No abstract

No abstract

The chemical examination of acetone extract of Dirinaria consimilis resulted in isolation of six depsides of which two novel metabolites namely antarvediside A (1) and antarvediside B (2) and four known metabolites i.e. sekikaic acid (3), atranorin (4), divaricatic acid (5) and 2’-O-methyl divaricatic acid (6). From the pharmacological screening of the isolates (1-6), it was found that 1 and 2 exhibited better inhibition of ABTS and superoxide free radicals than that of the standard and compound 4 showed significant inhibition of protein denaturation with IC50 value of 390 mg/mL with respect to indomethacin with 110 mg/mL. From the SRB assay results, the better IC50 values was determined by compound 2 of 10.5, 11.50 and 12.50 μg/mL on HeLa, MCF-7 and FADU cancer cell lines, respectively. Thus, the outcomes revealed that the D. consimilis is a new source to treat free radicals, inflammation and cancer.

Background: Lichen is a composite organism composed of fungus in association with algae or cyanobacteria. Particularly, lichen betide to mangroves are named as manglicolous lichens. From the folklore, lichen extracts were used in the management of many infections and diseases. Results: The chemical investigation of acetone extract of manglicolous lichen Roccella montagnei (RM-Ac) yielded nine known metabolites namely divarinolmonomethylether (1), ethyl divaricatinate (2), divarinol (3), orcinol (4), methyl 2,6-dihydroxy-4-methylbenzoate (5), haematommic acid (6), atranol (7), ethyl haematommate (8) and ethyl orsellinate (9). Except 4, all are for the first reported from this species. The RM-Ac and its metabolites (1-9) were screened for antioxidant (DPPH, ABTS and superoxide free radical assays), anti-inflammatory, anticancer (SRB assay using A549, DLD-1, FADU, HeLa and MCF-7) and acute toxicity studies. The pharmacological results showed that compounds 6 and 8 depicted potent inhibitory profile against ABTS free radical (with IC 50 value of 40.0 and 40.5 μg/mL, respectively) and protein denaturation (with IC 50 value of 435 and 403 μg/mL, respectively). LD 50 of RM-Ac was found to be above 2 g/Kg body weight. Moreover, the RM-Ac showed prominent inhibition of formalin-hind albino rat paw oedema at both the tested doses, i.e., 100 and 200 mg/Kg b.w than that of the standard drug (indomethacin). Furthermore, the compounds 6 and 8 exhibited significant degree of specificity against HeLa, FADU and A549; besides, they showed very little degree of specificity against NHME cell line specifying less toxicity to normal cells. Conclusion: It can be concluded that the manglicolous lichen R. montagnei has an aptitude to act against free radicals, inflammation and cancer, and the main metabolites responsible for its biological activity are 6 and 8.

Background: Traditionally, the whole plant of Cardiospermum canescens has wide applications in the management of oxidative stress and inflammation in Africa and Asia. The present study investigated the antioxidant, antiinflammatory, xanthine oxidase (XO) inhibitory, and anticancer activities of metabolites present in the crude methanolic extract of whole plant C. canescens (CCE). Results: Chemical examination of CCE revealed the presence of six known compounds (1-6). From the results of in vitro studies, it can confirm that CCE exhibited notably inhibition of DPPH and superoxide free radicals, along with COX-1, COX-2, 5-LOX, and XO enzymes. Compounds 2 and 3 showed significant inhibition of DPPH and superoxide free radicals. Also, compound 2 exhibited good inhibition of COX-1 and COX-2 enzyme with IC 50 of 87.0 and 88.0 μg/mL. Furthermore, CCE exhibited significant inhibition of 5-LOX and XO enzymes with IC 50 of 42.5 and 56.0 μg/mL, respectively, while standard with IC 50 of 42.5 and 56.0 μg/mL, respectively. Among the test series of cancer cell lines, compounds 2, 3, and CCE showed a significant percentage of cell growth lysis of DLD-1 with IC 50 values of 52.5, 72.5, and 32.5 μg/mL, respectively. Besides, all the metabolites and CCE showed a very weak degree of specificity against NHME, indicates less toxicity to normal cells. Conclusion: To conclude, the results of the present study indicated that the methanolic extract from the whole plant of C. canescens displayed antioxidant activity by inhibiting DPPH and superoxide free radicals; antiinflammatory effects by regulating enzymes COX-1, COX-2, 5-LOX, and XO; and anticancer activity by inhibiting the growth of MCF-7, DLD-1, HeLa, and A549. These activities can link to natural active compounds 2 and 3. This study supports the traditional uses of the root of C. canescens. These data findings suggest that C. canescens can be a promising natural source of biological medicines for oxidative stress, inflammation, gout, and cancer.