bluuebunny/crossref_metadata_2025 huggingface dataset:
Assessment of protective effects of Celastrus paniculatus seed extract against MPP+ induced damage in SH - SY5Ycells
Authors: Sankaramourthy Divya , SUBRAMANIAN KAVIMANI , SADRAS SUDHARANI , MURALIMOHAN UMAMAHESHWARI
Published: July 2024

In the Indian system of traditional medicine, Celastrus paniculatus seeds and oil have been recognized for their therapeutic efficacy in treating cognitive dysfunctions. This study unveils the protective effect of Celastrus paniculatus seed extract (CPME) against the neurotoxin 1-methyl - 4-phenlypyridinium (MPP+) induced damage in SH-SY5Y human neuroblastoma cell line. The protective effect of CPME was assessed by MTT assay by pretreating the SH-SY5Y cells with CPME at two different concentrations (10 and 25 µg/mL) prior to MPP+ exposure (250µM) and the percentage of viable cells was determined. Significant improvement in cell viability was observed with CPME pretreatment and the effect was well pronounced at 25µg/mL concentration. In addition, MPP+ treated cells with or without CPME pretreatment were analyzed for apoptotic cell death by different staining techniques like acridine orange/ethidium bromide (AO/EB), propidium iodide (PI) and 4’ 6 - diamidino - 2 - phenyl indoledihydrochloride (DAPI). Same way, changes in the mitochondrial membrane potential and intracellular ROS production were assessed by staining respectively with rhodamine 123 and 2’, 7’ - dichlorofluorescin diacetate (DCFDA). Quercetin served as a positive control in this study. Observations recorded in fluorescence microscopic image analysis indicated that pre - treatment with CPME caused appreciable protective effects against MPP+ induced cell death by alleviating apoptotic changes such as cell shrinkage, condensation/fragmentation of nuclear material along with restoring ROS levels and mitochondrial membrane potential. Altogether, results from this study points to the protective effects of CPME against MPP+ induced cell death by regulating the cellular production of ROS.
Synthesis and analgesic, anti-inflammatory activities of some novel Thiadiazole derivatives
Authors: Saxena Vaibhav , Sharma Chandra Shekhar
Published: July 2024

A series of novel 1,3,4-thiadiaoles was synthesized and investigated for in vivo analgesic and in vivo anti-inflammatory activity. The structures of all synthesized compounds were confirmed by means of elemental analysis, IR, 1H NMR, and LCMS. All compounds were evaluated for their analgesic and anti-inflammatory activities by tail-flick method and carrageenan-induced rat paw edema test, respectively. Among all the synthesized compounds, compounds 3d and 3e exhibited the most prominent and consistent anti-inflammatory activity. In acute ulcerogenicity study, it can be concluded that these compounds are devoid of the deadlier gastrointestinal toxicities.
Investigations on flavonoid rich extracts of Martynia annua Linn. and Tephrosia purpurea Linn. for Anti-inflammatory and Antihemorrhoidal effects in rats
Authors: Singh Rakesh , Kori Mohan Lal
Published: July 2024

The present study is aimed to study the anti-inflammatory and anti-hemorrhoidal effect of Martynia annua and Tephrosia purpurea extracts in rats. Aerial parts of Tephrosia purpurea and leaves of Martynia annua were selected for extraction with petroleum ether and ethanol. Flavonoid-rich extracts were tested for anti-inflammatory and anti-hemorrhoidal activities (200 and 300 mg/kg bwt.). The anti-inflammatory effect was investigated on Carrageenan and histamine-induced paw edema models by measuring percent inhibition of paw edema at different time intervals. The anti-hemorrhoidal activity was studied by using croton oil-induced hemorrhoid on rats. Effect was assessed by measuring pro-inflammatory mediators in blood, Severity score and Recto Anal Co-efficient and antioxidants level in rectoanal tissues of rats. Results of the study indicate that flavonoid-rich extract of Tephrosia purpurea and Martynia annua significantly inhibited edema in a dose-dependent manner with the treatment of 200 and 300 mg/kg b.wt p.o. in both methods. Both extracts are significantly able to restore pro-inflammatory mediators (TNF-α, IL-6 and PGE2) near normal level. Both, flavonoid-rich extracts treated group also maintained Severity score and rectoanal coefficient (0.268 ± 0.08 and 0.405 ± 0.11) near to the normal control group of animals. MDA level was found statistically significant (p < 0.001) decreased after five days of treatment. The tissue antioxidant level is very close to the normal level after treatment with both flavonoid-rich extracts. The present study concluded that the anti-inflammatory and anti-hemorrhoidal effect of flavonoid-rich extracts of Martynia annua and Tephrosia purpurea could be due to the presence of major flavonoid components, namely quercetin and luteolin in both plants.
Investigation of Anti-diabetic potential of the Flowers of Hibiscus syriacus L. Plant
Authors: DAS PRABHAT , Bhadore Narendra , Cholkar Anjali , Pillai Sujit
Published: July 2024

The present study was carried out to identify the phytochemicals and evaluate the anti-diabetic activity of Hibiscus syriacus L. Ethanol and aqueous extracts were studied for the Oral Glucose Tolerance Test (OGTT) study and sub-acute effects on alloxan-induced diabetic rats. Blood glucose levels, serum lipid profiles and histopathological study of the pancreas were performed. Alloxan induced diabetes in rats by damaging the beta cells of the pancreas. After H. syriacus L. treatment blood glucose, TC, TG, LDL and VLDL of all tested rats were significantly decreased and at the same time HDL was increased in alloxan-induced diabetic rats. However, the ethanolic extract of H. syriacus showed more significant anti-diabetic activity than the aqueous extract. The results reveal that H. syriacus L. flowers extract may have potent anti-diabetic activity, justifying the use of the drug for the treatment of diabetes mellitus.
Combination of Platelet-rich Fibrin and Stromal Vascular Fraction from Adipose Tissue Enhances the Wound Healing in Sprague Dawley Rats
Authors: Sharma Vijay , Sharma Anuka , Ghorpade Parag R , Nandanwar Manohar , Kansagara Atul , Tripathi Sandeep
Published: July 2024

Chronic non-healing ulcer is defined as a persistent defect in the skin for the period of more than six weeks and does not exhibit any tendency to heal following three or more months. Platelet-rich fibrin (PRF) and stromal vascular fraction (SVF) cells obtained from adipose tissue have been widely reported for diabetic wound heling. In this study, the efficacy of the SVF combined with PRF which contains abundant growth factors, for wound healing was evaluated using an animal model. PRF from venous blood was prepared from 8 donors and SVF from lipoaspirate were harvested from a single donor. Three groups were created (i) SVF + PRF as treatment group; (ii) Povidone Iodine (PI) - as standard of care; (iii) negative control group - allowing natural wound healing. Dorsal full thickness wounds were created in 40 male Sprague-Dawley (SD) diabetic rats. The SVF+PRF groups were subdivided into 3 groups having 40,000, one and two million cells per dose per application. On day seven of this study, rats were euthanized and wounds were analyzed microscopically and macroscopically. Wounds closed faster in the SVF + PRF group than in the control group or PI groups, with less inflammation, prominent signs of re-epithelization and blood vessels. The combination of SVF and PRF may provide an additive stimulatory effect to support angiogenesis and accelerate the wound healing process; accordingly. Our results suggest that the combination of SVF and PRF enhances wound healing.
ANTI-TUMOR PROPERTY OF PLANT PROTEASE INHIBITOR ON HUMAN CHRONIC MYELOID LEUKEMIA CELLS
Authors: Bhattacharjee Nilanjana
Published: July 2024

Many Plant Protease inhibitors are found to have effects of tumor suppression in certain cell lines. In this work attempt has been made to determine anti-tumor/apoptotic property of trypsin inhibitor protein (WbTI2) from plant Psophocarpus tetragonolobus (L.)D.C. (winged bean) on human chronic myeloid leukemia cells (K562). Pure winged bean trypsin inhibitor protein was purified by affinity chromatography from recombinant molecule and human chronic myeloid leukemia cells were treated by it. Then viability of the treated cells were determined by simple microscopic study, MTT assay and flow cytometric analysis. All results revealed significant effect of WbTI2 on the viability of the human chronic myeloid leukemia cells. The IC50 value was determined to be 5µg/ml in MTT assay. The data was found to be statistically significant.
HPLC METHOD DEVELOPMENT AND VALIDATION OF RABEPRAZOLE AND LEVOSULPIRIDE IN ITS BULK AND DOSAGE FORM
Authors: Dudhgaonkar Trupti , Lade Pravinkumar , Chopade Vitthal , Baravkar Atul , Jadhav Pranali
Published: July 2024

Analytical method is heart of pharmaceutical analysis. The present work was attempted to develop accurate, simple and sensitive method for simultaneous estimation of rabeprazole and levosulpiride. The mobile phase was consisted of Buffer: Acetonitrile, with ratio of (70:30) at flow rate was quite satisfactory. In our study, the percentage recovery of LEVO was found to be 99.98%, 100.06%, & 100.1% from 80%, 100%, 120% sample solution respectively. For RABE was found to be 98.99%, 99.46%, & 100.08% from 80%, 100%, 120% sample solution respectively. The obtained percentage recovery of both drugs was found to be within the range. This indicates the proposed method was more accurate than the existing methods. Precision is determined by using the method to assay a sample for a sufficient number of times to obtain statistically valid results. The precision is then expressed as the percentage relative standard deviation. Acceptance criteria for the precision of method is that % RSD should not be more than 2%. In the present study for intermediate precision % RSD for LEVO and RABE was found to be 0.344, 0.242 respectively. % RSD value indicate a good degree of precision within specified range.
Quality by Design based Development and Validation of UV-spectrometric Method for the Determination of Remdesivir in Bulk and Marketed Formulation
Authors: Thummar Kashyap , Pandya Malay , Patel Nisarg , Rawat Foram , Chauhan Sanjay
Published: July 2024

A simple and rapid UV spectrophotometric method was developed for quantification of remdesivir in bulk and its dosage form which was used in the treatment of COVID 19. Analytical Quality by Design (AQbD) approach was implemented for method development and the relationship between variable input parameters and the method performance characteristics were designed into Ishikawa diagram. The critical parameters were optimized for solvent, wavelength, scan speed and sampling interval, determined by using principal component analysis as well as by observation. The present method was validated according to ICH Q2 (R1) guideline. The method was found excellent linear (r2 ≥ 0.999) at concentration range of 2 -12 μg/mL at maximum wavelength of 245.5 nm. The detection limit and quantitation limit were satisfactorily found to sensitive and precise. The intraday and interday precision were achieved consistent and percentage relative standard deviation (% RSD) were found ≤ 2%. The overall results of forced degradation studies such as acidic, basic, oxidative, thermal and photolytic conditions imply that the developed method could be well implemented as a stability indicating method for the estimation of remdesivir. The result confirmed that the method can be useful for the routine quality control of remdesivir in their pharmaceutical formulations.
Binding interaction study of β-sitosterol and Luteolin – 7- glucoside with bovine serum albumin by Fluorescence Quenching
Authors: Garad Sunil Venkatrao , Patil S. S.
Published: July 2024

The study on drug–protein interactions is an important field of interest because of the prospective of unraveling of drug action mechanisms and the possibility of designing novel medicines. Bovine serum albumin (BSA) has been studied extensively, because of its structural homology with human serum albumin (HSA). β-Sitosterol is a phytosterol compound which has a variety of pharmacological properties Luteolin 7- glucoside is a glycosyloxy flavones, which has a role as an antioxidant.  In this study, the interaction between β-sitosterol and Luteolin – 7- glucoside with bovine serum albumin (BSA) was investigated at physiological pH 7.4 by fluorescence spectroscopy. The study revealed that the fluorescence quenching of BSA by molecules was a result of the formation of a molecule-BSA complex. Fluorescence quenching constants were determined using the Stern-Volmer to provide a measure of the binding affinity between the molecules and BSA. The results of thermodynamic parameters ΔG, ΔH, and ΔS at different temperatures indicated that action was an endothermic and spontaneous process, and hydrophobic interaction played a major role in molecule-BSA association.
Plumeria acuminata: An Herb with Abortifacient Potential
Authors: Rabadia Jay P. , Desai Tushar R. , Thite Vihang S.
Published: July 2024

Lack of access to safe, timely, affordable and respectful abortion is a critical public health and human rights issue. Abortion till date has been unique debated problem in the field of biomedical consciences. Ethnopharmacological data reveals that plant Plumeria acuminata, of the Apocynaceae family, has exhibited several activities like anti-fertility, anti-pyretic, anti-nociceptive, anti-bacterial, anti-diabetic, anti-tumour, and immune-modulatory as well as abortifacient activities. As per our knowledge, no exploratory studies have been conducted to discover the actual abortifacient potential of this plant till to date. For this purpose, the aim of this study was to evaluate the biological activity of P. acuminata leaves and roots ethanolic extracts with respect to their effects in hormonal and histological regulations, eventually leading to abortion. Ethanolic extracts of harvested P. acuminata leaves and roots were prepared through a cold maceration process, subjected to qualitative phytochemical analysis and acute toxicity test. Based on the LD50 values, 100, 200, and 400 mg/kg doses of both extracts were determined for abortifacient activity in mated adult Wistar female rats. Misoprostol was administered at 0.1 mg/kg, p.o, as a standard abortion-inducing drug. Standard and test-item treatments were given from gestation day (GD) 7 to 14. Morphological, hematological, hormonal, and histological examinations were performed on GD20 after euthanizing animals. Administration of extracts significantly altered the hormonal levels up to ~20-30% i.e., decrease in estrogen and progesterone as well as increased PGE-1 and acetylcholine. Anatomical alterations in reproductive organs were confirmed by observing cystic follicles and atrophied squamous cells during histopathological evaluation. Visual observations of uterine horns confirmed ~25% live fetus, ~28% early resorption, ~30% late resorption resulting in ~75% post-implantation loss. Obtained abortifacient results can be attributed to the presence of plumericin, sterol and lupeol triterpene groups of phytochemicals present in leaves and roots ethanolic extracts, making them a potent candidate for natural abortifacient medicines.
Stability-Indicating Assay UHPLC Method for Simultaneous Analysis of Cilnidipine and Chlorthalidone in Bulk and Pharmaceutical Matrices
Authors: Umbarkar Rahul P. , Mittal Abhilasha , Charde Manoj S.
Published: July 2024

A simple, rapid, precise and accurate stability-indicating ultra-high performance liquid chromatography (UHPLC) method was developed for the simultaneous estimation of Cilnidipine and Chlorthalidone in bulk material and pharmaceutical matrix. Accordingly, the scientific novelty of designed work was to develop a specific and precise stability-indicating UHPLC assay method for the simultaneous quantification of cited drugs in an extended-release fixed dose combinations (FDC). The reversed-phase UHPLC resolution was analyzed with the assistance of UPLC BEH C18 (150 mm  2.1 mm) with 1.7 µm particle size column at ambient temperature using a solvent system in a proportion of (70:30 % v/v) acetonitrile and water with a flow rate of 0.4 mL/min of a solvent system. The analytes were supervised at 275 nm by employing photodiode array recognition. The retention times were 1.731 ± 0.02 min and 1.061 ± 0.022 min for Cilnidipine and Chlorthalidone respectively. The Cilnidipine and Chlorthalidone have confirmed the linearity ranges of 2.0 – 12 μg/mL and 2.5 – 15 μg/mL, with 0.9998 and 0.9994 determination coefficients. The UHPLC method was effectually validated for accuracy, precision, sensitivity, robustness, ruggedness, and selectivity, and specificity. Moreover, the anticipated UHPLC method's capability to analyze the Cilnidipine and Chlorthalidone with no obstruction from degradation products.
Development and Optimization of Gastro-Retentive Mucoadhesive Formulation of Hydralazine HCl
Authors: ACHARYA HIMANSHU A. , Patel Rakesh P.
Published: July 2024

The present study was focused to develop and optimize a gastro retentive drug delivery system (GRDDS) dosage form suitable for controlled drug release. Gastroretention results from unfolding and swelling of the film and its bioadhesion to the gastric mucosa. Hydralazine hydrochloride (HZH) is very short and thus it requires frequency of dosing several times a day. Hence, in order to avoid frequent administrations, a long acting mucoadhesive oral dosage forms can be given which can keep on delivering the drug at controlled rate for a specified period of time. A mucoadhesive drug delivery systems is an optimum system that interacts with the mucus layer covering the mucosal epithelial surface and increase the residence time of the dosage form at the absorption site. A sustained release mucoadhesive gastro-retentive with reduced dosing frequency and increased drug bioavailability is developed. Inclusion of different polymers like hydroxy propyl methyl cellulose K4M (HPMC K4M), carbopol 940 and sodium alginate at different concentration were used in order to study and get desired results. The results indicate the dosage form is gastroretentive and can provide controlled release of drugs with a release drug profile upto 24 hours. The above said formulation was further optimized using box-behnken factorial design.
Quality Audit and Anti-Inflammatory Activity of Marketed Formulations of Ashokarishta Syrup and Chandraprabha Vati
Authors: Deswal Geeta , Dhingra Ashwani K. , Saini Vipin , Grewal Ajmer Singh
Published: July 2024

Herbal formulations play an important role in medicines; however, their suboptimal standardization, in terms of identity, purity, quality, efficacy and safety, has questioned their efficiency in treating various disorders. The present study was conducted to perform a quality audit of two herbal formulations, i.e., ashokarishta syrup and chandraprabha vati, of three different marketed brands. The quality auditing procedures included analysis of moisture content, ash value, pH, presence of heavy metals, pesticide residue, radioactive substances and microbial contamination. The formulations were pharmacologically evaluated for anti-inflammatory activity using the rat paw edema model. All the formulations passed the microbial contamination test. None of the heavy metals was detected with higher than permissible limits in any formulations. Moreover, all the formulations were found free from pesticides and radioactive substances. In addition, the formulations also possessed anti-inflammatory activity; however, their activity varied among brands. The present study concluded that all the formulations tested were successfully quality audited. This study can be used as a standardizing tool for the future perspective.
Enhancing the Solubility, Dissolution Rate and Oral Bioavailability of Poorly Water-soluble Drug, Satranidazole by Solid Dispersion prepared by using β-Cyclodextrin as a Carrier
Authors: AWATE PRAVIN , Kunjir Vaibhavi V. , Kardile Dipak P. , Bhagat Vishwas C. , Shete Rajkumar V. , Shinde Tushar B.
Published: July 2024

The present work aims to prepare and characterize solid dispersions of Santranidazole using β-Cyclodextrin to improve its aqueous solubility and dissolution with the aid of solvent evaporation technique. Solid dispersions showed marked improvement in the solubility behavior and stepped forward for drug launch. From all the formulations, F2 becomes an optimized method based on the characterization, solubility and dissolution studies. The enhancement of dissolution depends upon the nature and quantity of the carrier. The rise in the dissolution rate may be attributed to; the reduced particle size of drug deposited at the carrier’s floor and the enhanced wet capacity of the drug debris by the carrier. The optimized formulations have been evaluated through Differential Scanning Calorimetry (DSC), Fourier remodel infrared spectroscopy (FTIR) and Scanning electron microscopy (SEM).
Immune-Stimulants and Adaptogenic Properties of Selected Wild Edible Mushrooms Collected from the Western Ghats, India
Authors: NK Shahina , K Madhusudhanan , Mathew Angel
Published: July 2024

Virus outbreaks such as the COVID-19 virus demand nutrition interventions among people all over the world. Consumption of foods with immune-modulating and nutraceutical characteristics is an effective strategy to avoid or lessen the severity of viral attacks and side effects. Immune stimulants function by enhancing macrophage activity and killing pathogens and diseased cells, while adaptogens work by supporting and regulating the endocrine system. This paper foreshadows the use of mushrooms as a functional food for the prevention and treatment of COVID – 19 by citing peer-reviewed papers from Google Scholar, PubMed, the WHO database, Science direct, and the author’s own research. Pleurotus ostreatus, Termitomyces heimii, T. microcarpus, T. clypiatus, Auricularia auricula, Phlebopus portentos, Ganoderma lucidum, Coprinus micaceus, Cantharellus cibarius, C. minor, and Lentinus bambusinus were among the ethnomedicinal mushrooms studied. Immuno-modulating effects were found in polysaccharides, fungal immune-modulatory proteins (FIPs), terpenes, and terpenoids from wild mushrooms, as well as activation of immune effector cells such as lymphocytes, macrophages, and natural killer cells. They also cause the production of cytokines such as IFN-, IL-2, IL-4, IL-10, and TNF-. Similarly, mushrooms have been shown to have probiotic properties that can help to flatten the curve.
GC-MS analysis and memory-enhancing effect of hydroalcoholic extract of a polyherbal Unani formulation ‘Majoon Vaj’ in scopolamine- and diazepam-induced amnesic mice
Authors: Aleem Mohd , Khan Md Imran , Shamsi Shariq , Usmani Qamrul Islam
Published: July 2024

Majoon (M) Vaj is a polyherbal Unani formulation possessing multiple neuropharmacological activities. It is used to treat Nisyān (dementia) for centuries. It has been reported as improving memory and overall mental faculties. The current study was carried out to assess the nootropic and anti-amnesic activity of M. Vaj in mice to validate its use in Unani medicine. The exteroceptive behavior model elevated plus maze (EPM) and morris water maze (MWM) and interoceptive behavior model (scopolamine and diazepam) were used to evaluate nootropic activity in mice. Pre-treatment with M. Vaj extract (220 and 440 mg/kg, p.o.) for 15 days showed a significant decrease transfer latency (TL) in EPM and decrease escape latency (EL) during training and increase time spent in the target quadrant (TSTQ) during retrieval in the MWM test, indicating nootropic activity. M. Vaj also significantly reversed scopolamine and diazepam-induced amnesia, as observed by decreased TL in EPM and increased TSQT in MWM, indicating anti-amnesic activity. Also, both doses of the test drug showed a similar response, which was almost equal to that of the standard drug piracetam. Reversal of scopolamine and diazepam-induced amnesia by M. Vaj indicated the possible facilitation of cholinergic transmission or GABA benzodiazepine pathway. GC-MS of M. Vaj led to the identification of 141 compounds. α-asarone (72.12%) and β-asarone (72.12%) were found in the highest amount as compared to other compounds.
Synthesis, Characterization and Biological Evaluation of Novel Isoxazolo [5,4-b] Quinolines as potent Antimicrobial Agents
Authors: Snehi Varsha , Pathak Devender
Published: July 2024

In order to combat antimicrobial resistance, antimicrobial chemotherapy made advances in the development of new potent antibiotics and antifungal agents. This is because the microorganisms are becoming resistant to the drugs due to improvements in current antibiotic classes by changing their pore formation mechanism and membrane permeability as well as by adjusting to combat the efficacy of the drugs. In order to address the microbial resistance, a series of novel isoxazolo [5,4-b] quinolines are synthesized and evaluated for antibacterial and antifungal activities. The synthesized compounds 4c, 4f and 4g exhibited potent antibacterial activity, and 4c and 4e revealed moderate antifungal activity.
Formulation and In-vivo Evaluation of Azatanavir Selfnanoemulsifying Drug Delivery System
Authors: REDDY KOMALA DEVENDER , SANDHYA PAMU , MAMATHA PALANATI
Published: July 2024

Atazanavir is a human immunodeficiency virus (HIV) protease inhibitor. Due to its intense lipophilicity, the oral delivery of atazanavir encounters several problems such as poor aqueous solubility, pH-dependent dissolution and rapid first-pass metabolism in liver by CYP3A5, which result in low and erratic bioavailability. The current study aimed to develop self-nanoemulsifying drug delivery systems (SNEDDS) of atazanavir in an attempt to circumvent such obstacles. Equilibrium solubility studies indicated the choice of peceol oil - acrysol EL135-capmul MCMC8 for formulating the SNEDDS. Ternary phase diagram constructed with surfactant (Acrysol EL135), co-surfactant (Capmul MCMC8) and oil (peceol oil) representing each apex of the triangle. The pharmacokinetics studies of SNEDDS formulation were investigated in wistar rats. The optimal formulation (F9) with best self-nanoemulsified and solubilization ability consisted of 20% (w/w) peceol oilas oil, 60% (w/w) acrysol EL135 as surfactant and 20% (w/w) capmul MCMC8 as cosurfactant. The formulation displayed maximum drug content of 99, 98% entrapment efficiency and drug release of >98% in 60 minutes. The particle size for the optimized formulation of SNEDDS (F9) was found to be 51.6 nm with PDI 0.468 and zeta potential of -20.6 mV. The formulation found to be stable after storage at accelerated conditions at 40 ± 2°C/75 ± 5% RH for a period of six months. The pharmacokinetic study in rats indicate that the Cmax of the SNEDDS 0.33 ± 1.73 ng/mL was significant (p < 0.05) as compared to the pure drug 0.091 ± 0.39 ng/mL. Tmax of both SNEDDS formulation and pure drug was 1.5 ± 0.53 and 3 ± 0.72 hours, respectively. The AUC indicated significant enhancement in the rate and extent of bioavailability by the SNEDDS formulation compared to pure drug. The studies, therefore, indicate the successful formulation development of SNEDDS with distinctly improved bioavailability of atazanavir.
Screening of Some Hamamelitannin Derivatives against Staphylococcus Aureus: A Computational Perspective
Authors: Sarkar Kaushik , Sarkar Subhajit , Das Rajesh Kumar
Published: July 2024

Methicillin-resistant Staphylococcus aureus (S. aureus) is a common target for inhibiting the quorum sensing biofilm formation. Hamamelitannin (HAM) has a promising activity to combat these biofilm-associated infections and is used as a quorum sensing inhibitor (QSI). Here, we found different tested derivative compounds for designing S. aureus biofilm inhibitors by functionalization at various positions of HAM. In silico studies were carried out to find better drug candidature. Out of all, 14 derivatives have satisfied higher binding affinity as well as interactions against three different S. aureus target receptors, compared to HAM. DFT, ADME, and toxicity analysis are also performed for these compounds. The stability of the protein-ligand complexes is quantified by 30 ns molecular dynamics simulations. From these various studies, 14 ligands will be considered as potent inhibitors against S. aureus biofilm formation after successfully screening of in vitro and in vivo analysis.
Evaluation of Aphrodisiac Activity of Agave americana Leaves in Male Wistar Rats
Authors: KUMAR G SANTHANA , TANDEL BHAVYATA , PAUL ARINDAM PAUL
Published: July 2024

Agave americana has been known as century plant or American aloe. This plant consists of alkaloids, flavonoids, steroidal saponins, proteins, and saponins, indicating that the plant may have aphrodisiac properties. Although traditionally, it has been used to treat inflammation, aphrodisiac nature is not evaluated. The current study was designed to evaluate the aphrodisiac activity of A. americana on male albino wistar rats. The presence of different plant constituents in the plant extract was determined by the preliminary phytochemical screening methods. For the experimental procedure, the female rats were allowed to be ovariectomized for 1 month before the behavioral activity. Hydroalcoholic extracts of A. americana at doses of 100, 200, and 400 mg /kg were administrated for 21 days. The female rats involved in mating were made receptive by hormonal treatments. The common matting behaviors, libido, potency, mounting frequency, intromission frequency and orientation activity were studied. Results revealed there was a significant raise in the mounting frequency, intromission frequency, libido activity, erection, quick flip, long flip activities. Additionally, a significant increase in the serum testosterone hormone levels in male rat was found. Current study concludes the hydroalcoholic extract of A. americana shows aphrodisiac activity at a dose of 400 mg/kg body weight.
Design and Therapeutic Potential of 2,5-substituted diphenyl-1,3,4-oxadiazole Derivatives
Authors: Sharma Jyoti , AGARWAL NIDHI
Published: July 2024

In the present study, new class of 2,5-substituted diphenyl-1,3,4-oxadiazole derivatives were developed by combining substituted aromatic acids with hydrazine hydrate in the presence of POCl3 reagent under various  reaction conditions. The compounds were also evaluated for their antimicrobial potential against some bacteria (E. coli and S. aureus) and fungi (C. albicans and A. Niger). As the result of the newly synthesized compounds were characterized as 2-(4-chlorophenyl) compounds-5-(4-nitrophenyl)-1,3,4-oxadiazole (13), 2-(4-methylphenyl)-5-(4-nitrophenyl)-1,3,4-oxadiazole (16), 2-(4-chlorophenyl)-5-(4-methoxyhenyl)-1,3,4-oxadiazole (17), 4-[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]phenol (18), and 2-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-1,3,4-oxadiazole (25). The results also revealed that these compounds have good potential to inhibit microbes. It may be concluded that oxadiazole nucleus may be a profitable source for the synthesis of drugs against infectious diseases.
Identification of Lead Molecules against Multi-target of SARS-CoV-2 from Carica papaya L. through In-silico Method
Authors: Sugathan J Keerthi , S Sreekumar , Biju Charuvila Kamalan
Published: July 2024

The efficacy of currently used vaccines against severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is questionable since the virus is rapidly mutating. A single drug that can simultaneously act on multi-target at different stages of disease causing pathways is the best option to fight against it. The multi-target inhibitory activities of many phytochemicals have been reported. The present investigation was aimed to screen the multi-target inhibitory activity of 215 phytochemicals from Carica papaya L. against three targets of SARS-CoV-2 viz spike protein (SP), main protease (Mpro), RNA-dependent RNA-polymerase (RdRp) and a target from host, angiotensin-converting enzyme 2 (ACE-2) using the docking tool, AutoDock Vina in PyRx 0.8. The docked results with free energy of binding ≤ -6 kcal/mol were considered active/hit molecules. Of the 215 phytochemicals, 48 have binding energy ≤ -6 kcal/mol against all the targets. Further molecular interaction between the ligand and targets, pharmacokinetics and ADMET analysis of the top ranked five hits obtained against each target revealed that the compound hesperidin can be selected as the best lead since it has the least binding energy, admissible ADMET and a better binding score than the control drugs. Hesperidin has been used as an approved drug to treat vascular disease. Overall, results revealed that C. papaya is a rich source of phytochemicals with activity on multi-target of SARS-CoV-2 infection and multiplication in the human host.
Design and Development of Some Pyrimidine Analogues as an Anthelmintic Agent
Authors: Pawar Smita J. , Dorugade Rahul , Kale Amol P. , Zope Dhanashri
Published: July 2024

Anthelmintic drugs are used to treat parasitic infections and acknowledge the challenge in developing effective anthelmintics due to the significant homology between parasites and their hosts. Despite the existence of various anthelmintic drugs in the market, the emergence of drug resistance necessitates the continuous development of new and more efficient drugs to combat parasitic infections. The development of anthelmintic drugs involves a multi-faceted process that aims to create effective treatments against parasitic infections. Pyrimidines have been investigated for their potential anthelmintic activity. Therefore, the present study involves the synthesis of derivatives based on pyrimidine. The series of 4-amino-2-hydroxy-6-substituted phenyl pyrimidine-5-carbonitrile was synthesized by treating substituted benzaldehyde with malononitrile and urea. The synthesized compounds were subsequently screened for their anthelmintic efficacy. The chemical structures were confirmed by infrared (IR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anthelmintic activity was performed on the adult Indian earthworm Pheretima posthuma. In-vitro anthelmintic studies revealed that, among all the screened compounds, compound 1f demonstrated significant or appreciable anthelmintic properties. Molecular docking was conducted on quinol-fumarate reductase to elucidate potential interactions between the newly synthesized pyrimidine derivatives and the specific cavity of the quinol-fumarate reductase enzyme. This analysis aimed to gain insights into the binding interactions and the possible mechanism of action of the synthesized compounds.
Nephroprotective effect of the methanolic fruit extract of Musa balbisiana Colla against carbon tetrachloride-induced toxicity in Swiss albino mice
Authors: Baruah Nabanita , Das Madhubanti , Saikia Kandarpa Kumar , Kalita Jogen Chandra
Published: July 2024

Renal failure is the loss of renal functions owing to multiple factors, including oxidative stress, and it is a global concern, as it costs millions of lives every year. Carbon tetrachloride is a standard toxicant exploited to induce nephrotoxicity in experimental animals to study oxidative stress-related renal injury. This study was conducted to determine the nephroprotective activity of a methanolic extract derived from the unripe fruit pulp of Musa balbisiana Colla (MBME) in carbon tetrachloride-induced toxicity in Swiss albino mice. Multiple groups of mice were treated with a single dose of carbon tetrachloride (1-mg/kg body weight) intraperitoneally once in a week followed by oral administration of the methanolic fruit extract of M. balbisiana Colla (MBME) at two different doses (200 and 400 mg/kg body weight) consecutively for 28 days. Treatment with carbon tetrachloride reduced body weight along with enzymatic and non-enzymatic antioxidants in the renal tissue, elevated kidney weight, renal biomarkers, lipid peroxidation, IL-6, TNF-α, and TGF-β levels in the blood serum, impaired antioxidant system and up-regulated TGF-β expression in the kidney tissue, and brought histological changes in the architecture of renal tissues. Our data revealed that the oral administration of the methanolic fruit extract of M. balbisiana Colla (MBME) dose wisely restored kidney and body weight, renal biomarkers, enzymatic and non-enzymatic antioxidants in the renal tissue, reduced lipid peroxidation, interleukin 6 (IL-6), tumor necrosis factor-alpha (TNF-α), and transforming growth factor-β (TGF-β) levels in the blood serum, re-established antioxidant system and down-regulated TGF-β expression in the kidney tissue, and re-established the architecture of renal tissues. Thus, this study reported the nephroprotective effects of methanolic fruit extract of M. balbisiana Colla (MBME) in carbon tetrachloride-induced toxicity in Swiss albino mice through possible antioxidant and anti-inflammatory activity.
Metabolite profiling and in-vitro evaluation of cytotoxic efficacy of Psychotria dalzellii Hook.f. on MCF-7 and L929 cell lines
Authors: Thejashree Aralahalli Borappa , Naika Raja
Published: July 2024

In the current study Psychotria dalzellii Hook.f. stem-bark samples were procured from Joida, Western Ghats, Karnataka, India. air-dried and subjected to Soxhlet extraction. The obtained extracts were screened for preliminary phytochemicals which resulted in the existence of flavonoids, alkaloids, glycosides, phenols, tannins, steroids, triterpenoids, saponins, carbohydrates and lignins. Subsequently, the ethanolic stem bark extracts were subjected to GC-MS analysis to quantitatively estimate the phytoconstituents. It reveals the presence of 20 bioactive chemicals. Among them, 2-Furancarboxaldehyde, 5-(hydroxymethyl)- (59.26%); p-Mesyloxyphenol (10.68%); 2-Furaldehyde diethyl acetal (4.54%); 4H-Pyran-4-one, 2,3-dihydro-3,5-dihydroxy-6-methyl (4.11%) were noted to be the principal compounds detected. Furthermore, in-vitro cytotoxic activities on MCF-7 and L929 cell lines were determined by 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay. The extract exhibited considerable cytotoxic activity towards MCF-7 cell lines at higher concentrations with an IC50 value of 440.82 µg/ml and it showed very less toxicity towards L929 normal cell lines. Which indicates its potential as a possible source of bioactive constituents for medicinal and pharmaceutical exploration.
An Investigation of Type II Anti-diabetic activity of Biologically Active phytochemical(s) of Coccinia Indica Fruits in High Sugar Diet Induced Diabetic Rats
Authors: ALI ABDULLAH ALI MOHAMMED , RAJASHEKHAR U. , Jha Deepak Kumar
Published: July 2024

Unhealthy diets and lifestyles cause a resistance to and/or relative deficiency of insulin production. Therefore, it is thought worthwhile to develop a natural remedy that may effectively manage the disease symptoms to a certain extent without causing adverse consequences. The objective was to develop the active biological constituent(s) for the use of Coccinia indica and its relationship to treating type II diabetic rats. The soxhlet extraction method was used to get the cocktail of phytochemicals of C. indica by using methanol. The composition of a high-sugar diet, followed by fructose (66%), was used to induce T2DM in rats. The preliminary predictive markers were body weight (pre- and post-treatment), blood glucose level (pre- and post-treatment), serum insulin, and pancreatic insulin. And the secondary outcomes were the pro-inflammatory mediators interleukin 6 (IL-6), transforming growth factor-β (TGF-β), and tumour necrosis factor alpha (TNF alpha). Additionally, pancreatic tissue was used to estimate beta cell mass, size, and necrosis, and the cell supernatant was used to observe superoxide dismutase (SOD), lipid peroxidation (LPO), and catalase (CAT). High sugar diet showed significant increase in body weight (p < 0.01), fasting blood glucose level (p < 0.001), and decrease in serum and pancreatic insulin levels (p < 0.001), whereas rats treated with methanolic extract of C. indica showed significant reduction in post-treatment body weight (p < 0.01), blood glucose levels (p < 0.01), and increase in serum and pancreatic insulin (p < 0.001), especially in higher doses, i.e., 400 mg/kg. Pro-inflammatory cytokines (IL-6, TGF-beta, and TNF-α) can increase insulin resistance, which results in poor glucose homeostasis, which has been reduced by treatment with C. indica (p<0.001). Superoxide radicals and a deficiency in catalase, both of which are linked to diabetes, but the extract of the plant has been shown to enhance the secretion of enzymes SOD and CAT (p<0.001). It has been proven to have a crucial role in the regulation of apoptosis because it lowers oxidative stress and similarly reduces the level of LPO (p<0.01). Additionally, the treated rat pancreas shows islets of Langerhans that are normal in number and size. No necrosis or reduction in size was seen. The current study conclusively shows that the phytoconstituents of C. indica have the potential to tackle long-term health complications and manage symptoms.
Bio-inspired Synthesis of Ag, Au, and Ag-Au Bimetallic Nanoparticles using Capsicum annuum Aqueous Leaf Extract and Assess their In-vitro Antibacterial and Anticancer Potential
Authors: Naveena A. , Jeyasundari J. , VENGATESH PRIYA P.
Published: July 2024

Noble bimetallic nanoparticles (BNPs) exhibit strong anticancer and antibacterial activities. They are known to be stable, less toxic, environmental friendly and biocompatible nature.  Due to their enhanced biological properties, they are well suits for the biomedical applications such as cancer therapy, gene therapy and drug delivery. In the current study, we examine the anticancer and antibacterial potential of bio-mediated mono and bimetallic nanoparticles. Here, aqueous Capsicum annuum leaf extract was employed as a good reducing and capping agent for producing Ag, Au monometallic, and Ag-Au bimetallic nanoparticles. The formation of C.A- Ag, Au MPNs and Ag-Au BNPs was initially confirmed by visible color change of the reaction mixture and UV-Visible spectra show the Surface Plasmon Resonance (SPR) band observed at 543 nm. Furthermore, phytofabrication, crystallinities, structural alignments, particle size and elemental composition were studied by following standard physico-chemical techniques such as FT-IR (Fourier Transform Infrared), XRD (X-Ray diffraction), HR-TEM (High resolution-Transmission Electron Microscopy), SEM-EDX (Scanning Electron Microscopy and Energy- dispersive X-Ray Spectroscopy) respectively. The results were obtained from various characterization techniques confirmed that the C.A. mediated Ag, Au MNPs and Ag-Au BNPs were spherical in shape and FCC structure with nanoscale range (10-25 nm). The BNPs exhibit strong efficacy against bacterial strains. These nanoparticles were subjected to investigate the anticancer activity against human lung cancer cells (A549 cell line) through MTT assay. The cell viability was determined by this assay. The occurrence of cell apoptosis and necrotic were quantified by using dual fluorescent staining (AO/EB) and flow cytometry analysis. However, Ag-Au bimetallic nanoparticles showed highest cytotoxic potential with low IC50 - 57.35 ± 0.05 µM values. This IC50 value is comparatively lower than, Ag, Au MNPs and C.A. aqueous leaf extract. IC50 values of C.A- Ag-Au BNPs predominantly induced the cell apoptosis, necrotic and the death of A549 cells suggested the anticancer potential of C.A. mediated Ag-Au BNPs to treat the lung cancer cells.
An LC-MS/MS Method Development and Validation for the Quantification of Infigratinib in K2EDTA Human Plasma
Authors: Jogeswara Rao P. , Bhikshapathi D.V.R.N.
Published: July 2024

A validated liquid chromatography with tandem mass spectrometry (LC-MS-MS) technology was developed for the quantification of infigratinib, using a simple and specific approach. This method utilizes a liquid-liquid extraction (LLE) strategy to achieve high sensitivity. The analytical approach that was developed underwent validation in terms of many characteristics including specificity, sensitivity, carry-over, recovery, precision, matrix effect, accuracy, and stability. The elution of the drug and IS occurred in a time frame of 6.5 minutes using a PhenomenexSB-C18 column (250 × 4.6 mm x 5 μm). The mobile phase consisted of a mixture of acetonitrile and 0.1% v/v formic acid in water, with a ratio of 80:20. The infusion flow rate was set at 0.9 mL/min. The retention times (RT) of infigratinib and IS were determined to be 5.12 and 3.31 minutes, respectively. The elution time required for complete separation of infigratinib was 6.5 minutes. The equation of the linear regression line was determined to be y = 0.994x + 2.662, and the coefficient of determination (r2) was calculated to be 0.999. The coefficient of variation (%CV) obtained for the calibration graph of infigratinib was determined to be less than or equal to 3.73. The matrix effect was assessed by calculating the coefficient of variation (%CV) for the High and low quality control (QC) samples, yielding values of 1.64 and 0.70% respectively.
Hair growth potential of Helianthus annuus seed oil extract and Martynia annua seed oil extract on albino mice
Authors: Kumar Abhishek , Kori Mohan Lal
Published: July 2024

The surface scalp of hair matrix cells differentiation during migration induces by vigorous proliferation result hair growth. The objective of current investigation was to explore the needs to know of Helianthus annuus seed oil extract and Martynia annua seed oil extract as a potential of hair growth. In albino mice on to the back skin surface spread prepared oil extract to assess telogen to anagen phase transition. The quantitative and qualitative analysis was performed and observed. The outcomes of their research revealed that Helianthus annuus seed oil extract of petroleum ether and Martynia annua oil extract of petroleum ether in combination shows exhibited prominent activity. In different dosage of petroleum ether oil extract of both plant combinations of dosage applied topically 10 mg/ml, 20 mg/ml and 30 mg/ml, in to the shaved skin of albino mice treated groups observed for 21 days. Result shown that petroleum ether oil extract of both plant in combination shown significantly hair growth potential in a different dosage dependent manner observed, particularly on albino mice. Albino mice groups treated with petroleum ether 30 mg/ml of both plants required shorter time to the control (positive) group and 2% minoxidil (standard) group at different growth stages. The hair length of albino mice treated with petroleum ether 30 mg/ml oil extract of both plants showed remarkable increase 21.35±0.25 mm. and the thickness of hair of albino mice group treated with combination of both plant oil extract is 0.020±0.0010 mm with respect to 2% minoxidil (0.021±0.008). These finding suggested that Helianthus annus seed oil extract and Martynia annua oil extract have the potential of show hair growth.