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使用岩藻依聚糖和阿卡波糖联合抑制2型糖尿病相关酶的方法。

A Combination Approach in Inhibiting Type 2 Diabetes-Related Enzymes Using Fucoidan and Acarbose.

作者信息

Mabate Blessing, Daub Chantal Désirée, Malgas Samkelo, Edkins Adrienne Lesley, Pletschke Brett Ivan

机构信息

Enzyme Science Programme (ESP), Department of Biochemistry and Microbiology, Faculty of Science, Rhodes University, Makhanda 6140, South Africa.

Department of Biochemistry, Genetics and Microbiology, University of Pretoria, Pretoria 0028, South Africa.

出版信息

Pharmaceutics. 2021 Nov 22;13(11):1979. doi: 10.3390/pharmaceutics13111979.

Abstract

Although there are chemotherapeutic efforts in place for Type 2 diabetes mellitus (T2DM), there is a need for novel strategies (including natural products) to manage T2DM. Fucoidan, a sulphated polysaccharide was extracted from . The integrity of the fucoidan was confirmed by structural analysis techniques such as FT-IR, NMR and TGA. In addition, the fucoidan was chemically characterised and tested for cell toxicity. The fucoidan was investigated with regards to its potential to inhibit α-amylase and α-glucosidase. The fucoidan was not cytotoxic and inhibited α-glucosidase (IC 19 µg/mL) more strongly than the standard commercial drug acarbose (IC 332 µg/mL). However, the fucoidan lacked potency against α-amylase. On the other hand, acarbose was a more potent inhibitor of α-amylase (IC of 109 µg/mL) than α-glucosidase. Due to side effects associated with the use of acarbose, a combination approach using acarbose and fucoidan was investigated. The combination showed synergistic inhibition (>70%) of α-glucosidase compared to when the drugs were used alone. The medicinal implication of this synergism is that a regimen with a reduced acarbose dose may be used, thus minimising side effects to the patient, while achieving the desired therapeutic effect for managing T2DM.

摘要

尽管目前已有针对2型糖尿病(T2DM)的化疗方法,但仍需要新的策略(包括天然产物)来管理T2DM。从……中提取了一种硫酸化多糖岩藻依聚糖。通过傅里叶变换红外光谱(FT-IR)、核磁共振(NMR)和热重分析(TGA)等结构分析技术确认了岩藻依聚糖的完整性。此外,对岩藻依聚糖进行了化学表征并测试了其细胞毒性。研究了岩藻依聚糖抑制α-淀粉酶和α-葡萄糖苷酶的潜力。岩藻依聚糖无细胞毒性,且比标准商业药物阿卡波糖(IC 332 µg/mL)更强烈地抑制α-葡萄糖苷酶(IC 19 µg/mL)。然而,岩藻依聚糖对α-淀粉酶缺乏效力。另一方面,阿卡波糖对α-淀粉酶(IC为109 µg/mL)的抑制作用比对α-葡萄糖苷酶更强。由于使用阿卡波糖存在副作用,因此研究了使用阿卡波糖和岩藻依聚糖的联合方法。与单独使用药物相比,联合用药对α-葡萄糖苷酶表现出协同抑制作用(>70%)。这种协同作用的医学意义在于,可以使用降低剂量的阿卡波糖方案,从而将对患者的副作用降至最低,同时实现管理T2DM的理想治疗效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b4ef/8619669/022813b2f14d/pharmaceutics-13-01979-g001.jpg

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