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Antidiabetic Activity of Ficusonolide, a Triterpene Lactone from Ficus foveolata (Wall. ex Miq.): In Vitro, In Vivo, and In Silico Approaches
ACS Omega ( IF 3.7 ) Pub Date : 2021-10-05 , DOI: 10.1021/acsomega.1c04230 Ala Ud Din 1 , Maria Khan 1 , Muhammad Zahir Shah 2 , Abdur Rauf 3 , Umer Rashid 4 , Anees Ahmed Khalil 5 , Khair Zaman 6 , Yahya S Al-Awthan 7, 8 , Mohammed A Al-Duais 9, 10 , Omar Bahattab 7 , Adil A H Mujawah 11 , Naveed Muhammad 12
ACS Omega ( IF 3.7 ) Pub Date : 2021-10-05 , DOI: 10.1021/acsomega.1c04230 Ala Ud Din 1 , Maria Khan 1 , Muhammad Zahir Shah 2 , Abdur Rauf 3 , Umer Rashid 4 , Anees Ahmed Khalil 5 , Khair Zaman 6 , Yahya S Al-Awthan 7, 8 , Mohammed A Al-Duais 9, 10 , Omar Bahattab 7 , Adil A H Mujawah 11 , Naveed Muhammad 12
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Diabetes is a chronic condition which is locally managed through the stem of Ficus foveolata. To find the exact chemical constituent responsible for this activity, a triterpene lactone (ficusonolide) isolated from F. foveolata was studied for antidiabetic potential through the in vitro antidiabetic paradigm employing L-6 cells and an in vivo antidiabetic assay against non-insulin-dependent rats. The results on glucose uptake in the L-6 cell line indicated that ficusonolide has enhanced the uptake of glucose by 53.27% over control at a dose of 100 μg/mL, while at doses of 50 and 25 μg/mL, the glucose uptake was enhanced by 22.42 and 14.34%, respectively. The extract of F. foveolata (100 mg/kg) and ficusonolide (50 mg/kg) demonstrated a significant (p < 0.001) decline in streptozotocin-induced hyperglycemia of diabetic rats. Ficusonolide displayed conspicuous inhibitory activity against the molecular docking studies with proteins such as dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase subjected to molecular targets. Detailed computational and structural insights affirmed promising interactions between target proteins and ficusonolide. In conclusion, the plant and its isolated compound have significant antidiabetic activity with a possible mechanism of interaction with DPP-IV, PTP-1B, α-glucosidase, and α-amylase.
中文翻译：
Ficusonolide（一种来自 Ficus foveolata (Wall. ex Miq.) 的三萜内酯）的抗糖尿病活性：体外、体内和计算机方法
糖尿病是一种慢性疾病，可通过小叶榕的茎进行局部治疗。为了找到负责这种活性的确切化学成分，通过使用 L-6 细胞的体外抗糖尿病范例和针对非胰岛素依赖性药物的体内抗糖尿病试验，研究了从F. foveolata中分离出的三萜内酯（ficusonolide）的抗糖尿病潜力。老鼠。 L-6细胞系葡萄糖摄取结果表明，在100 μg/mL剂量下，ficusonolid比对照增加了53.27%的葡萄糖摄取，而在50和25 μg/mL剂量下，葡萄糖摄取量较对照组提高了53.27%。分别提高了22.42%和14.34%。 F. foveolata (100 mg/kg) 和 ficusonolid (50 mg/kg) 的提取物显示出链脲佐菌素诱导的糖尿病大鼠高血糖显着下降 ( p < 0.001)。 Ficusonolide 对二肽基肽酶-IV (DPP-IV)、蛋白酪氨酸磷酸酶 1B (PTP-1B)、α-葡萄糖苷酶和 α-淀粉酶等蛋白质的分子对接研究显示出显着的抑制活性。详细的计算和结构见解证实了目标蛋白和无花果酸内酯之间有希望的相互作用。总之，该植物及其分离的化合物具有显着的抗糖尿病活性，其可能的机制是与 DPP-IV、PTP-1B、α-葡萄糖苷酶和 α-淀粉酶相互作用。
更新日期：2021-10-19
中文翻译：
Ficusonolide（一种来自 Ficus foveolata (Wall. ex Miq.) 的三萜内酯）的抗糖尿病活性：体外、体内和计算机方法
糖尿病是一种慢性疾病，可通过小叶榕的茎进行局部治疗。为了找到负责这种活性的确切化学成分，通过使用 L-6 细胞的体外抗糖尿病范例和针对非胰岛素依赖性药物的体内抗糖尿病试验，研究了从F. foveolata中分离出的三萜内酯（ficusonolide）的抗糖尿病潜力。老鼠。 L-6细胞系葡萄糖摄取结果表明，在100 μg/mL剂量下，ficusonolid比对照增加了53.27%的葡萄糖摄取，而在50和25 μg/mL剂量下，葡萄糖摄取量较对照组提高了53.27%。分别提高了22.42%和14.34%。 F. foveolata (100 mg/kg) 和 ficusonolid (50 mg/kg) 的提取物显示出链脲佐菌素诱导的糖尿病大鼠高血糖显着下降 ( p < 0.001)。 Ficusonolide 对二肽基肽酶-IV (DPP-IV)、蛋白酪氨酸磷酸酶 1B (PTP-1B)、α-葡萄糖苷酶和 α-淀粉酶等蛋白质的分子对接研究显示出显着的抑制活性。详细的计算和结构见解证实了目标蛋白和无花果酸内酯之间有希望的相互作用。总之，该植物及其分离的化合物具有显着的抗糖尿病活性，其可能的机制是与 DPP-IV、PTP-1B、α-葡萄糖苷酶和 α-淀粉酶相互作用。
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