Antihyperglycemic activity with DPP-IV inhibition of alkaloids from seed extract of Castanospermum australe: Investigation by experimental validation and molecular docking

被引：51

作者：

Bharti, Sudhanshu Kumar ^{[1
]}

Krishnan, Supriya ^{[2
]}

Kumar, Amit ^{[3
]}

Rajak, Kaushal Kishore ^{[4
]}

Murari, Krishna ^{[5
]}

Bharti, Binod Kumar ^{[5
]}

Gupta, Ashok Kumar ^{[1
,6
]}

机构：

[1] Univ Patna, Dept Biochem, Patna 800005, Bihar, India

[2] Magadh Univ, Global Entrepreneurship & Management Acad, Patna, Bihar, India

[3] Jawaharlal Nehru Univ, Sch Computat & Integrat Sci, New Delhi 110067, India

[4] Indian Vet Res Inst, Div Virol, Naini Tal, Uttarakhand, India

[5] Bihar Agr Univ, Sanjay Gandhi Inst Dairy Technol, Sabour, Bihar, India

[6] Natl Inst Pharmaceut Educ & Res, Dept Biotechnol, Hajipur, Bihar, India

来源：

PHYTOMEDICINE | 2012年 / 20卷 / 01期

关键词：

Type; 2; diabetes; Insulin resistance; Hyperglycemia; Glucose tolerance; DPP-IV inhibitor; DIPEPTIDYL-PEPTIDASE-IV; GLUCAGON-LIKE PEPTIDE-1; INSULIN-RESISTANCE; TYPE-2; SAXAGLIPTIN; POTENT; DRUG; DEGRADATION; ALOGLIPTIN; MANAGEMENT;

D O I：

10.1016/j.phymed.2012.09.009

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

The antidiabetic actions of Castanospermum australe Cunn., seed (CAS) extract were evaluated in Poloxamer-407 (PX-407) induced T2DM rats. The CAS extract (100 and 150 mg/kg body weight) was administered orally once a day for 5 weeks after the animals were confirmed diabetic. A significant increase in blood glucose, HbA(1)c and serum insulin levels were observed in T2DM rats in comparison to citrate control rats. Treatment with CAS extract in T2DM rats reduced the elevated levels of blood glucose, HbA(1)c and insulin with significant (p <= 0.001) improvement in OGT. The CAS extract treatment also increased (p <= 0.001) the K-ITT and prevented increase in HOMA-R level in 12DM rats. The DPP-IV inhibitory potential of CAS extract showed IC50 value of 13.96 mu g/ml whilst the standard Diprotin A displayed the IC50 value of 1.543 mu g/ml. Molecular docking of the three reported alkaloids from the seeds of C. australe showed comparable DPP-IV inhibition with berberine. Our data suggest that CAS extract (150 mg/kg body weight) normalizes hyperglycemia in T2DM rats with strong DPP-IV inhibitory potential. The molecular docking showed that among the three alkaloids of seed extract 7-Deoxy-6-epi-castanospermine is a potent DPP-IV inhibitor similar to berberine. (C) 2012 Elsevier GmbH. All rights reserved.

引用

页码：24 / 31

页数：8

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