Munish Garg

Prevalence of obesity in Indian women

Comparison of two major studies conducted by National family health survey (NFHS‐2) in 1998–1999 and NFHS‐3 in 2005–2006 shows that prevalence of obesity among Indian women has elevated from 10.6% to 12.6% (increased by 24.52%). The prevalence is more profound in the women of age between 40–49 years (23.7%), residing in cities (23.5%), having high qualification (23.8%), belonging to Sikh community (31.6%) and households in the highest wealth quintile (30.5%). Highest percentage of obese women is found in Punjab (29.9%). Although this number seems small in the international perspective, it is significant because of the sheer size of population in India. While the problem of under‐nutrition still exists in many parts of India, the additional burden of obesity due to increasing sedentary lifestyle, junk food habits in some urban and economically sound areas is really alarming. Prevention and control of this serious problem through awareness programmes to adopt diversified nutritional food and healthy lifestyle are strongly recommended.

A review of traditional use, phytoconstituents and biological activities of Himalayan yew, Taxus wallichiana.

Plants synthesize certain phytoconstituents for their protection, which, because they are not of primary need, are known as secondary metabolites. These secondary metabolites of plants, have often been found to have medicinal uses for human beings. One such gymnosperm having secondary metabolites of medicinal potential for humans is Taxus wallichiana (Himalayan yew). Besides being the source of taxol, this plant has been investigated for its essential oil, diterpenoids, lignans, steroids, sterols and biflavonoids. Traditionally, it is used to treat disorders of the digestive, respiratory, nervous and skeletal systems. Although pharmacologically underexplored, it has been used for antiepileptic, anti-inflammatory, anticancer, antipyretic, analgesic, immunomodulatory and antimicrobial activities. The present review compiles traditional uses, phytochemical constituents (specifically the secondary metabolites) pharmacological activities and the toxicity of T. wallichiana.

Development and optimization of boswellic acid-loaded proniosomal gel

Abstract Context: Boswellic acids (BAs) are isolated from oleo gum of Boswellia serrata and are mainly used as potential anti-inflammatory, hypolipidemic, immunomodulatory, and antitumor agents. Pharmacokinetic investigations of BAs uncover its poor bioavailability through digestive system thus creates a need for improved therapeutic responses which can possibly be achieved by developing formulations through novel delivery system. Objective: Present study was conducted to design topical BA-loaded proniosomal gel for the management of inflammatory disorders with enhanced bioavailability. Materials and methods: Nonionic surfactant vesicles were prepared using the coacervation phase separation method. A central composite design was employed to statistically optimize formulation variables using Design-Expert software. Three independent variables were evaluated: amount of surfactant (X1), amount of soya lecithin (X2), and amount of cholesterol (X3). The encapsulation efficiency percentage (Y1) and particle size (Y2) were selected as dependent variables. Results and discussion: The optimum formulation (F10) displayed spherical bi-layered vesicles under transmission electron microscopy with optimum particle size of 707.9 nm and high entrapment efficiency as 98.52%. In vitro skin permeation study demonstrated the most sustained release of 84.83 ± 0.153 mg/cm2 in 24 h. Anti-inflammatory activity of the gel showed a significant (p < 0.001) higher percentage inhibition as compared to the marketed gel at the same dose. Conclusion: The present study exhibited that BA-loaded proniosomal gel was better in terms of absorption, bioavailability, and release kinetics.

Development of a new, rapid, and sensitive validated high-performance thin-layer chromatographic method for the estimation of berberine in Tinospora cordifolia

A straightforward, delicate, and fast elite thin-layer chromatographic system (high-performance thin-layer chromatography [HPTLC]) has been produced and validated for the quantitative determination of berberine in Tinospora cordifolia. The chromatographic development was completed on HPTLC plates precoated with silica gel 60 F254 utilizing a blend of methanol, acetic acid, and water (8:1:1, v/v) as the mobile phase. Detection was completed densitometrically at 366 nm. The RF estimation of berberine was observed to be 0.71 ± 0.02. The system was validated according to the International Conference on Harmonization (ICH) guidelines regarding linearity, precision, accuracy, robustness, and so forth. The calibration curve was observed to be straight over a scope of 120–360 ng spot−1 with a regression coefficient of 0.971. The accuracy was observed to be as high as 98.56%, and the relative standard deviation (% RSD) values for intra-day and between-day variations were under 2%. The system showed high affectability and specificity. The strategy is new, basic, and economical for the routine estimation of berberine in T. cordifolia plant tests to help the commercial ventures and, in addition, scientists for their quick touchy determination of critical phytoconstituent berberine, requiring little to no effort in routine examination.

NO-sGC-cGMP signaling influence the anxiolytic like effect of lithium in mice in light and dark box and elevated plus maze

Glutamate is an excitatory neurotransmitter implicated in the pathogenesis of psychiatric disorders. Glutamate results in the activation of an enzyme called glycogen synthase kinase-3 (GSK-3) acting through N-methyl-d-aspartate (NMDA) receptors. Impaired expression of GSK-3 affects behavior and neurochemicals level in the brain responsible for the pathogenesis of mood disorders. It has been reported that lithium acts as an inhibitor of GSK-3 and inhibit the enzyme GSK-3 in an uncompetitive manner. In the present study, anxiolytic like effect of lithium in mice is investigated through light and dark box (LDB) and elevated plus maze (EPM). Lithium (50, 100 and 200 mg/kg, i.p.) was administered to the mice to determine the anxiety related behavior. Results obtained suggests that the administration of lithium (100 mg/kg, i.p.) reversed the anxiety related behavior of mice and decreased the levels of glutamate and nitrite as compared to control. Glutamate acting through the NMDA receptor has been found to regulate the expression of enzyme neuronal nitric oxide synthase (nNOS), which is responsible for the release of nitric oxide (NO), suggesting a possible link between NO and GSK-3 also. Therefore, to determine the possible interaction with NO, sub-effective dose of lithium was administered in combination with NO donor i.e. l-Arginine (50 mg/kg, i.p.), NOS and soluble guanylate cyclase (sGC) inhibitor i.e. methylene blue (1 mg/kg, i.p.) and phosphodiesterase inhibitor i.e. sildenafil (1 mg/kg, i.p.). The results obtained demonstrated that the anxiolytic like effect of lithium was abolished by the pretreatment with NO donor and potentiated by the pretreatment with NOS inhibitor. Therefore, it is suggested that NO signaling pathway influence the anxiolytic like activity of lithium in mice, further suggesting the link between the GSK-3 and NO signaling in the regulation of anxiety related behavior.

Anxiolytic-like effect of pyridoxine in mice by elevated plus maze and light and dark box: Evidence for the involvement of GABAergic and NO-sGC-cGMP pathway

ABSTRACT Present study was carried out to investigate the ‘anxiolytic‐like’ effect of pyridoxine in mice. Pyridoxine (90, 180 and 360 mg/kg) was administered by intraperitoneal (i.p.) route to the experimental mice and anxiety‐related behavior was evaluated by light and dark box (LDB) and elevated plus maze (EPM) models. Glutamate, GABA and nitrite levels were also determined in the isolated whole brain of mice. It was observed that pyridoxine (180 mg/kg, i.p.) exerted ‘anxiolytic‐like’ effect in mice in EPM and LDB models. Also, there was a significant increase in the levels of GABA whereas; the levels of glutamate and nitrite were decreased as compared to the control group. Administration of pentamethylene tetrazole (PTZ; 20 mg/kg, i.p.) exerted anxiogenic effects in mice, but the combination of PTZ and pyridoxine (180 mg/kg, i.p.) abolished the ‘anxiolytic‐like’ effect of pyridoxine, thereby, suggesting the possible role of GABA in the ‘anxiolytic‐like’ effect of pyridoxine in mice. Further, the influence of NO‐sGC‐cGMP pathway was investigated by administering the sub‐effective dose of pyridoxine in combination with sub‐threshold doses of NO modulators i.e. l‐arginine (50 mg/kg, i.p.; NO donor); methylene blue (1 mg/kg, i.p.; NO and soluble guanylate cyclase inhibitor) and sildenafil (1 mg/kg, i.p.; phosphodiesterase inhibitor and cGMP modulator). It was observed that the ‘anxiolytic‐like’ effect of pyridoxine in mice was counteracted by the NO donor and potentiated by the NO inhibitors. Thus, the present study confirmed the involvement of GABAergic and NO‐sGC‐cGMP pathway in the ‘anxiolytic‐like’ effect of pyridoxine in mice. HighlightsPyridoxine exerted anxiolytic like effects in mice in EPM and LDB.Pyridoxine administration increased the levels of GABA and reduced the levels of glutamate and nitrite in the brain of mice.PTZ treatment in combination with pyridoxine abolished the anxiolytic like effects of pyridoxine in mice.NO‐sGC‐cGMP pathway influenced the anxiolytic like effects of pyridoxine in mice.

IN-VITRO HYPOGLYCEMIC EVALUATION OF FRACTIONS OF HYDRO-ACOHOLIC EXTRACT OF HEARTWOOD OF TECOMELLA UNDULATA LINN.

Objective: To screen α-amylase and α-glucosidase inhibitors from the different fractions of crude hydro-alcoholic extract of heartwood of Tecomella undulata Linn. Methods: Four fractions of crude hydro-alcoholic extract of heartwood of plant were used for in-vitro inhibitory assays against digestive enzymes: α-amylase and α-glucosidase. For assay, different concentrations (20, 40, 60, 80, 100 µg/ml) were used for all fractions. Standard protocol was used for preliminary phytochemical screening of different bioactive components present in all fractions. Results: The fractions have shown moderate to highest inhibitory activity against both enzymes. But, the strong inhibition was revealed by acetone fraction against α-amylase with very minimal inhibitory concentrations at IC 50 values when compared with a standard drug acarbose. Several medicinally active phytocomponents such as flavanoids, saponin, anthraquinones, tannins, triterpenoids and phenols were observed in all studied fractions. Conclusion: The different fractions prepared from crude hydro-alcoholic extract of heartwood of plant are capable of inhibiting α-amylase and α-glucosidase and it can be concluded that heartwood of Tecomella undulata Linn. is partially active against postprandial hyperglycemia, thus diabetes mellitus. Keywords: Tecomella undulata Linn., Diabetes mellitus, α-Amylase, α-Glucosidase.

Cytotoxic potential of few Indian fruit peels through 3-(4,5-dimethylthiazol-yl)-2,5-diphenyltetrazolium bromide assay on HepG2 cells.

Objective: To investigate in vitro anticancer activity of a few Indian fruit peels through 3-(4,5-dimethylthiazol-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against HepG2 cells. Materials and Methods: Hydroalcoholic extracts were prepared of five fruit peels, i.e., banana, lemon, guava, orange, and papaya by maceration and thereafter subjected for MTT assay to evaluate anticancer potential on HepG2 cells. Plant extract showed best activity was further fractionated with petroleum ether, chloroform, and ethyl acetate successively and screened again. Phytochemical analysis was then carried out to find out responsible components for the observed activity. Results: Out of the 40 samples from five fruit peel extracts with rich folklore usage, papaya extract showed maximum activity with least inhibitory concentration50 (IC50) value of 18.5 μg/ml. Further analysis after fractionation of the papaya peel extract, aqueous fraction showed the maximum inhibitory activity with least IC50 value of 17.3 μg/ml. Phytochemical analysis of the aqueous fraction of papaya peel extract revealed the presence of flavonoids and glycosides. Total flavonoid content found to be 72.25 mg/g. Conclusion: Papaya fruit extract demonstrated the best activity against MTT assay which may be due to the presence of flavonoids.

Neuropharmacological activities of Taxus wallichiana bark in Swiss albino mice

Aims: The bark of Taxus wallichiana is widely used for preparing a decoction and consumed as a tea by several tribal communities of the Indian subcontinent. The sedative, motor coordination, anxiolytic, and antidepressant effects of the hydroalcoholic extract of T. wallichiana bark and its ethylacetate fraction were evaluated in mice models of behavior analysis. Materials and Methods: The effects were evaluated on diazepam-induced sleeping time, elevated plus maze and light and dark box, and on the forced swimming test. General locomotor activity and motor coordination effects were evaluated in the actophotmeter and rota-rod tests respectively. Statistical Analysis: Results are expressed as mean ± standard error of the mean. Statistical analysis was performed using ANOVA, followed by post-hoc Dunnetts test. *P < 0.05, **P < 0.01, ***P < 0.001 were considered as significant. Results: Both the hydroalcoholic extract and ethylacetate fraction showed a marked decrease in latency of sleep onset, prolonged the diazepam-induced sleeping time, decreased spontaneous locomotor activity; whereas ethylacetate fraction produced anxiolytic and antidepressant activity. Conclusions: Both hydroalcoholic extract and its ethylacetate fraction of the bark of T. wallichiana have bioactive principles, which induce neuropharmacological changes.

Cardioprotective effect of ammonium glycyrrhizinate against doxorubicin-induced cardiomyopathy in experimental animals

Objective: The objective of this study was to evaluate the cardioprotective effect of herbal bioactive compound ammonium glycyrrhizinate against doxorubicin-induced cardiomyopathy, in experimental animals. Materials and Methods: Ammonium glycyrrhizinate (50, 100, 200 mg/kg, p.o.) was administered for four weeks in albino rats. Cardiomyopathy was induced with a dose of 2.5 mg/kg i.p. of doxorubicin on 1th, 7th, 14th, 21th, 28th day in the experimental animals. At the end of the experiment, on 29th day, serum and heart tissues were collected and hemodynamic, biochemical and histopathological studies were carried out. Results: Administration of doxorubicin in normal rats showed significant (P < 0.001) changes in body weight, feed intake, urine output, hemodynamic parameters like (blood pressure, heart rate, cardiac output) and in lipid profile (cholesterol, triglyceride, high density lipoprotein, low density lipoprotein, very low density lipoprotein) indicating cardiomyopathy symptoms. Animals treated with ammonium glycyrrhizinate significantly (P < 0.05) decreased triglyceride, cholesterol, low density lipoprotein (LDL) and very low density lipoprotein (VLDL) levels. Moreover, high density lipoprotein (HDL) levels increased in rats treated with ammonium glycyrrhizinate as compared with the normal group. Conclusion: Ammonium glycyrrhizinate is effective in controlling serum lipid profile and cardiac complications in experimentally induced cardiomyopathy in animals.