Inhibition Of Bacterial Activity Research Articles

Antibacterial activity of ethyl acetate extract of endophytic fungus (Paraconiothyrium brasiliense) through targeting dihydropteroate synthase (DHPS)

Endophytic fungi are innumerable sources of bioactive metabolites with various biomedical applications. Hence, this study was aimed to isolate and identify the endophytic fungus Paraconiothyrium brasiliense (PB) from the fruit of Capsicum annuum and evaluated their biochemical, antimicrobial, antioxidant, cell viability, and cytotoxicity behavior. Results showed that ethyl acetate extract (EAE) of PB contains flavonoid (31.53 ± 0.9 mg of QE/g of extract) and phenolic (2.59 ± 0.06 mg of GAE/g of extract). The PB-EAE showed significant antioxidant activity in terms of free radicals (DPPH, ABTS, and Fe3+) scavenging. The antioxidant potential of PB-EAE reflects in normal cell viability and anticancer activity against prostate cancer (PC3) cells. The bacterial inhibitory activity of PB-EAE was equal to commercial antibiotic tetracycline hydrochloride (TCH). Further, GC–MS analysis confirmed the presence of volatile molecules such as o-cymene (CH3C6H4CH(CH3)2), dipentene (C10H16), γ-terpinene (C10H16), 4-carvomenthenol (C10H18O), heneicosane (CH3(CH2)19CH3), and 2,5-piperazinedione (C4H6N2O2). Also, molecular docking analysis demonstrated the significant interactions between the compounds of PB-EAE with dihydropteroate synthase (Protein ID:5JQ9; DHPS). This study revealed that endophytic P. brasiliense could be a novel source for isolation of antimicrobials.

Antimicrobial Activity and Action Mechanisms of Arg-Rich Short Analog Peptides Designed from the C-Terminal Loop Region of American Oyster Defensin (AOD).

American oyster defensin (AOD) was previously purified from acidified gill extract of the American oyster, Crassostrea virginica. AOD is composed of 38 amino acids with three disulfide bonds and exhibits strong antimicrobial activity against Gram-positive bacteria as well as significant activity against Gram-negative bacteria. Here, to develop promising peptides into antibiotic candidates, we designed five arginine-rich analogs (A0, A1, A2, A3, and A4), predicted their loop and extended strand/random structures—including nine amino acids and a disulfide bond derived from the C-terminus of AOD—and described their antimicrobial and cytotoxic effects, as well as their modes of action. In our experimental results, the A3 and A4 analogs exhibited potent antimicrobial activity against all test organisms—including four Gram-positive bacteria, six Gram-negative bacteria, and Candida albicans—without cell toxicity. A sequence of experiments, including a membrane permeabilization assay, DNA binding study, and DNA polymerization inhibition test, indicated that the two analogs (A3 and A4) possibly did not act directly on the bacterial membrane but instead interacted with intracellular components such as DNA or DNA amplification reactions. AOD analogs also showed strong bacterial inhibition activity in the plasma environment. In addition, analog-treated microbial cells clearly exhibited membrane disruption, damage, and leakage of cytoplasmic contents. Collectively, our results suggest that two analogs, A3 and A4, have potent antimicrobial activity via DNA interaction and have the potential for development into novel antimicrobial agents.

Bacterial Inhibition and Antioxidant Activity of Probiotic Yoghurt Developed Using Microbial Isolates from Soymilk

The aim of this study was to investigate the bacterial inhibition and antioxidant activities of probiotic yoghurts developed using microbial isolates from Soymilk. Bacterial inhibitory activity of yoghurt was evaluated against Staphyloccocus aureus, Bacillus subtillis, Escherichia coli and Pseudomonas flourescens by using the disk diffusion method. The yoghurt showed some inhibitory activities against all the organisms tested. Antioxidant activity of yoghurt was measured using three different methods- Diphenyl-1-picryl hydroxyl (DPPH) radical scavenging activity, lipid peroxidase assay and hydroxyl radical scavenging activity against Butylated hydroxyanisole (BHA) as standard. The results showed that probiotic yoghurt exhibits relative high antioxidant activities as compare to BHA. However, by implications this study suggests that probiotic yoghurt has some inhibitory activities against all the bacteria tested, also can be consider among the most promising functional foods for their antioxidant activity and ability to prevent oxidative damage and attendant ageing.

The Antimicrobial Activity of Silver Nanoparticles in Ag/Ag2O Composites Synthesized by Oxygen Plasma Treatment of Silver Thin Films

In this work, Ag/Ag2O composites were synthesized by treating silver thin films manufactured by thermal evaporation method with oxygen plasma afterglow. In order to verify the antibacterial behavior of these composites, inhibition zone tests were realized for Staphylococcus aureus. The results showed that individual silver nanoparticles at concentrations that can be controlled by the stoichiometric ratios of the Ag/Ag2O composites, were the main factor in the inhibition of bacteria. In addition, we found that the degree of degradation of individual silver nanoparticles absorption peaks represented a suitable criterion for determining the bacterial inhibition activity of the prepared silver oxide films. The results also showed that the sample treated at 1000 watts gave the highest rate of bacterial inhibition. This research includes an attempt to correlate the bacterial inhibition activity of silver oxide thin films with the structural and spectroscopic properties of these films.

Comparing the Effect of Different Antibiotics in Frozen-Thawed Ram Sperm: Is It Possible to Avoid Their Addition?

It is crucial to perform a deep study about the most extensively used antibiotics in sperm extenders. Most of the protocols and concentrations used in ram are direct extrapolations from other species. It is important to establish species-specific antibiotic treatments to optimize their use and if it is possible to reduce the quantity. Previews studies have assessed some aspects of sperm quality in vitro, but this study aimed to go further and assess the effect of three different antibiotic treatments, which are the most extensively used, not only in sperm quality or assessing the inhibitory effect on bacterial growth but also assessing these important parameters of productivity such as fertility, prolificacy, fecundity, and sex-ratio during a freeze-thaw process. Gentamicyn (G) treatment showed the worst results, not only concerning sperm quality but also in the reproductive trials exhibiting a toxical effect at the experiment concentration, and being the most powerful inhibiting bacterial growth. For its part, Lincomicyn-spectinomycin (LS) showed similar results inhibiting bacterial growth but it did not show a detrimental effect either in sperm quality or in reproductive parameters. Penicillin-streptomycin (PS) showed good results in the sperm quality and in the reproductive in vivo trials, but it showed a very poor effect inhibiting bacterial growth probably due to some kind of antibiotic resistance. According to our results, there is not a significant positive relationship between the higher bacterial inhibitory activity of LS and PS samples, and the sperm quality respect Control samples (without antibiotics). In the case of G, which exhibited the most effective as antibacterial, we observed a toxic effect on sperm quality that could be translated on productivity parameters. Our results suggest that the bacterial contamination control in frozen-thawed semen may be possible without the use of antibiotics, although the effects of longer periods of cooling storage and different temperatures of storage need to be further investigated for animal semen. At this point, a reflection about a drastic reduction in the use of antibiotic treatments in sperm cryopreservation is mandatory, since freezing conditions could keep sperm doses contamination within the levels recommended by regulatory health agencies.

Fabrication and Bacterial Inhibitory Activity of Essential Oil Linalool Loaded Biocapsules Against Escherichia Coli

Fabrication and Bacterial Inhibitory Activity of Essential Oil Linalool Loaded Biocapsules Against Escherichia Coli

SKRINING FITOKIMIA DAN UJI AKTIVITAS ANTIBAKTERI EKSTRAK ETANOL BULU BABI (Diadema setosum) TERHADAP PERTUMBUHAN Staphylococcus aureus DI PERAIRAN DESA PELAUW

Sea urchin (Diadema setosum) is an aquatic biota that has high nutritional value. Bioactive compounds produced by sea urchins have the potential to be used as natural antibacterial compounds. This study aims to identify chemical compounds and determine the antibacterial activity of ethanol extract of sea urchins (Diadema setosum) against the growth of Staphylococcus aureus bacteria. The research method used is the agar diffusion method. The results of phytochemical screening of sea urchin extract (Diadema setosum) showed the presence of alkaloids and saponins. By using variations in the concentration of ethanol extract of sea urchin (Diadema setosum) at a concentration of 80% it had an inhibitory power of 18 mm, a concentration of 90% had an inhibitory power of 23 mm, a concentration of 100% had an inhibitory power of 28 mm and for a concentration of 110% had an inhibitory power of 35 mm. The positive control has a resistance of 30 mm and the negative control is 0 mm. The results showed that the ethanol extract of sea urchins (Diadema setosum) had a strong bacterial inhibitory activity against Staphylococcus aureus bacteria.

Bacterial biofilm inhibition activity of ethanolic extract of Hemidesmus indicus

Multi-drug resistance is one of the biggest nightmares in the field of healthcare today. Adding on to this, some bacteria like Staphylococcus aureus and Pseudomonas aeruginosa have the ability to form biofilms. These essentially are large colonies of bacteria that are held together by polysaccharides and other biomolecules which in turn facilitate in their adherence to solid substrate – both natural and synthetic. This further creates a life-threatening implication leading to nosocomial infections like pneumonia, Urinary tract infections (UTI), etc. increasing the co-morbidities and mortality of critically-ill patients. The combination of antimicrobial resistance, ability to form biofilms and threat of nosocomial infections calls for a need to investigate newer, safer alternatives. Plant based medicaments have been used for centuries and they are a great alternative to synthetic drugs. In the present study, ethanolic extracts of Hemidesmus indicus was evaluated against clinically-important multi-drug resistant organisms. Percentage biofilm inhibition of plant extracts of Hemidesmus indicus by crystal violet assay method. Triplicate analysis was done and data obtained was statistically interpreted using Microsoft Excel. Alcoholic extracts of Hemidesmus indicus exhibited significant biofilm inhibitory activity against the common bacteria Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis. Further, isolation of the chief active constituent responsible for Anti-biofilm activity is in process.

In vitro antimicrobial and antipro-inflammation potential of honokiol and magnolol against oral pathogens and macrophages

Honokiol and magnolol are natural components isolated from Magnolia bark that is used in traditional Chinese and Japanese herbal medicine. These two isomers are used as a component of dietary supplements and cosmetic products. In this study, we investigated the antimicrobial effect of honokiol and magnolol on pathogens causing oral diseases, their mechanism of action in biofilm formation and drug resistance of oral pathogens, and inflammatory regulation in mammalian cells. We determined the minimum inhibitory concentration and minimum bactericidal concentration of honokiol and magnolol, and their stability at different temperatures and pH. We also evaluated their effect on biofilm formation, antibiotic-resistance gene expression in MRSA, and pro-inflammatory gene expression in mammalian cells. Honokiol showed better antimicrobial activity than magnolol. Both honokiol and magnolol showed stable bacterial inhibitory activity over a wide range of temperature and pH, reduced biofilm formation, and antibiotic resistance in oral pathogens. The biofilm formation- and antibiotic resistance-related gene expression was consistent with the respective phenotypes. Furthermore, these two isomers repressed the expression of pro-inflammatory genes in RAW264.7cells. Our study provides evidence of the potential application of honokiol and magnolol in dental medicine to cure or prevent oral diseases.

Biosynthesis, Characterization, and Biological Activities of Procyanidin Capped Silver Nanoparticles.

In this study, procyanidin dimers and Leucosidea sericea total extract (LSTE) were employed in the synthesis of silver nanoparticles (AgNPs) and characterized by ultraviolet-visible (UV-Visible) spectroscopy, high-resolution transmission electron microscopy (HRTEM), selected area electron diffraction (SAED), X-ray diffraction (XRD), and dynamic light scattering (DLS) techniques. AgNPs of about 2–7 nm were obtained. DLS and stability evaluations confirmed that the AgNPs/procyanidins conjugates were stable. The formed nanoparticles exhibited good inhibitory activities against the two enzymes studied. The IC50 values against the amylase enzyme were 14.92 ± 1.0, 13.24 ± 0.2, and 19.13 ± 0.8 µg/mL for AgNPs coordinated with LSTE, F1, and F2, respectively. The corresponding values for the glucosidase enzyme were 21.48 ± 0.9, 18.76 ± 1.0, and 8.75 ± 0.7 µg/mL. The antioxidant activities were comparable to those of the intact fractions. The AgNPs also demonstrated bacterial inhibitory activities against six bacterial species. While the minimum inhibitory concentrations (MIC) of F1-AgNPs against Pseudomonas aeruginosa and Staphylococcus aureus were 31.25 and 15.63 µg/mL respectively, those of LSTE-AgNPs and F2-AgNPs against these organisms were both 62.50 µg/mL. The F1-AgNPs demonstrated a better bactericidal effect and may be useful in food packaging. This research also showed the involvement of the procyanidins as reducing and capping agents in the formation of stable AgNPs with potential biological applications.

Structural basis of quinolone derivatives, inhibition of type I and II topoisomerases and inquiry into the relevance of bioactivity in odd or even branches with molecular docking study

The structural modification of quinolone derivatives has been a hot spot in recent years, especially the modification of the N-1 position, which is the part that this article focuses on. In this paper, series of synthesized quinoline quaternary ammonium salts with odd and even carbon number alkyl groups in N-1 position were used to explain the influence of the alkyl side chain on activity. With respect to all the recently synthesized twenty products, the biological activity results exhibited significant antitumor and antibacterial activity with obvious differences in the target alkyliodine substituted compounds and the antibacterial activities apparently had the prominent odd-carbon number predominance. Compound 8-((4-(benzyloxy)phenyl)amino)-7-(ethoxycarbonyl)-5-propyl-[1,3]dioxolo[4,5-g]quinolin-5-ium (4d) was found to be the most potent derivative with IC50 values of 4 ± 0.88, 4 ± 0.42, 14±1.96, and 32±3.66 against A-549, Hela, SGC-7901, and L-02 cells, respectively, stronger than the positive control 5-FU and MTX. Furthermore, it had the most potent bacterial inhibitory activity of MIC value against E. coli (ATCC 29213) and Staphylococcus aureus (ATCC 8739) at 3.125 nmol mL−1. With respect to molecular simulations, in order to illustrate the possible mechanism of the difference between the series of compounds in the even or odd carbon chain alkyliodine substitution, this paper simulated the conceivable mode and explained the main interactions. Finally, we could find that the position and proportion of hydrogen bonds and other interactions in each series were regarded as the main reasons for this difference in activity.

Induction of Antibacterial Metabolites by Co-Cultivation of Two Red-Sea-Sponge-Associated Actinomycetes Micromonospora sp. UR56 and Actinokinespora sp. EG49.

Liquid chromatography coupled with high resolution mass spectrometry (LC-HRESMS)-assisted metabolomic profiling of two sponge-associated actinomycetes, Micromonospora sp. UR56 and Actinokineospora sp. EG49, revealed that the co-culture of these two actinomycetes induced the accumulation of metabolites that were not traced in their axenic cultures. Dereplication suggested that phenazine-derived compounds were the main induced metabolites. Hence, following large-scale co-fermentation, the major induced metabolites were isolated and structurally characterized as the already known dimethyl phenazine-1,6-dicarboxylate (1), phenazine-1,6-dicarboxylic acid mono methyl ester (phencomycin; 2), phenazine-1-carboxylic acid (tubermycin; 3), N-(2-hydroxyphenyl)-acetamide (9), and p-anisamide (10). Subsequently, the antibacterial, antibiofilm, and cytotoxic properties of these metabolites (1–3, 9, and 10) were determined in vitro. All the tested compounds except 9 showed high to moderate antibacterial and antibiofilm activities, whereas their cytotoxic effects were modest. Testing against Staphylococcus DNA gyrase-B and pyruvate kinase as possible molecular targets together with binding mode studies showed that compounds 1–3 could exert their bacterial inhibitory activities through the inhibition of both enzymes. Moreover, their structural differences, particularly the substitution at C-1 and C-6, played a crucial role in the determination of their inhibitory spectra and potency. In conclusion, the present study highlighted that microbial co-cultivation is an efficient tool for the discovery of new antimicrobial candidates and indicated phenazines as potential lead compounds for further development as antibiotic scaffold.

Design, Synthesis, and Dual Evaluation of Quinoline and Quinolinium Iodide Salt Derivatives as Potential Anticancer and Antibacterial Agents.

A series of novel quinoline and quinolinium iodide derivatives were designed and synthesized to discover potential anticancer and antibacterial agents. With regard to anticancer properties, in vitro cytotoxicities against three human cancer cell lines (A-549, HeLa and SGC-7901) were evaluated. The antibacterial properties against two strains, Escherichia coli (ATCC 29213) and Staphylococcus aureus (ATCC 8739), along with minimum inhibitory concentration (MIC) values were evaluated. The target alkyliodine substituted compounds exhibited significant antitumor and antibacterial activity, of which compound 8-((4-(benzyloxy)phenyl)amino)-7-(ethoxycarbonyl)-5-propyl-[1,3]dioxolo[4,5-g]quinolin-5-ium (12) was found to be the most potent derivative with IC50 values of 4.45±0.88, 4.74±0.42, 14.54±1.96, and 32.12±3.66 against A-549, HeLa, SGC-7901, and L-02 cells, respectively, stronger than the positive controls 5-FU and MTX. Furthermore, compound 12 had the most potent bacterial inhibitory activity. The MIC of this compound against both E. coli and S. aureus was 3.125 nmol ⋅ mL-1 , which was smaller than that against the reference agents amoxicillin and ciprofloxacin.

BMP2-loaded titania nanotubes coating with pH-responsive multilayers for bacterial infections inhibition and osteogenic activity improvement.

Bacterial infection and surface biointertness are two main causes for titanium (Ti)-based orthopedic implants failure. To improve the antibacterial ability and enhance poor osteogenic property of Ti substrates, in this work, we employed titania nanotubes (TNTs) as Bone Morphogenetic Protein 2 (BMP2) carrier, and a pH-responsive multilayer film composed of alginate dialdehyde-gentamicin (ADA-Gen) and chitosan (Chi) was constructed onto BMP2-loaded TNTs substrates through layer-by-layer (LBL) assembly technique, resulting in TNT-BMP2-LBLg samples. The release experiments revealed that acidic environment could trigger the release of Gen from the multilayer films and in turn accelerate the release of BMP2 from TNTs. Moreover, antibacterial assay against E. coli and S. aureus confirmed that the TNT-BMP2-LBLg had excellent antibacterial capacity both in early (6 h) and in long-term (72 h). Meanwhile, in vitro cellular tests demonstrated that TNT-BMP2-LBLg had good cytocompatibility toward osteoblasts even co-cultured with S. aureus. Importantly, the obtained TNT-BMP2-LBLg promoted differentiation of osteoblasts, including enhanced alkaline phosphatase activity, improved mineralization capability and stimulated osteogenic-relative gene expression. This study thus provides a promising strategy to develop pH-responsive antibacterial and enhance bone integrative Ti-based implants for potential orthopedic application.

Synthesis of bio-surfactant based Ag/ZnO nanoparticles for better thermal, photocatalytic and antibacterial activity

Abstract In recent years, synthesis of nanoparticles using natural materials is the essential constituent in the medicinal and clinical laboratory due to inexpensive, recyclable and without use of toxic chemicals. In this present work, SW-Ag/ZnO nanoparticles were synthesized by simple in situ chemical precipitation approach. Padina gymnospora was taken as a bio-surfactant material for preparing Ag nanoparticles and these are further intercalated with ZnO particles. The synthesized nanoparticles were charecterized and confirmed by Fourier transform infra-red spectroscopy, X-ray diffraction analysis, UV–Visible Diffuse reflectance spectroscopy, High resolution scanning electron microscopy and Transmission electron microscopy techniques. The SW-Ag/ZnO was appeared in large clusters with different shaped particles, the size of them was obtained in 14–40 nm. Seaweed capped Ag/ZnO particles showed the greater UV protection values achieved the 45.2% than RSW and SW-Ag. Thermal degradation characteristics of SW-Ag/ZnO have greater thermal stability than RSW and SW-Ag nanoparticles. Moreover, the photocatalytic degradation performances of nanoparticles were tested under the sunlight irradiation using phenol pollutants. Their photocatalytic degradation reaction was well fitted with the first order reaction kinetics. In addition, the antimicrobial activity of nanoparticles was also tested against (Gram (+ve) and Gram (-ve) microbial pathogens and it could be exhibited the higher bacterial inhibition activity obtained for SW-Ag/ZnO than that of RSW and SW-Ag nanoparticles.

Inhibiting effect of textile wastewater on the activity of sludge from the biological treatment process of the activated sludge plant.

Textile industry represents an important source of toxic substances rejected in environment. Indeed, effluent of these industries contains dyes and chemicals. They are rejected in environment without any treatment. The aim of this work is to evaluate ecotoxicological effect of industrial textile effluents on the sludge harvested from activated sludge treatment plant of Marrakech city (Morocco). For this, we are interested in determining the inhibition condition that corresponds to 50% decrease of bacterial activity in sludge. Obtained results showed that inhibition percentage of bacterial activity depends narrowly on contact time and on added effluent volume, until a limit concentration where there is no degradation of substratum. In fact, substratum degradation speed shows about 65 times decrease when 80% (v/v) of textile wastewater is added, in comparison with the controlled one. Consequently the inhibition constant (Ki) that corresponds to 50% of bacterial inhibition activity is estimated to 0.65 mg l−1 of dye. These studies confirm a real ecotoxicological risk of these effluents. Therefore, a treatment is mandatory before their rejection in environment.

Efficient microwave‐assisted synthesis of glycerol monodecanoate

Solvent‐free microwave‐assisted synthesis was carried out to prepare 2,3‐dihydroxypropyl decanoate, by esterification of decanoic acid in the presence of two distinct glycerol derivatives, glycidol, and glycerol carbonate, respectively. The process described is based on microwaves heating source with electrical power in the range of 200–400 W, involving stoichiometric proportions of decanoic acid and glycerol derivatives, and using catalytic amounts of TBAI used as organocatalyst. Conversion and selectivity rates of esterification reactions were monitored by 1H and 13C{1H} NMR spectroscopy. The predominantly formed ester, 2,3‐dihydroxypropyl decanoate was fully characterized by infrared and NMR spectroscopy, mass spectrometry, and elemental analysis. Compared with the classical heating procedures, and whatever the glycerol derivatives used, total conversions were obtained with considerably reduced reaction times. Thus, under 300 W, esterification requires only 1 min exposure from glycidol and 5 min from glycerol carbonate. The use of heating with conventional oil bath conditions needs residence times of more than 1 h (even 24 h in the case of glycerol carbonate). The microwave‐assisted synthesis also notably enhances the selectivity in 2,3‐dihydroxypropyl decanoate (at 300 W, 90, and 50%, respectively), reinforcing the efficiency and the interest of the method.Practical applications: The results establish that microwave heating is well suited for the solvent‐free synthesis of glycerol monodecanoate from decanoic acid and two glycerol derivatives, glycidol, and glycerol carbonate. Reaction times are drastically reduced, and in both cases, marked improvements of the conversion and selectivity are recorded. The target α‐monoglyceride, 2,3‐dihydroxypropyl decanoate, has various potential applications such as antimicrobial properties, bacterial inhibitory activity, or denture disinfectant.Solvent‐free microwave heating conditions are applied to the synthesis of 2,3‐dihydroxypropyl decanoate by esterification of decanoic acid in the presence of two glycerol derivatives, glycidol, and glycerol carbonate. In both cases, conversion and selectivity gains, as well as notable reductions of reaction times are record.

Drug-Porous Silicon Dual Luminescent System for Monitoring and Inhibition of Wound Infection.

Wound monitoring and curing is of great importance in biomedical research. This work created a smart bandage that can simultaneously monitor and inhibit wound infection. The main components of the smart bandage are luminescent porous silicon (LuPSi) particles loaded with ciprofloxacin (CIP). This dual luminescent system can undergo accelerated fluorescent color change from red to blue upon the stimulation of reactive oxygen species (ROS) and elevated pH, which are main biomarkers in the infected wound. The mechanism behind the chemical-triggered fluorescent color change was studied in detail. In vitro experiment showed that the ratiometric fluorescent intensity (IRed/IBlue) of CIP-LuPSi particles decreased from 10 to 0.03 at pH 7.5 after 24 h, while the value deceased from 10 to 2.15 at pH 7.0. Strong correlation can be also found between the IRed/IBlue value and ROS concentration ranging from 0.1 to 10 mM. In addition, the oxidation of LuPSi also simultaneously triggered the release of CIP molecules, which exhibited bacterial inhibition activity. Therefore, the ratiometric fluorescent intensity change at red and blue channels can indicate not only the wound infection status but also the release of antibiotics. In vivo test proved that the smart bandage could distinguish infected wounds from acute wounds, just relying on the naked eyes or a cell phone camera. On the basis of the Si nanotechnology established in this work, theranostic wound care will be realized in future.

Grilling enhances antidiarrheal activity of Terminalia bellerica Roxb. fruits

Ethnopharmacological relevanceTerminalia bellerica Roxb. fruits are rich in a variety of biologically active ingredients. Tharu and Buksa tribes of Udham Singh Nagar, Uttarakhand, India use grilled fruits of Terminalia bellerica as an effective cure for diarrhea Aim of the studyWe validated the ethnobotanical claim by comparing the antidiarrheal effect of grilled fruits (GF) with dried fruits (DF). Materials and methodsThe 50% ethanolic extracts of GF and DF were successively fractionated; the antioxidant and bacterial inhibition activity were studied using DPPH free radical scavenging, anti-lipid peroxidation and broth dilution method respectively. Difference in metabolites of ethyl acetate fractions of GF and DF was analyzed using GC-MS, gallic acid content was determined through HPTLC. Further the in-vivo antidiarrheal effect of ethyl acetate fractions of DF and GF was studied on castor oil induced diarrhea model. ResultsThe ethyl acetate fractions showed potential DPPH free radical scavenging (IC50 11.13µg/ml in DF and 8.56µg/ml in GF), anti-lipid peroxidation and antibacterial activity. The non-targeted metabolic profiling showed higher content of tartaric acid, valeric acid, gallic acid, succinic acid, oxalic acid, malonic acid, malic acid, 1,2,3 trisbenzene, uridine and 11-eicosenoic acid in GF. The HPTLC results indicated that gallic acid content was 2.8 (±0.14) and 4.92 (±0.28) mg/g while ellagic acid content was 4.7 (±0.32) and 4.45 (±0.45) mg/g dry powder in DF and GF respectively. According to in vivo antidiarrheal activity DF and GF (100mg/kg oral) inhibited diarrhea by 41.87% and 71.72% respectively. ConclusionGrilling significantly altered the levels of metabolites in T. bellerica fruits which could be responsible for its increased therapeutic potential.

The in vitro antitumor activity of oligonuclear polypyridyl rhodium and iridium complexes against cancer cells and human pathogens

Synthesis, characterization and biological activity of mono, bi and tri nuclear pentamethylcyclopentadienyl rhodium and iridium complexes with 1,3,5-tris(di-2-pyridylaminomethyl)benzene (L) ligand have been described. These complexes have general formula [(Cp*MCl)nL]n+ {M = Rh; n = 1 (1), n = 2 (2), n = 3 (3); M = Ir; n = 1 (4), n = 2 (5), n = 3 (6)} and have been characterized by various spectroscopic techniques. Crystal structure of the complexes 1, 2 and 4–6 has been obtained by single crystal X-ray diffraction analyses. The electronic transition and orbital occupation of complexes have been rationalized by density functional theory studies. The comparative abilities of bacterial inhibition and antiproliferative activity of complexes 1–6 towards four human pathogens (Staphylococcus aureus MTCC96; Escherichia coli MTCC739; Klebsiella pneumonia MTCC2653 and Pseudomonas aeruginosa MTCC2453) and four cancerous cells {B16F10 (Mouse melano carcinoma), THP-1 (human acute monocytic leukemia), PC3 (Human prostate carcinoma) and SK-OV-3 (Human ovarian carcinoma)} have been investigated by agar well diffusion method and MTT assay respectively. An in vitro cytotoxicity study of the complexes (2 and 3) found significant activity against B16F10 and THP-1 cancer cell lines. The structure-activity relationship on aforementioned cancer cell lines indicates that rhodium complexes are more active than iridium complexes.