Antidiabetic and Antioxidant Activities of Indian Bay Leaf (Cinnamomum tamala (Buch.‐Ham.) T. Nees & Eberm.) Essential Oils Collected from Meghalaya

Article

作者: Kumar Chaudhary, Sushil ; Shukla, Jitendra K. ; Sharma, Nanaocha ; Bhowmick, Shovonlal ; Kharlyngdoh, Evanylla ; Thorat, Sunil S. ; Bhardwaj, Pardeep K. ; Kumar Mukherjee, Pulok

AbstractThe current work investigates the chemodiversity, in vitro antioxidant, α‐amylase and α‐glucosidase inhibitory potential of Cinnamomum tamala (CT) leaf essential oil (EO) collected from different localities of East Khasi Hills District of Meghalaya, India. Gas chromatography‐mass spectrometry (GC‐MS) analysis of all the extracted leaf essential oils facilitated the identification of several compounds in a variable range along with eugenol as the major component (74.79–95.12 %). CT8 exhibited the highest antioxidant activity (IC50=11.23±0.27 μg/mL for 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) and IC50=21.54±0.37 μg/mL for 2,2’‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid (ABTS) among all EO evaluated. The results showed that the ferric reducing antioxidant power (FRAP) and oxygen radical absorbance capacity (ORAC) values for CT8 were 83.26±1.92 μM trolox/g oil and 70.29±1.90 ascorbic acid equivalents (AAE)/g of oil. α‐amylase and α‐glucosidase inhibition were highest in sample CT8 with IC50 values of 3.62±0.42 μg/mL and 16.29±0.32 μg/mL respectively. Caryophyllene, cyclohexene, 1, 5, 5‐trimethyl‐6‐(2‐propenylidene), germacrene D and eugenol showed strong binding potential toward α‐amylase and α‐glucosidase. It concluded that the chemodiversity and antidiabetic potential of C. tamla oil from Khasi Hills have never been studied. It can be taken as a dietary supplement as an antioxidant and antidiabetic to control blood glucose.

2021-01-01·Biochemical Pharmacology2区 · 医学

Targeting of HER/ErbB family proteins using broad spectrum Sec61 inhibitors coibamide A and apratoxin A

2区 · 医学

Article

作者: Ruiz-Saenz, Ana ; Ishmael, Jane E ; Mattos, Daphne R ; Moasser, Mark M ; Paavilainen, Ville O ; Kawaguchi, Shinsaku ; Badr, Christian E ; Dolan, Brian P ; Serrill, Jeffrey D ; McPhail, Kerry L ; Oishi, Shinya ; Kazemi, Soheila

Coibamide A is a potent cancer cell toxin and one of a select group of natural products that inhibit protein entry into the secretory pathway via a direct inhibition of the Sec61 protein translocon. Many Sec61 client proteins are clinically relevant drug targets once trafficked to their final destination in or outside the cell, however the use of Sec61 inhibitors to block early biosynthesis of specific proteins is at a pre-clinical stage. In the present study we evaluated the action of coibamide A against human epidermal growth factor receptor (HER, ErbB) proteins in representative breast and lung cancer cell types. HERs were selected for this study as they represent a family of Sec61 clients that is frequently dysregulated in human cancers, including coibamide-sensitive cell types. Although coibamide A inhibits biogenesis of a broad range of Sec61 substrate proteins in a presumed substrate-nonselective manner, endogenous HER3 (ErbB-3) and EGFR (ErbB-1) proteins were more sensitive to coibamide A, and the related Sec61 inhibitor apratoxin A, than HER2 (ErbB-2). Despite this rank order of sensitivity (HER3 > EGFR > HER2), Sec61-dependent inhibition by coibamide A was sufficient to decrease cell surface expression of HER2. We report that coibamide A- or apratoxin A-mediated block of HER3 entry into the secretory pathway is unlikely to be mediated by the HER3 signal peptide alone. HER3 (G11L/S15L), that is fully resistant to the highly substrate-selective cotransin analogue CT8, was more resistant than wild-type HER3 but only at low coibamide A (3 nM) concentrations; HER3 (G11L/S15L) expression was inhibited by higher concentrations of either natural product. Time- and concentration-dependent decreases in HER protein expression induced a commensurate reduction in AKT/MAPK signaling in breast and lung cancer cell types and loss in cell viability. Coibamide A potentiated the cytotoxic efficacy of small molecule kinase inhibitors lapatinib and erlotinib in breast and lung cancer cell types, respectively. These data indicate that natural product modulators of Sec61 function have value as chemical probes to interrogate HER/ErbB signaling in treatment-resistant human cancers.

2019-01-01·Journal of Oleo Science4区 · 农林科学

Potent <i>in vitro</i> Anti-mouth Cancer (KB) and Immunostimulating Activities of the Job’s Tears (<i>Coix lachryma-jobi</i> Linn.) Seed Semi-purified Extract Cocktails Containing Linoleic Acid

4区 · 农林科学

Article

作者: Manosroi, Jiradej ; Kitdamrongtham, Worapong ; Manosroi, Worapaka ; Manosroi, Aranya ; Chankhampan, Charinya

The crude methanolic and hexane extracts of non-cooked, steamed and roasted from three Job's Tears cultivars were prepared and further semi-purified by liquid-liquid extraction techniques and silica gel column. The six single semi-purified extracts (F1-F6) were combined as nine cocktails (CT1, CT6, CT8, CT13, CT14, CT21, CT24, CT25 and CT31) according to the IC₅₀ values from the preliminary study and investigated for anti-proliferative and apoptotic induction on mouth cancer cell line (KB) and immunostimulating as well as antioxidative activities. The highest anti-proliferative activity was observed in CT13 showing the IC₅₀ value of 0.53±0.45 µg/mL which was higher than 5-fluorouracil and doxorubicin of 20.34 and 1.60 times, respectively. CT1 which was the combination of F1-F6 and CT13 which was the combination of F4-F6 exhibited significant strong synergistic activity with the combination index value (CI) of 0.28. CT1 at 200 µg/mL showed the highest percentages of apoptotic cells (40.65±10.97%) with no necrotic cells, but lower than cisplatin (100 µg/mL) of 2.18 times. CT14 gave the highest immunostimulating activity with the phagocytosis percentage of 13.0±1.7%, but lower than lipopolysaccharide of 1.08 times. CT31 gave the highest free radical scavenging and metal chelating activities with the SC₅₀ and MC₅₀ values of 0.73±0.07 and 1.99±0.24 µg/mL, but lower than ascorbic acid and EDTA of 18.25 and 4.33 times, respectively. The linoleic acid contents related to anti-cancer activity were also examined by HPLC. This study has demonstrated that CT1 composing of F1-F6 at the percentage ratio of 0.71:2.06:81.38: 8.47:4.92:2.46 was the potential cocktails of the semi-purified extracts from the Job's Tears which can be further developed as a novel active compound for oral cancer treatment.

100 项与 CT-8 (Channel) 相关的药物交易

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