Sunil Jalalpure

Antidiabetic activity of aqueous bark extract of Cassia glauca in streptozotocin-induced diabetic rats

The leaves and bark of Cassia glauca Lam., a glabrous tree in the family Fabaceae, are used in folk medicine for the treatment of diabetes. The aim of this study was to investigate the antidiabetic activity of the aqueous extract of C. glauca bark. The various parameters that were studied in treated or untreated normoglycemic and STZ-induced diabetic rats included the effect of the aqueous extract on oral glucose tolerance, fasting blood glucose, body weight, serum lipids, liver glycogen, serum insulin, and glycosylated haemoglobin. Oral administration of the aqueous extract of C. glauca bark at a dose of 500 mg/kg significantly reduced the effect of external glucose load. In a chronic treatment model, aqueous extract and glibenclamide (0.25 mg/kg) were administered for 21 days. At the end of the treatment, there was a significant increase in liver glycogen, serum insulin, and HDL cholesterol for both treatments. A significant decrease in fasting blood glucose, glycosylated haemoglobin, total cholesterol, and serum triglycerides was also observed. The body weights of the animals were observed to be consistent throughout the study. The findings showed the significant antidiabetic potential of the extract in ameliorating the diabetic condition in the diabetic rats. No significant activity was found in the normoglycemic rats.

Resolving identification issues of Saraca asoca from its adulterant and commercial samples using phytochemical markers

Saraca asoca (Roxb.) De Wilde (Ashoka) is a highly valued endangered medicinal tree species from Western Ghats of India. Besides treating cardiac and circulatory problems, S. asoca provides immense relief in gynecological disorders. Higher price and demand, in contrast to the smaller population size of the plant, have motivated adulteration with other plants such as Polyalthia longifolia (Sonnerat) Thwaites. The fundamental concerns in quality control of S. asoca arise due to its part of medicinal value (Bark) and the chemical composition. Phytochemical fingerprinting with proper selection of analytical markers is a promising method in addressing quality control issues. In the present study, high-performance liquid chromatography of phenolic compounds (gallic acid, catechin, and epicatechin) coupled to multivariate analysis was used. Five samples each of S. asoca, P. longifolia from two localities alongside five commercial market samples showed evidence of adulteration. Subsequently, multivariate hierarchical cluster analysis and principal component analysis was established to discriminate the adulterants of S. asoca. The proposed method ascertains identification of S. asoca from its putative adulterant P. longifolia and commercial market samples. The data generated may also serve as baseline data to form a quality standard for pharmacopoeias. Abbreviations used: HPLC: High Performance Liquid Chromatography; RP-HPLC: Reverse Phase High Performance Liquid Chromatography; CAT: Catechin; EPI: Epicatechin; GA: Gallic acid; PCA: Principal Component Analysis.

In vitro antioxidant and anticancer activity of Leea indica leaf extracts on human prostate cancer cell lines

Background To determine the phytochemical constituents, antioxidant, and anticancer activities of Leea indica leaf extracts on DU-145 and PC-3 human prostate cancer cell lines. Methods Leaf sample was subjected to Soxhlet extraction method with increasing polarity of solvents, namely, chloroform, ethyl acetate, methanol, ethanol, and aqueous. Phytochemical screening was done using different biochemical tests. Quantitative analysis for phenol was determined by Folin–Ciocalteu reagent method. The antioxidant activity was tested using 2,2-diphenyl-1-picrylhydrazyl, ferric ion reducing power assay, and phosphomolybdenum assay. In vitro anticancer activity on DU-145 and PC-3 human prostate cancer cell lines was evaluated by (3-(4, 5-dimethyl thiazole-2yl)-2, 5-diphenyl tetrazolium bromide) MTT assay. Results Phytochemical screening confirmed the presence of phyto-constituents like alkaloids, flavonoids, glycosides, phenols, lignins, saponins, sterols, tannins, anthraquinone, and reducing sugar. Methanol and ethanol extracts exhibited higher phenolic content as compare to aqueous extract. Antioxidant capacities were shown highest in methanol and ethanol extracts based on the test performed. The methanol and ethanol leaf extracts were found to be selectively cytotoxic in vitro to (DU-145 and PC-3) prostate cancer cell lines with IC50 values 529.44 ± 42.07 μg/mL and 677.11 ± 37.01 μg/mL for DU-145 and 547.55 ± 33.52 μg/mL and 631.99 ± 50.24 μg/mL for PC-3 respectively, while it had no cytotoxic effect on normal mice embryo fibroblast cells. Conclusion The results indicate that Leea indica was a promising antioxidant and anticancer agent for DU-145 and PC-3 human prostate cancer cell lines. However, further studies are needed to conclude its therapeutic use.

Natriuretic and saluretic effects of Hemidesmus indicus R. Br. root extracts in rats

Objective: The present study was aimed to investigate the diuretic effects of aqueous (AqE) and ethanolic (EtE) crude extracts of Hemidesmus indicus R. Br. roots (family – Asclepiadaceae) using acute model in rats. Materials and Methods: A single individual dose of AqE and EtE of H. indicus root (200 mg/kg and 400 mg/kg, p.o., each), frusemide and hydrochlorothiazide, (25 mg/kg, p.o., each) as reference diuretic drugs were administered orally to dehydrated rats. Control group rats were fed with normal saline (25 ml/kg, p.o.). All rats were caged in metabolic cages in a pairs and their urine output was monitored at 5 and 24 h intervals. Results: Both extracts significantly increased the urine output in higher doses. Although, the onset of this diuretic action was gradual (within 5 h), it lasted throughout the studied period (up to 24 h). Further, the intensity of diuresis induced by AqE (400 mg/kg) in 5 h was almost similar to that of frusemide and hydrochlothiazide. AqE of H. indicus root also caused marked increase in urinary Na+ and K+ levels. However, the routine urinalysis showed non-significant alterations in pH and specific gravity by either dose of crude extracts of H. indicus roots. Conclusions: These effects demonstrate possible diuretic actions of H. indicus root extracts and support its folklore use in various urinary ailments. Further study need to be done to characterize active phytoconstituents.

Design, synthesis and pharmacological analysis of 5-[4′-(substituted-methyl)[1,1′-biphenyl]-2-yl]-1H-tetrazoles

In the present paper 5-[4′-({4-[(4-aryloxy)methyl]-1H-1,2,3-triazol-1-yl}methyl)[1,1′-biphenyl]-2-yl]-1H-tetrazoles (5a–g) and [2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl-substituted-1-carbodithioates (11h–q) have been designed and synthesized. These compounds were subjected to docking (against AT1 receptor protein enzyme in complex with Lisinopril), in vitro angiotensin converting enzyme inhibition, anti-proliferative, anti-inflammatory screening (through egg albumin denaturation inhibition and red blood cell membrane stabilization assay) and finally anti-fungal activity analyses. Some of the compounds have shown significant pharmacological properties.

Some novel Schiff bases of [1,2,4]triazole bearing haloarene moiety—synthesis and evaluation of antituberculosis properties and neutrophil function test

A series of novel Schiff bases of [1,2,4]triazole-bearing haloarene moiety (5a–l) were synthesized from 4-amino-3-methyl-5-mercapto-4H-[1,2,4]triazole (3) and were confirmed by FT-IR, 1H-NMR, 13C-NMR, LC-Mass spectra and elemental analyses and screened for in vitro antituberculosis properties and for neutrophil function test, where they exhibited moderate neutrophil functions and antituberculosis properties. Compounds (5a), (5c), (5f), (5h) and (5i) were moderately sensitive to antituberculosis activity, while (5a), (5b), (5g) and (5h) were sensitive for neutrophil functions in the series. The acute oral toxicity studies on the Swiss albino mice according to the OECD/OCDE guidelines 423 confirmed that the compounds were slightly toxic and hence they may be considered as drug candidates for microbial pathogens. The antituberculosis studies by both ZOI and MIC tests confirmed that the novel derivatives are moderately sensitive towards Mycobacterium tuberculosis (H37RV) strain.

Phytosynthesis of gold nanoparticles: Characterization, biocompatibility, and evaluation of its osteoinductive potential for application in implant dentistry

Gold nanoparticles have been extensively used in diagnostics, biomedical imaging, and drug delivery owing to simple method of synthesis and versatile surface functionalization. Present investigation aims to evaluate the osteoinductive property of Salacia chinensis (SC) mediated gold nanoparticles (GNPs) for its application in implant dentistry. The formation of GNPs was assessed initially using the visual method and characterized analytically by using UV-visible spectroscopy, Zetasizer, X-RD, ICP-AES, AFM, and TEM. Green synthesized GNPs exhibited a remarkable stability in various blood components (0.2 M histidine, 0.2 M cysteine 2% bovine serum albumin, and 2% human serum albumin) and were found to be nontoxic when evaluated for their cytocompatibility and blood compatibility using periodontal fibroblasts and erythrocytes respectively. Exposure of GNPs to MG-63 cell lines displayed increased percent cell viability (138 ± 27.4) compared to the control group (96 ± 3.7) which confirms its osteoinductive potential. Herein, it can be concluded that the stable, biocompatible and eco-friendly GNPs can be used as an effective bone inductive agent during dental implant therapy.

Formulation of thermoreversible gel of cranberry juice concentrate: Evaluation, biocompatibility studies and its antimicrobial activity against periodontal pathogens

The present work aims to investigate the efficacy of thermoreversible gel of cranberry juice concentrate (CJC) as local drug delivery for the treatment of periodontitis. CJC was initially tested for its antimicrobial activities like MIC, MBC, antiadhesion, antibiofilm and time kill assay against the panel of organisms (S. mutans (SM), E. faecalis (EF), A. actinomycetemcomitans (AA), P. gingivalis (PG), T. forsythia (TF)) responsible for periapical and periodontal infections. Antimicrobial activity of CJC showed MIC value of 50mg/ml and MBC value of 100mg/ml with desirable antiadhesion (83-90%) and antibiofilm activity (70-85%). CJC was evaluated for its biocompatibility using periodontal fibroblasts by cell based MTT assay and found to be nontoxic. Influence of CJC on periodontopathogen PG derived virulence factors (fimA and kgp) was studied using real time polymerase chain reaction (RT-PCR) technique wherein down regulation of selected genes demonstrated inhibitory effect against PG virulence factors. Thermoreversible gel of CJC was formulated by cold method using poloxamer 407 as thermosensitive polymer and carbopol 934 as mucoadhesive polymer and evaluated for its gelation temperature, viscosity, gel strength and mucoadhesive strength. Comparison of optimized thermoreversible gel of CJC (500mg/ml) with commercially available chlorhexidine gluconate gel (0.2%) using agar well diffusion demonstrated equal zone of inhibition against SM, EF, AA, PG & TF. Hence the formulated thermoreversible gel of CJC could serve as a novel herbal alternative to currently available periodontal treatment modalities.

Effect of hydro-alcoholic extract of Vernonia cinerea Less. against ethylene glycol-induced urolithiasis in rats

Objective: Aim of this study is to evaluate antiurolithiatic potential of whole plant hydro-alcoholic (30:70) extract of Vernonia cinerea Less. in accordance to its claims made in ancient literature and also being one of the ingredients of cystone, a marketed formulation widely used in the management of urolithiasis. Materials and Methods: To induce urolithiasis, 0.75% v/v ethylene glycol was administered orally for 14 days. The curative dose of 400 mg/kg b.w. and preventive doses of 100, 200, and 400 mg/kg b.w. were administered from 15th to 28th and 1st to 28 days, respectively. Cystone 750 mg/kg b.w. was selected as the reference standard for both curative and preventive doses. On 28th day, urinate of 24 h was collected and subjected for estimation of calcium, oxalate, and phosphates. Serum biochemical and kidney homogenate analysis was done for determination of renal oxalate contents. Results: The diseased Group II showed marked increase (P < 0.001 vs. normal Group I) in levels of urine calcium, oxalate, and phosphate. Serum creatinine, urea, and uric acid levels were also increased. Histopathological studies of kidney sections revealed significant changes. Treatment with hydro-alcoholic extract of V. cinerea showed significant (P < 0.01 vs. calculi-induced Group II) dose-dependent activity. A progressive increase in urine output, body weight, and decline in concentrations of stone-forming components such as calcium, oxalates, and phosphates was observed. Conclusion: It can be inferred that V. cinerea Less. is effective in ethylene glycol-induced urolithiasis and may have a potential in preventing and curing urolithiasis.

Transition metal complexes of a hydrazone derived from hydralazine hydrochloride and 3,5-di-tert-butylsalicylaldehyde

Mononuclear Co(III), Ni(II) and Cu(II) coordination compounds of (E)-1-(3,5-di-tert-butyl-2-hydroxybenzylidene)-2-(phthalazin-1-yl)hydrazine (LH) were prepared and characterized by physicochemical and spectroscopic methods. The metal-to-ligand ratio was found to be 1:2 in [Co(L)2]Cl·2H2O (1) and [Ni(L)2]·2H2O (2), while it is 1:1 in [Cu(L)Cl]·2CH3OH (3). The X-ray crystal structures of LH and complex 1 is are reported. LH shows monobasic behavior, coordinating through NNO donor atoms. The complexes were investigated for their antimicrobial properties. Complexes 1 and 3 show excellent antibacterial and antifungal activities, respectively.