profile, antioxidant capacity, and hepatoprotective effect of Andrographis paniculata. The investigation specifically targets its effectiveness in mitigating liver dysfunction induced by carbon tetrachloride (CCl4) in Wistar albino rats, aiming to uncover its promising role as a natural remedy for liver-related ailments. A. paniculata leaf extract was screened for phytoconstituents and antioxidant and hepatoprotective effects in Wistar albino rats against CCl4-induced liver dysfunction. Phytochemical analysis revealed the presence of flavonoids, alkaloids, and phenolic compounds in all extracts. The phenolic concentration ranged from 10.23 to 19.52 mg gallic acid per gram of the sample, while the highest flavonoid concentration was found in the ethanol fraction (8.27 mg rutin equivalents per gram). The antioxidant a...

Objective: This study aimed to investigate the antioxidants and free radicals scavenging properties of ethanolic extracts from Tribulus terrestris fruit (TTF) and Mesua ferrea flower (MFF). Methods: The antioxidant and free radical scavenging activities were measured by using standard protocols against phytoextracts used at 50, 100, 150, 200 and 250 µg/ml concentration. Total phenolic and flavonoid content were estimated using Folin-Ciocalteu and aluminium-chloride reagent assay methods. Results: Among the extracts, MFF showed the highest total antioxidant ability followed by TTF. With regard to various scavenging activities, MFF had the highest radical scavenging activity than TTF extract closely resembled the standards. Also, the reducing capacity on ferrous ion was high in MFF than TTF. The quantified phenolic contents of TTF and MFF ethanolic extracts were 27.0±0.36 and 57.0±0.32 mg gallic acid equivalent per gram extract respectively. A positive correlation (p value<0.001) was observed between phenolic content and free radical scavenging efficiencies. Conclusion: The results confirm that both MFF and TTF are important sources of natural antioxidants and serves as an effective free radical scavengers and/or inhibitors. Hence, both extracts are suitable plant-based pharmaceutical products can be used to handle 'free radical-mediated diseases.

Objectives: This study aims to evaluate the enzymic antioxidants and free radical scavenging present in the ethanolic leaf extracts of Crescentia cujete. Methods: Enzymic antioxidants such as superoxide dismutase (SOD), catalase (CAT), glutathione reductase, glutathione peroxidase, and glutathione S-transferase (GST) were estimated by standard methods. Free radical scavenging potential was evaluated by diphenylpicrylhydrazyl (DPPH), nitric oxide, and hydroxyl radical methods using an ethanolic extract of C. cujete leaf. Results: The leaf extract of C. cujete showed the maximum activity of CAT, SOD, GST, glutathione reductase, and peroxidase activity. CAT activity was formed to be highest in the ethanolic extract of C. cujete leaf. DPPH radical scavenging activity was reported as 38.5 µg/ml, nitric oxide was found to be 200.77 µg/ml, and hydroxyl radical scavenging exhibited 108.42 µg/ml normalized with ascorbic acid. Conclusion: From the results, it has concluded that the ethanol extract of the C. cujete leaf has a prospective source of natural antioxidant that would be a great significance as therapeutic agents in preventing or slowing the progress of reactive oxygen species and related oxidative stress-related degenerative diseases.

Abstract: Medicinal plants play an important role in folk medicine, and different plant species have been used in the treatment of many diseases. The plant species Plumbago zeylanica (known vernacularly as chitarak) of the family Plumbaginaceae is distributed as a perennial herb ...

Nasal dosage forms (nasal preparations) are traditionally used for local drug delivery, often for cold and flu symptoms&#39; therapy. Apart from conventional dosage forms such as nasal drops, ointments and gels and aqueous nasal products, nasal sprays are even more frequently used, where the active pharmaceutical ingredient can, depending on its solubility, be formulated as a solution or suspension (liquid sprays), or as nasal powders, and the judicious choice of packing material, i.e. the applicator (delivery device) is stressed. When about to formulate nasal sprays, apart from the choice of appropriate excipients, one should take care about the pump/dozer characteristics, dose uniformity, particle size and size distribution in bulk (in nasal suspensions and powders), but also during the application (nasal aerosol), mode of content dispensing, weight loss (stability), possible content leakage… Besides the local effect, intranasal application is being immensely explored as a potenti...

The antioxidant activity within the body has been well correlated with the body's defense mechanism against toxic free radicals. Alcohol ingestion increases the generation of free radicals. The present study was conducted to assess antioxidant potential of seed extract of Ziziphus mauritiana, which was standardized with HPLC. DPPH assay and Fenton reaction system was applied to assess free radical scavenging potential. The Swiss albino mice were used to evaluate the inhibitory activity of extract on oxidative stress induced by alcohol. The animals were treated with graded doses of extract (100-400 mg/kg body weight) before the administration of alcohol. After 6 weeks animals were sacrificed and their livers were assessed for catalase, superoxide dismutase, glutathione and lipid peroxidation. The results indicated that the extract of Ziziphus mauritiana potentially scavenged the free radicals in a concentration-dependent manner. The pretreatment of animals with Ziziphus mauritiana extract inhibited lipid peroxidation significantly, and increased the levels of reduced glutathione, catalase activity and superoxide dismutase in all extract treated groups (p<0.05) as compared to alcohol treated groups. The plant provides protection against the induction of oxidative stress by alcohol either by converting free radicals into stable products or by strengthening the antioxidant system.

An antimicrobial substance producing strain designated as A52 was isolated from a marine sediment sample and identified as Bacillus sp., based on 16S rRNA gene sequence analysis. The ANI and dDDH analysis of the genome sequence displayed high identity with two strains of B. subtilis sub sp. subtilis. Strain A52 yielded two antimicrobial peptides (AMPs) that differed in activity spectrum. MALDI mass spectrometry analysis of HPLC purified fractions revealed mass of peptides as 3881.6 and 1061.9 Da. The antiSMASH analysis of genome sequence unraveled presence of identical biosynthetic cluster involved in production of sublancin from B. subtilis sub sp. subtilis strain 168, which yielded peptide with identical mass. The low molecular weight peptide is found to be a cyclic lipopeptide containing C 16 β-hydroxy fatty acid that resembled surfactin-like group of biosurfactants. However, it differed in fatty acid composition and antimicrobial spectrum in comparison to other surfactins produced by strains of B. subtilis. It exhibited broad spectrum antibacterial activity, inhibited growth of pathogenic strains of Candida and filamentous fungi. Further, it exhibited hemolytic activity, but did not show phytotoxic effect in seed germination experiment. The emulgel formulation of surfactin-like lipopeptide showed antimicrobial activity in vitro and did not show any irritation effects in animal studies using BALB/c mice. Moreover, surfactin-like lipopeptide displayed synergistic activity with fluconazole against Candida, indicating its potential for external therapeutic applications.

Corona is an avian and mammalian Ribovirus which generally evade host immune mechanism hampering respiratory tract of the host. Structurally it has an envelope of protein enclosing a single-stranded positively coiled RNA genome. Coronavirus uses around 4-5 different classes of protein for its replication in the host cell. Due to the high mutation rate of the viral genome development of a vaccine against corona has been a difficult task. In the current scenario, the world is facing a problem with CoViD-19 as the biggest pandemic. Several combinations of drugs like Hydroxychloroquine, Plaquine, Chloroquine, etc. targeting viral protein have been utilized for controlling viral infection. The possibility of insect brain proteins was checked against the selected non-structural proteins of CoViD-19 that take an active role in the replication of the virus in the host. Molecular docking methodology plays an important role in predicting interaction between the insect proteins with non-structural protein (nsp) of coronavirus. The results predict good bonding affinity with possible interaction as hydrogen bond and salt bridge between antibacterial protein and nsp of CoViD-19 indicating as afuture alternative medications.

Secretion from female reproductive accessory glands of the dipteran Ceratitis capitata was found to have antibacterial properties against E. coll. At least two basic polypeptides with mol. wt 15.5 and 4.7 kDa respectively, were identified as responsible for such activity. Furthermore, the 15.5 kDa protein is active against a number of Gram-positive and-negative bacterial strains. Lysozyme activity is also present in the secretion.

Daniellia oliveri is one of the most extensively utilized medicinal plants in Nigeria and some West African countries for the treatment of various ailments. In the present study, the GC-MS profiles and effect of ethanolic extracts of stem bark and leaves of Daniellia oliveri on lipid peroxidation, Na+/K+-ATPase activity and thiols status in H2O2 and Fe2+ (fenton reaction) assaulted cerebral and hepatic tissue homogenates was investigated. The stem bark and leaves were extracted with absolute ethanol for 72hrs and concentrated in a rotary evaporator. Wistar rats were euthanized and the brains and livers were removed, homogenized, centrifuged and the supernatants were used for lipid peroxidation, Na+/K+-ATPase activity, and thiol assays in the presence of prooxidants (1mM H2O2 or 10μM Fe2+ or H2O2 and Fe2+).The results revealed that ethanol extract of both the leaf and stem-bark inhibited lipid peroxidation induced by H2O2, Fe2+ and combination of H2O2 and Fe2+ and this was evident in...

1Laboratory of Food Science and Technology, Food and Nutrition Division, University of Calcutta, Kolkata-700 027, West Bengal, India 2Department of Conservation Biology, Durgapur Government College, Kazi Nazrul University, Durgapur-713 214, West Bengal, India 3Department of Biochemistry, University of Calcutta, Kolkata-700 019, West Bengal, India 4Division of Bacteriology, National Institute of Cholera and Enteric Disease (NICED), Beliaghata, Kolkata-700 010, West Bengal, India

In the study of designing pharmacophore models for analgesic, a series of 4-[4-chloro-3-(tri uoromethyl)-phenyl]-4-piperidinol (TFMP) derivatives were synthesized and characterized by physical and spectral method (HR-EIMS, HR-FABMS, 1 H-NMR, 13 C-NMR, UV, and FT-IR). The analgesic action of the synthesized derivatives was estimated by means of Hot Plate Method. Most of the compounds displayed potent analgesic e cacy and an ultrashort to long duration of action. The results indicate that these compounds are useful as analgesics. Qualitatively nine compounds resemble morphine in pharmacological action, whereas three derivatives are devoid of any signi cant analgesic potential. In conclusion, among active compounds (188%), 5 (137%), 6 (162%), and 8 (107%) respectively emerged as most effective analgesic and they depressed peripheral and centrally mediated pain by opioid dependent and independent systems.