Bangladesh is endowed with an abundance of excellent medicinal plant resources. A well‐known traditional medicinal plant Piper chaba H. from the Piperaceae family is rich in bioactive phytochemicals that have antidiarrheal, antimicrobial, analgesic, antioxidant, anticancer, and cytotoxic effects. This plant is locally known as “Chuijhal,” and the stem is used as spices. In the current research program, the stems of the P. chaba plant were selected and its chemical and biological investigations such as antidiarrheal, antimicrobial, and analgesic effects were performed. Moreover, docking models were accomplished by exploiting PyRx‐Virtual Screening software and implied that isolated compounds of P. chaba exert different pharmacological activity by inhibiting their targeted receptors. Phytochemical investigations revealed the isolation of Chingchengenamide A, a relatively rare alkaloid from the stems of P. chaba . Another alkaloid Chabamide I which is a piperine dimer was also isolated. Their structures were confirmed by comparing these compounds' spectral data ( 1 H and 13 C NMR) with their previously published spectral data. Antidiarrheal activity shows a percent reduction of diarrhea by 46.67% and 40%, respectively, for Chabamide I and Chingchengenamide A (at 20 mg/kg b.w.) compared with an 80% reduction by standard loperamide. Similarly, the percent reduction of writhing was 53.06% and 42.86%, respectively, for Chabamide I and Chingchengenamide A at similar doses compared with an 80% reduction by diclofenac sodium considered as standard. Both the alkaloids showed auspicious outcomes against test microorganisms during disk diffusion antimicrobial assay. Molecular docking and ADME/T analysis of the alkaloids also validate a potent pharmacological basis for the traditional utilization of P. chaba in treating diarrhea, pain, and microbial infection. These results emphasize the need to investigate P. chaba as a potential source of natural therapies for common health issues, laying the foundation for future research.
1 January 2017 in Asian Pacific Journal of Tropical Biomedicine
ObjectiveTo investigate the presence of different phytoconstituents in Mangifera indica (M. indica) peel and evaluate its cytotoxicity to Artemia salina and hypoglycemic potential in Swiss albino mice.MethodsThe methanolic extract of M. indica peel was used to determine the presence of phytoconstituents. Brine shrimp lethality bioassay method was followed to determine the cytotoxic potential of plant extract. In the case of hypoglycemic activity, oral administration of extract at 200 and 400 mg/kg and standard glibenclamide at 10 mg/kg was done, followed by determining the percentage of reduction of plasma glucose from the initial level.ResultsThe methanolic extract of M. indica peel showed the presence of flavonoid, saponin, steroid, tannins, terpenoids, glycosides and alkaloids. In brine shrimp lethality bioassay, the LC50 of the extract and standard vincristine sulfate was found to be 2.04 and 0.41 μg/mL, respectively. After 90 and 150 min, the methanolic extract at 200 and 400 mg/kg showed prominent plasma glucose reduction of 13.95%, 22.48% and 14.16%, 26.18% respectively compared to standard glibenclamide showing 14.90% and 20.67% plasma glucose reduction.ConclusionsThis current research affirms prominent cytotoxic and moderate hypoglycemic potential of M. indica peel. Further bioactivity guided isolation of phytoconstituents and investigation on higher animals can lead to development of new drug molecules
Clitoria ternatea L. (CT) is a perennial herbaceous plant with deep blue flowers native to tropical Asia. This work explores the endometrial pain (EP) regulation of CT flower through a multifaceted approach. Phytochemical screening unveiled the presence of alkaloids, steroids, flavonoids, glycosides, and tannins in CT flower methanolic extract (ME). In the in vitro membrane stabilizing experiment, the ME demonstrated 91.47% suppression of heat-induced hemolysis. Upon carrageenan-induced paw edema assay conducted on male Swiss albino mice at doses of 200 mg/kg and 400 mg/kg, 65.28% and 81.89% inhibition rates, respectively, of paw edema were reported. For the same doses, upon acetic acid-induced-writhing assay, 75.6% and 76.78% inhibition rates, respectively, were observed. For network pharmacology analyses, a protein–protein interaction network was constructed for 92 overlapping gene targets of CT and EP, followed by GO and KEGG pathway enrichment analyses. Network pharmacology-based investigation identified the anti-EP activity of CT to be mostly regulated by the proteins SRC homology, ESR1, and PI3KR1. Physicochemical, pharmacokinetic, and toxicity property predictions for the compounds with stable ligand–target interactions and a molecular dynamics simulation for the highest interacting complex further validated these findings. This work affirmed the anti-EP role of CT flower against EP, suggesting a probable molecular mechanism involved.
Here, we describe the anticancer activity of our novel bis-triazoles MS47 and MS49, developed previously as G-quadruplex stabilizers, focusing specifically upon the human melanoma MDA-MB-435 cell line. At the National Cancer Institute (NCI), USA, bis-triazole MS47 (NCS 778438) was evaluated against a panel of sixty human cancer cell lines, and showed selective, distinct multi-log differential patterns of activity, with GI50 and LC50 values in the sub-micromolar range against human cancer cells. MS47 showed highly selective cytotoxicity towards human melanoma, ovarian, CNS and colon cancer cell lines; in contrast, the leukemia cell lines interestingly showed resistance to MS47 cytotoxic activity. Further studies revealed the potent cell growth inhibiting properties of MS47 and MS49 against the human melanoma MDA-MB-435 cell line, as verified by MTT assays; both ligands were more potent against cancer cells than MRC-5 fetal lung fibroblasts (SI > 9). Melanoma colony formation was significantly suppressed by MS47 and MS49, and time- and dose-dependent apoptosis induction was also observed. Furthermore, MS47 significantly arrested melanoma cells at the G0/G1 cell cycle phase. While the expression levels of Hsp90 protein in melanoma cells were significantly decreased by MS49, corroborating its binding to the G4-DNA promoter of the Hsp90 gene. Both ligands failed to induce senescence in the human melanoma cells after 72 h of treatment, corroborating their weak stabilization of the telomeric G4-DNA.
24 January 2020 in Clinical Hemorheology and Microcirculation
BACKGROUND: Microvascular dysfunction is a main contributor to morbidity and mortality worldwide. Sophisticated technical tools (e.g. miniaturizedhardware, automated software), along with skilled personnelare the prerequisite for quantitative observa