Biodiversity contributes significantly towards human livelihood and development and thus plays a predominant role in the well being of the global population. According to WHO reports, around 80 % of ...the global population still relies on botanical drugs; today several medicines owe their origin to medicinal plants. Natural substances have long served as sources of therapeutic drugs, where drugs including digitalis (from foxglove), ergotamine (from contaminated rye), quinine (from cinchona), and salicylates (willow bark) can be cited as some classical examples.Drug discovery from natural sources involve a multifaceted approach combining botanical, phytochemical, biological, and molecular techniques. Accordingly, medicinal-plant-based drug discovery still remains an important area, hitherto unexplored, where a systematic search may definitely provide important leads against various pharmacological targets.Ironically, the potential benefits of plant-based medicines have led to unscientific exploitation of the natural resources, a phenomenon that is being observed globally. This decline in biodiversity is largely the result of the rise in the global population, rapid and sometimes unplanned industrialization, indiscriminate deforestation, overexploitation of natural resources, pollution, and finally global climate change.Therefore, it is of utmost importance that plant biodiversity be preserved, to provide future structural diversity and lead compounds for the sustainable development of human civilization at large. This becomes even more important for developing nations, where well-planned bioprospecting coupled with nondestructive commercialization could help in the conservation of biodiversity, ultimately benefiting mankind in the long run.Based on these findings, the present review is an attempt to update our knowledge about the diverse therapeutic application of different plant products against various pharmacological targets including cancer, human brain, cardiovascular function, microbial infection, inflammation, pain, and many more.
Stress is a global menace fortified by the advancement of industrialization. Failure of stress management is due to lack of proper evaluation of anti-stress products. We explored the anti-stress ...potential of the Ginkgo biloba (G. biloba, 30 mg/kg, p.o.) and compared it with that of Panax ginseng (P. ginseng, 100 mg/kg, p.o.) against acute stress (AS) and chronic stress (CS) models in rats. Immediately after AS and CS, the rats were sacrificed, and adrenal glands and stomach were dissected out for weight determination and scoring of the ulcer index (UI), respectively, as well as changes in biochemical parameters like plasma glucose (GL), triglycerides (TG), cholesterol (CL), creatine kinase (CK), and serum corticosterone (CORT) were also estimated. AS significantly increased UI, adrenal gland weight (AGW), GL, CK activity, and CORT, whereas G. biloba significantly reduced them. P. ginseng significantly reverted GL and CK activity. In CS, a significant increase was found in the UI, AGW, CK activity, and CORT with a decrease in the level of CL and TG. G. biloba did not produce any significant effect on CS-induced alterations. P. ginseng reduced the UI, AGW, plasma GL, TG, CK activity, and CORT level significantly. From the above study, G. biloba is more effective in AS, whereas for CS, P. ginseng will be a better option. Hence these extracts possess significant anti-stress properties and can be used for the treatment of stress-induced disorders.
Objective:To evaluate the wound healing activity of the methanolic root extract of Buchanania lanzan Spreng.(B.lanzan),with a focus on antimicrobial and anti-biofilm properties.Methods:The extract ...was evaluated for its wound healing properties(excision and incision models)as evident from the analysis of tensile strength and wound contraction.The extract was also screened for antibacterial properties against different Cram positive and Gram negative bacterial strains.B.lanzan was also studied for its effect on biofilm formation and disruption of preformed biofilms.The synergistic effect of B.lanzan was determined in combination with gentamicin.Results:Topical application of B.lanzan(10%w/w ointment)significantly increased(40.84%)the tensile strength in the incision wound model.B.lanzan also showed significant wound healing activity in excision model and such significant activity was observed from the 9th day.Whereas Soframycin displayed significant wound healing activity from the 6th day.It was found that root extracts of B.lanzan revealed significant inhibition against all tested pathogens.B.lanzan displayed antimicrobial activity against Cram positive(MIC 0.625 mg/mL)and Cram negative(MIC0.625-1.25 mg/mL).B.lanzan was able to reduce biofilm formation and also caused disruption of preformed biofilms in a manner similar to ciprofloxacin.However,gentamicin was found to be ineffective against biofilms formed by Gram negative organism.According to the fractional inhibitory concentration index,B.lanzan displayed synergistic activity when it was combined with gentamicin.Conclusions:From this study it may be concluded that the root extract of B.lanzan revealed significant wound healing potential,which was supported and well correlated with pronounced antibacterial activity of the tested plant parts.
Accumulating evidence indicates that G protein-coupled receptors can assemble as dimers/oligomers but the role of this phenomenon in G protein coupling and signaling is not yet clear. We have used ...the purified leukotriene B4 receptor BLT2 as a model to investigate the capacity of receptor monomers and dimers to activate the adenylyl cyclase inhibitory Gi2 protein. For this, we overexpressed the recombinant receptor as inclusion bodies in the Escherichia coli prokaryotic system, using a human α5 integrin as a fusion partner. This strategy allowed the BLT2 as well as several other G protein-coupled receptors from different families to be produced and purified in large amounts. The BLT2 receptor was then successfully refolded to its native state, as measured by high-affinity LTB4 binding in the presence of the purified G protein Gαi2. The receptor dimer, in which the two protomers displayed a well defined parallel orientation as assessed by fluorescence resonance energy transfer, was then separated from the monomer. Using two methods of receptor-catalyzed guanosine 5′-3-O-(thio)triphosphate binding assay, we clearly demonstrated that monomeric BLT2 stimulates the purified Gαi2β1γ2 protein more efficiently than the dimer. These data suggest that assembly of two BLT2 protomers into a dimer results in the reduced ability to signal.
Cyclophosphamide (CP) is one of the widely used anticancer agents; however, it has serious deleterious effects on normal host cells due to its nonspecific action. The essential trace element Selenium ...(Se) is suggested to have chemopreventive and chemotherapeutic efficacy and currently used in pharmaceutical formulations. Previous report had shown Nano-Se could protect CP-induced hepatotoxicity and genotoxicity in normal Swiss albino mice; however, its role in cancer management is still not clear. The aim of present study is to investigate the chemoprotective efficacy of Nano-Se against CP-induced toxicity as well as its chemoenhancing capability when used along with CP in Swiss albino mice against Ehrlich’s ascites carcinoma (EAC) cells. CP was administered (25 mg/kg b.w., i.p.) and Nano-Se was given (2 mg Se/kg b.w., p.o.) in concomitant and pretreatment schedule. Increase levels of serum hepatic marker, hepatic lipid peroxidation, DNA damage, and chromosomal aberration in CP-treated mice were significantly (
P
< 0.05) reversed by Nano-Se. The lowered status of various antioxidant enzymes in tumor-bearing mice after CP treatment was also effectively increased by Nano-Se. Administration of Nano-Se along with CP caused a significant reduction in tumor volume, packed cell volume, viable tumor cell count, and increased the survivability of the tumor-bearing hosts. The results suggest that Nano-Se exhibits significant antitumor and antioxidant effects in EAC-bearing mice. The potential for Nano-Se to ameliorate the CP-evoked toxicity as well as to improve the chemotherapeutic effect could have beneficial implications for patients undergoing chemotherapy with CP.
In the present study, we have tried to establish the correlation between changes in Zeta potential with that of cell surface permeability using bacteria (
Escherichia coli
and
Staphylococcus aureus
...). An effort has been made to establish Zeta potential as a possible marker for the assessment of membrane damage, with a scope for predicting alteration of cell viability. Cationic agents like, cetyl trimethyl ammonium bromide and polymyxin B were used for inducing alteration of Zeta potential, and the changes occurring in the membrane permeability were studied. In addition, assessment of poly-dispersity index (PDI), cell viability along with confocal microscopic analysis were performed. Based on our results, it can be suggested that alteration of Zeta potential may be correlated to the enhancement of membrane permeability and PDI, and it was observed that beyond a critical point, it leads to cell death (both Gram-positive and Gram-negative bacteria). The present findings can not only be used for studying membrane active molecules but also for understanding the surface potential versus permeability relationship.
Methotrexate (MTX), a folate antagonist, is currently used as first line therapy for autoimmune diseases like rheumatoid arthritis and psoriasis, but its use is limited by the associated ...hepatotoxicity. As leaves of
Piper betle
, belonging to family Piperaceae, have antioxidant and anti-inflammatory properties, the present study was undertaken to investigate the potential of
Piper betle
leaf extract (PB) in attenuating MTX-induced hepatotoxicity. Rats pre-treated with PB (50 or 100 mg kg
−1
b.w., p.o.) were administered with a single dose of MTX (20 mg kg
−1
, b.w., i.p.) and its hepatoprotective efficacy was compared with folic acid (1 mg kg
−1
b.w., i.p.), conventionally used to minimize MTX-induced toxicity. MTX-induced hepatotoxicity was confirmed by increased activities of marker enzymes, alanine transaminase, aspartate transaminase, and alkaline phosphatase which were remitted by pre-treatment with PB and corroborated with histopathology. Additionally, MTX-induced hepatic oxidative stress which included increased generation of reactive oxygen species, enhanced lipid peroxidation, depleted levels of glutathione and decreased activities of antioxidant enzymes was effectively mitigated by PB, indicative that its promising antioxidant-mediated hepatoprotective activity was worthy of future pharmacological consideration.
A novel reactor system, the rotating disk bioreactor (RDBR), was used to mimic the niche environmental conditions of three salt-tolerant estuarine actinobacteria isolated from the Sundarbans region ...off the Bay of Bengal, designated MS310 (99% similar in its 16S rRNA gene sequence to
Streptomyces parvallus
), MS3/20 and MS1/7. The RDBR, operated at a rotational speed of one revolution per day, 50% submergence of discs, aeration rate of 1.0 vvm, and with a sucrose-containing medium, faithfully mimicked the intertidal estuarine habitat of these marine isolates, and supported biofilm formation and production of antimicrobial metabolites—in particular, actinomycin D by MS310. Onset of antibiotic production by MS310 occurs at 20 h in the RDBR compared to 55 h in a conventional stirred-tank bioreactor (STBR). Furthermore, peak antimicrobial activity is attained much earlier in the RDBR with MS310 (at 45 h) than that reported with a terrestrial strain of
S. parvallus
grown in a STBR (at 144 h). Peak antimicrobial activity of metabolites produced by MS1/7 and MS3/20 were also attained earlier in the RDBR (at 25 and 12 h, respectively) than in a STBR (at 80 and 28 h, respectively). Antibiotic synthesis in the three isolates, in general, appears to be associated with their growth. Overall, the RDBR may be considered the preferred alternative to the STBR for production of antimicrobials by biofilm-forming estuarine bacteria for its much higher surface/volume ratio, lower costs, and easy operability.
The present work reports on the successful one-pot surfactant-free in situ synthesis of silver incorporated ZnO-chemically converted graphene (CCG) nanocomposites (AZG) by adopting a low temperature ...solution technique from zinc acetate dihydrate, silver nitrate and graphene oxide, and the varying silver content (up to 20% Ag with respect to Zn) in the precursors. X-ray diffraction and transmission electron microscopy studies confirmed the presence of Ag and ZnO nanoparticles (NPs), distributed uniformly with CCG. FTIR, Raman, UV-visible and X-ray photoelectron spectroscopic analyses confirmed the existence of interaction between CCG with the inorganic moieties (ZnO/Zn2+ and Ag NPs) of the AZG samples. In vitro cytotoxicity and quantitative cell viability of the human ovarian teratocarcinoma cell line (PA1) was studied up to a maximum sample concentration of 200 mu g ml-1. Antibacterial activity was also measured on E. coli and S. aureus to confirm the efficiency of the nanocomposite, especially for killing bacterial cells without any major effect on the surrounding cells. Among the nanocomposites, the 10% Ag incorporated sample at a 6.25 mu g ml-1 dose showed excellent antibacterial activity with negligible cytotoxicity. This simple strategy could be applied in the synthesis of Ag incorporated different metal oxide-CCG nanohybrids for antibacterial applications.
Gymnema sylvestre is traditionally used for diabetes mellitus. A literature survey revealed very few reports, particularly on rat liver microsomal stability, caco-2 permeability and efflux concerns ...and its correlation with the bioavailability of gymnemagenin, an important component of G. sylvestre. Therefore, the objective of our study was to investigate the in vitro rat liver microsomal stability and caco-2 permeability along with the efflux of gymnemagenin and establish a probable correlation of these in vitro findings with pharmacokinetic parameters after oral and intravenous administration in rats.Rat liver microsomal stability studies to estimate the in vitro intrinsic half-life, clearance, and Caco-2 permeability after 21 days of culture to determine the apparent permeability from apical to basal and from basal to apical, and efflux ratio of gymnemagenin were performed using liquid chromatography-tandem mass spectrometry. A sensitive, robust bioanalytical method was validated and successfully applied to determine the plasma exposure of gymnemagenin. In vitro rat liver microsomal stability demonstrated that gymnemagenin metabolizes rapidly with a short apparent and intrinsic half-life (~ 7 min) and high intrinsic clearance, i.e., 190.08 µL/min/mg of microsomes. The results of the Caco-2 study indicated a poor permeability (1.31 × 10(- 6 )cm/sec) with a very high efflux ratio. The pharmacokinetic study revealed poor oral bioavailability (~ 14 %) of gymnemagenin and it was found to have a short half-life and a high clearance in rats. Our in vitro findings indicated low metabolic stability and poor Caco-2 permeability with high efflux, which might have a role in the observed poor oral bioavailability in rats.
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