Department of Biochemistry, University of Malakand, Chakdara 18800, Khyber Pakhtunkhwa, Pakistan.
Department of Botany, University of Malakand, Chakdara 18800, Khyber Pakhtunkhwa, Pakistan.
Molecules. 2021 Jul 24;26(15):4464. doi: 10.3390/molecules26154464.
The increase in resistance of microbes against conventional drugs is currently a hot issue, whereas diabetes is another main cause of mortalities encountered throughout the world after cancer and heart attacks. New drug sources in the form of plants are investigated to get effective drugs for the mentioned diseases with minimum side effects. Thunb. is a medicinal plant used for the management of stress related disorders like diabetes and other health complications. The active constituents of the chloroform extract derived from berries was isolated by silica gel column chromatography which were identified as morin, phloroglucinol, and 1-hexyl benzene through various spectroscopic techniques (electron ionization mass spectrometry, 1H-NMR, and 13C-NMR spectroscopy). The possible protective effects (antioxidant, antibacterial, and antidiabetic activity) of isolated compounds were evaluated using reported methods. Morin exhibited strong in vitro antiradical potential against DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid) radicals along with prominent antibacterial activities against selected bacterial strains (, , , , and ). Among the isolated compounds the more potent one (morin) was assessed for its in vivo antidiabetic potential in streptozotocin-induced diabetic rat model. The in vivo effects observed were further confirmed in ex vivo experiments where the effect of isolated compound on antioxidant enzyme like glutathione peroxidase (GPx), total content of reduced glutathione (GSH), % DPPH inhibition, and the lipid peroxidation MDA (Malondialdehyde) level in pancreatic tissues homogenates were evaluated. In vivo morin at tested doses (2, 10, 15, 30 and 50 mg/kg body weight) significantly restored the alterations in the levels of fasting blood glucose level and body weight loss along with significant decrease in levels of cholesterol, triglycerides, low density lipoprotein, HbA1c level, and significantly increased the high-density lipoprotein in diabetic rats. Morin also effectively ameliorated the hepatic enzymes, and renal functions like serum creatinine. Morin significantly increased the antioxidant enzyme like GPx activity, GSH content, and % DPPH inhibition activity, while reduced the lipid peroxidation MDA (malondialdehyde) level in pancreatic tissues homogenates, and modification of histopathological changes in diabetic rats. Morin exhibited high antioxidant, antibacterial, and antidiabetic potentials as compared to phloroglucinol and 1-hexyl benzene, that could, therefore, be considered as a promising therapeutic agent to treat diabetes mellitus and bacterial infections.
微生物对抗生素的耐药性增加是当前的一个热门话题,而糖尿病是继癌症和心脏病之后全球另一个主要的死亡原因。人们正在研究以植物为新来源的药物,以寻找具有最小副作用的治疗这些疾病的有效药物。Thunb. 是一种药用植物,用于治疗与糖尿病和其他健康并发症有关的应激障碍。通过各种光谱技术(电子电离质谱、1H-NMR 和 13C-NMR 光谱),从浆果的氯仿提取物中分离出硅胶柱色谱分离的活性成分,分别鉴定为杨梅素、间苯三酚和 1-己基苯。使用报道的方法评估了分离化合物的可能保护作用(抗氧化、抗菌和抗糖尿病活性)。杨梅素对 DPPH(2,2-二苯基-1-苦基肼)和 ABTS(2,2'-偶氮双-3-乙基苯并噻唑啉-6-磺酸)自由基具有很强的体外抗自由基潜力,对选定的细菌菌株(、、、、和)具有显著的抗菌活性。在分离的化合物中,更有效的化合物(杨梅素)在链脲佐菌素诱导的糖尿病大鼠模型中被评估其体内抗糖尿病潜力。在体内观察到的作用在离体实验中得到了进一步证实,其中分离化合物对抗氧化酶如谷胱甘肽过氧化物酶 (GPx)、还原型谷胱甘肽 (GSH) 的总含量、DPPH%抑制率以及胰腺组织匀浆中的丙二醛 (MDA) 水平的影响进行了评估。体内杨梅素在测试剂量(2、10、15、30 和 50mg/kg 体重)显著恢复了空腹血糖水平和体重减轻的改变,同时显著降低了胆固醇、甘油三酯、低密度脂蛋白、HbA1c 水平,并显著增加了糖尿病大鼠的高密度脂蛋白。杨梅素还有效改善了肝酶和肾功能,如血清肌酐。杨梅素显著增加了抗氧化酶如 GPx 活性、GSH 含量和 DPPH%抑制活性,同时降低了胰腺组织匀浆中的脂质过氧化 MDA(丙二醛)水平,并改善了糖尿病大鼠的组织病理学变化。杨梅素表现出高抗氧化、抗菌和抗糖尿病潜力,优于间苯三酚和 1-己基苯,因此可被视为治疗糖尿病和细菌感染的有前途的治疗剂。