School of Life Sciences, University of KwaZulu-Natal, Durban, Westville 4000, South Africa.
Department of Biotechnology and Food Technology, Durban University of Technology, P.O. Box 1334, Durban 4000, South Africa.
Biomolecules. 2019 Sep 22;9(10):520. doi: 10.3390/biom9100520.
Diabetes mellitus (DM) is a chronic metabolic disorder which has become a major risk to the health of humankind, as its global prevalence is increasing rapidly. Currently available treatment options in modern medicine have several adverse effects. Thus, there is an urgent need to develop alternative cost-effective, safe, and active treatments for diabetes. In this regard, medicinal plants provide the best option for new therapeutic remedies desired to be effective and safe. Recently, we focused our attention on drimane sesquiterpenes as potential sources of antimalarial and antidiabetic agents. In this study, iso-mukaadial acetate (Iso) (), a drimane-type sesquiterpenoid from the ground stem bark of , was investigated for glucose uptake enhancement in the L6 rat myoblast cell line. In vitro assays with L6 skeletal muscle cells were used to test for cytotoxicity, glucose utilisation, and western blot analysis. Additionally, the inhibition of carbohydrate digestive enzymes and 1,1-diphenyl-2- picrylhydrazyl (DPPH) scavenging activity were analysed in vitro. The cell viability effect of iso-mukaadial acetate was the highest at 3 µg/mL with a percentage of 98.4. Iso-mukaadial acetate also significantly and dose-dependently increased glucose utilisation up to 215.18% (12.5 µg/mL). The increase in glucose utilisation was accompanied by enhanced 5' adenosine monophosphate-activated protein kinase (AMPK)and protein kinase B (AKT) in dose-dependent manner. Furthermore, iso-mukaadial acetate dose-dependently inhibited the enzymes α-amylase and α-glucosidase. Scavenging activity against DPPH was displayed by iso-mukaadial acetate in a concentration-dependent manner. The findings indicate the apparent therapeutic efficacy of iso-mukaadial acetate isolated from as a potential new antidiabetic agent.
糖尿病（DM）是一种慢性代谢紊乱疾病，其全球患病率迅速上升，已成为人类健康的主要风险因素。目前现代医学中的治疗选择有多种不良反应。因此，迫切需要开发替代的具有成本效益、安全且有效的糖尿病治疗方法。在这方面，药用植物为开发新的治疗方法提供了最佳选择，这些方法需要既有效又安全。最近，我们将注意力集中在裂烷倍半萜类化合物作为抗疟和抗糖尿病药物的潜在来源上。在这项研究中，从 的地茎皮中分离得到的裂烷型倍半萜iso-mukaadial 乙酸酯（Iso）（），用于研究其在 L6 大鼠成肌细胞系中增强葡萄糖摄取的作用。采用 L6 骨骼肌细胞进行体外测定，以测试细胞毒性、葡萄糖利用和 Western blot 分析。此外，还分析了体外抑制碳水化合物消化酶和 1,1-二苯基-2-苦基肼（DPPH）清除活性。iso-mukaadial 乙酸酯的细胞活力效应在 3 µg/mL 时最高，为 98.4%。Iso-mukaadial 乙酸酯还显著且剂量依赖性地增加了葡萄糖的利用，最高可达 215.18%（12.5 µg/mL）。葡萄糖利用的增加伴随着 5' 腺苷单磷酸激活蛋白激酶（AMPK）和蛋白激酶 B（AKT）的增强，呈剂量依赖性。此外，iso-mukaadial 乙酸酯剂量依赖性地抑制了α-淀粉酶和α-葡萄糖苷酶。Iso-mukaadial 乙酸酯对 DPPH 的清除活性呈浓度依赖性。这些发现表明，从 中分离得到的 iso-mukaadial 乙酸酯作为一种有潜力的新型抗糖尿病药物具有明显的治疗效果。
