The most affordable type of tablet is the immediately compressible tablet, which uses microcrystalline cellulose (MCC), a popular pharmaceutical excipient, as a filler or binder. To make it compatible with different active drugs and excipients, we tried to change some physical properties of the MCC. In the current study, we used a chelating agent to pretreat the waste cotton before pulping, bleaching, and finally, hydrochloric acid degradation with a concentration of 2N at 100 °C temperature for 20 min to prepare MCC. The prepared MCC was treated with different concentrations of sodium hydroxide at room temperature or at −20 °C followed by precipitation with hydrochloric acid or ethanol with complete washing with distilled water till neutralization. Evaluation of the degree of polymerization (DP) and FT-IR spectrum confirm the identity of the microcrystalline cellulose. The DP was found to be 216. The bulk density of the unmodified MCC was 0.21 while that of modified MCC varied from 0.253 to 0.594. The modified MCC powder showed good flow properties compared to the unmodified MCC as evaluated by the Hausner index, Carr’s index and the angle of repose. The scanning electron microscopy (SEM) of the MCC revealed that the rod shape has been changed to an oval shape due to treatment with sodium hydroxide at −20 °C. The X-ray crystallographic (XRD) analysis indicated that the unmodified MCC and standard MCC showed the crystallinity index (CrI) value of 86.82% and 87.63%, respectively, while the value ranges from 80.18% to 60.7% among the modified MCC powder. The differences in properties of the MCC might be due to the variation of rearrangement of the cellulose chain among the MCC particles due to treatment with different concentrations of a base at different temperatures and precipitation environments. This has enabled us to prepare MCC with different properties which might be compatible with different drugs.
Obesity, a chronic disorder of global prevalence, is associated with major health problems leading to mortality. Because of the presence of diverse types of bioactive molecules in plants, attention is being concentrated on the exploration of plant-based drugs to treat the disease. Inhibition of pancreatic lipase by the natural compounds in plants is one of the popular mechanisms for the management of obesity. The current study investigates the mechanism of the anti-obesity effect of the ethanol extract of seeds of Syzygium cumini seeds and roots of Dioscoria bulbifera in fatty diet-induced obese white albino Wister rats (age 8-9 weeks, average weight 110±8 gm). The total phenolic substances present in the ethanol extract of S. cumini was 103.79±3.45 and that of and D. bulbifera was 69.31 ± 2.99 mg GAE/g of dry extract. Correlating the phenolic contents, we also got the DPPH antioxidant activity of the plant extracts. The IC50 value of ethanol extract of S. cumini, D. bulbifera and standard Butyrated hydroxyl toluene (BHT) was found to be 93.03±6.23, 177.13±7.52, and 10.84±0.92 µg/mL, respectively. The body weight of fatty diet-induced rats was significantly reduced by S. cumini, D. bulbifera ethanol extract with a dose of 500 mg/kg bw during 12 weeks of treatment. The anti-obesity effect of the plant extracts is comparable to that of Orlistat with a dose of 10 mg/kg bw. The Orlistat at a concentration of 0.1 mg/ml could be able to inhibit 95.71% activity of Porcine pancreatic lipase while the ethanol extract of S. cumini, D. bulbifera with a concentration of 1.0 mg/ml showed 60.84% and 54.59% of anti-lipase activity. Moreover, the increased TG, LDL and cholesterol in HFD induced rats were significantly reduced by the plant extract as well as Orlistat. Molecular Docking study reveals that quercetin and isoquercetin bind with the rat lipase enzyme at the same site as that of orlistat with high affinity. Taken together, we can conclude that the ethanol extracts of causes anti-obesity effect by inhibiting the pancreatic lipase enzyme.
Introduction: Liver being the most important metabolic organ of the body performs a wide variety of vital functions. Hepatic cell injury occurs by the activation of reactive oxygen species (ROS) by CCl 4 , xenobiotics and other toxic substances generated through cytochrome P450 dependent step resulting from covalent bond formation with lipoproteins and nucleic acids. Observing the alarming state of hepatotoxic patients worldwide, different medicinal plants and their properties can be explored to combat against such free radical degermation of liver. This paper evaluates the antioxidant property of Gynura procumbens in both in silico and in an in vivo assay, and its hepatoprotective activity in CCl 4 induced hepatotoxicity. Materials and Methods: Gynura procumbens leaves were collected and extracted using 50% ethanol. Required chemicals (CCl 4 ), standard drug (Silymarin) and blood serum analyzing kits were stocked. The in vivo tests were performed in 140 healthy Wister albino male rats under well controlled parameters dividing into 14 groups, strictly maintaining IEAC protocols. In silico molecular docking and ADMET studies were performed and the results were analyzed statistically. Results and discussion: The body weight increased significantly in CCl 4 induced, G. procumbens administered hepatotoxic rats. The increase in SGPT, SGOT, ALP, creatinine, LFH, triglycerides, LDL, SOD, MDA, total cholesterol, DNA fragmentation ranges, γGT levels of CCl 4 treated group was decreased by both standard drug Silymarin and G. procumbens leaf extract. On the other hand, G. procumbens increased HDL levels and displayed contrasting results in CAT level tests. Some results contradicted with the negative controlled group displaying varying efficacy between leaf extract and Silymarin. In the molecular docking analysis, G. procumbens phytoconstituents performed poorly against TGF-β1 compared to the control drug Galunisertib while 26 phytoconstituents scored better than the control, bezafibrate against PPAR-α. Flavonoids and phenolic compounds performed better than other constituents in providing hepatoprotective activity.