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Abstract Background Different plant parts of Roylea cinerea (D. Don) Baill. (Lamiaceae), Clematis grata Wall. (Ranunculaceae), Cornus capitata Wall. (Cornaceae) are traditionally used in the management of diabetes and various other diseases. Method The air-dried plant parts from different plants were coarsely powdered and macerated in methanol to obtain their crude extracts. The crude extracts were evaluated for their α-glucosidase inhibitory activity. On the basis of results obtained, the methanolic crude extract of Cornus capitata Wall. was further sequentially fractionated in hexane, diethyl ether, ethyl acetate, n-butanol. Fractions obtained were also evaluated for their α-glucosidase inhibitory potential. The kinetic study was performed using Lineweaver Burk plot to evaluate the type of inhibition. Furthermore, in silico analysis was also carried with active sites of the enzyme (PDB ID: 3WY1) using Autodock4. Results Among all the plant extracts, Cornus capitata extract showed maximum inhibitory activity. Therefore its methanolic extract was further fractionated with the help of different solvents and the maximum activity was shown by the ethyl acetate fraction (IC50 50 μg/mL). Kinetic analysis indicated that Vmax and Km were increased indicating a competitive type of inhibition. In docking studies, among different constituents known in this plant, betulinic acid showed minimum binding energy (− 10.21 kcal/mol). The kinetic and docking studies have strengthened the observation made in the present study regarding the α-glucosidase inhibitory activity of Cornus capitata. Conclusion The study provided partial evidence for pharmacological basis regarding clinical applications of Cornus capitata in the treatment of diabetes suggesting it to be a suitable candidate for the treatment of postprandial hyperglycemia.

Abstract Background The present study was carried out to prepare multi-herbal combination via comparing antioxidant activity and polyphenolic composition of five medicinal plant extracts of Punica granatum L., Putranjiva roxburghii Wall., Swertia chirata Buch.-Ham., Tinospora cordifolia (Willd.) Miers and Trigonella corniculata L. Methods The herbs were individually evaluated using in vitro antioxidant assays and analyzed by HPLC-PDA. The resultant data was examined using principal component analysis (PCA). Further, herbal combination was prepared on the basis of PCA. Results The PCA divided the plants into three groups. The leading or primary group contained P. granatum and P. roxburghii with the highest antioxidant activity strongly correlated with high amount of kaempferol. S. chirata was acknowledged as nourisher herb in one and T. cordifolia and T. corniculata were identified as stimulator herbs in other group. The herbal combination exhibited high antioxidant activity as compared to the individual plants. The combination revealed good antiproliferative efficacy against hepatocellular carcinoma (HepG2) cells with IC50 of 75.864 μg/ml. Conclusions The activity observed in vitro with HepG2 cells suggests that the herbal combination can provide therapeutic activity in vivo in future. The study may provide information regarding precise preparation of multi-herbal formulations using PCA as a tool in pharmaceutical industries.

Abstract Background Oxidative stress in an intracellular environment created by the accumulation of reactive oxygen species results in oxidative damage to biomolecules which ultimately become a hallmark for severe diseases like cancer, aging, diabetes, and cardiovascular and neurodegenerative diseases. Methods Various in vitro assays were employed to assess the antioxidant potential of strain, DNA protective activity was demonstrated using DNA nicking assay and cytotoxicity of the extract was evaluated using MTT assay. Further identification of the compounds was done using UPLC analysis. Results The extract of Streptomyces cellulosae strain TES17 demonstrated significant antioxidant activity with percentage inhibition of 78.47 ± 0.23, 91.08 ± 0.98 and 82.08 ± 0.93 for DPPH, ABTS and superoxide radical assays at 5 mg/mL, respectively. Total antioxidant and reducing power were found to be 76.93 ± 0.76 and 231.96 ± 0.51 mg AAE/100 mg of dry extract, respectively. Moreover, the extract was shown to inhibit lipid peroxidation upto 67.18 ± 1.9% at 5 mg/mL. TPC and TFC measured in the extract was 55 mg GAE/100 mg and 11.17 ± 4.05 mg rutin/100 mg, respectively. The protective nature of the TES17 extract to oxidative stress induced damaged DNA was shown by percentage of supercoiled DNA i.e. Form I was increased from 26.38 to 38.20% at concentrations ranging from 2 μg to 10 μg. TES17 extract also showed the cytotoxic activity against lung cancer cell line with 74.7 ± 1.33% inhibition whereas, limited toxicity was observed against normal cell line with percentage viability of 87.71 ± 6.66 at same concentration (30 μg/mL) tested. The antioxidant capacity of extract was well correlated with its TPC and TFC and this in turn was in keeping with the UPLC analysis which also revealed the presence of phenolic compounds that were responsible for the antioxidant and cytotoxic potential of S. cellulosae strain TES17. Conclusions The present study describes that S. cellulosae strain TES17 isolated from the rhizosphere of Camellia sinensis (tea) plant; produces potent compounds with antioxidant activity, further might be developed into therapeutic drugs to combat oxidative stress.

Abstract Cancer, the main cause of human deaths in the modern world is a group of diseases. Anticancer drug discovery is a challenge for scientists because of involvement of multiple survival pathways of cancer cells. An extensive study on the regulation of each step of these pathways may help find a potential cancer target. Up-regulated HIF-1 expression and altered metabolic pathways are two classical characteristics of cancer. Oxygen-dependent (through pVHL, PHDs, calcium-mediated) and independent (through growth factor signaling pathway, mdm2 pathway, HSP90) regulation of HIF-1α leads to angiogenesis, metastasis, and cell survival. The two subunits of HIF-1 regulates in the same fashion through different mechanisms. HIF-1α translation upregulates via mammalian target of rapamycin and mitogen-activated protein kinase signaling pathways, whereas HIF-1β through calmodulin kinase. Further, the stabilized interactions of these two subunits are important for proper functioning. Also, metabolic pathways crucial for the formation of building blocks (pentose phosphate pathway) and energy generation (glycolysis, TCA cycle and catabolism of glutamine) are altered in cancer cells to protect them from oxidative stress and to meet the reduced oxygen and nutrient supply. Up-regulated anaerobic metabolism occurs through enhanced expression of hexokinase, phosphofructokinase, triosephosphate isomerase, glucose 6-phosphate dehydrogenase and down-regulation of aerobic metabolism via pyruvate dehydrogenase kinase and lactate dehydrogenase which compensate energy requirements along with high glucose intake. Controlled expression of these two pathways through their common intermediate may serve as potent cancer target in future.