Effect of a novel biphenyl compound, VMNS2e on ob/ob mice

Kurundkar, Sucheta Banerjee; Sachan, Narsingh; Kodam, Kisan M.; Kulkarni, Vithal M.; Bodhankar, Subhash L.; Ghole, Vikram S.

doi:10.1016/j.ejphar.2010.09.067

Cited by 4 publications

(1 citation statement)

References 44 publications

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“…Interestingly, the SAR study revealed that the compounds' activity against both AMPK and PTP1B shows an inverse correlation with the number of H‐bond acceptors, suggesting that binding might be impaired by repulsive interactions (Figure 3). Generally, activity against both enzyme is strongly associated with the presence of unfunctionalized biphenyl moiety, which corresponds to the previously reported data (Kurundkar et al, 2011; Lan et al, 2017; Spasov, Zhukovskaya, et al, 2017). For PTP1B, N , N ‐dimethylaminoethyl‐ and 2‐piperidinoethyl side chains also benefited the inhibitory activity.…”

Section: Resultssupporting

confidence: 91%

Discovery and evaluation of biphenyl derivatives of 2‐iminobenzimidazoles as prototype dual PTP1B inhibitors and AMPK activators with in vivo antidiabetic activity

et al. 2023

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This work describes the synthesis of series hydrobromides of N-(4-biphenyl) methyl-N′-dialkylaminoethyl-2-iminobenzimidazoles, which, due to the presence of two privileged structural fragments (benzimidazole and biphenyl moieties), can be considered as bi-privileged structures. Compound 7a proved to activate AMP-activated kinase (AMPK) and simultaneously inhibit protein tyrosine phosphatase 1B (PTP1B) with similar potency. This renders it an interesting prototype of potential antidiabetic agents with a dual-target mechanism of action.Using prove of concept in vivo study, we show that dual-targeting compound 7a has a disease-modifying effect in a rat model of type 2 diabetes mellitus via improving insulin sensitivity and lipid metabolism.

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Section: Resultssupporting

confidence: 91%

Discovery and evaluation of biphenyl derivatives of 2‐iminobenzimidazoles as prototype dual PTP1B inhibitors and AMPK activators with in vivo antidiabetic activity

et al. 2023

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Effects of blue honeysuckle containing anthocyanin on anti-diabetic hypoglycemia and hyperlipidemia in ob/ob mice

Lee

Chun³

et al. 2022

Journal of Functional Foods

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Antiobese and Antidiabetic Effects of Yookmijihwang-tang-gamibang, a Traditional Polyherbal Formula on the Obese and Type II Diabetic C57BL/6JHam-ob/ob Mice

Kim¹,

Kang²

2013

Herbal Formula Science

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Objectives : The object of this study was to observe the pharmacological effects of Yookmijihwang-tang-gamibang (Liuweidihuang-tang-jiaweifang, YGB) consisted of 17 types of herbs has been traditionally used in Korean medicine for treating various disorders in clinics, aqueous extracts on the genetically obese and type II diabetic C57BL/6JHam-ob/ob(ob/ob) mice.Methods :Three different dosages of YGB were orally administered, once a day for 28 days to ob/ob mice with ob/ob control and C57BL/6JJms normoglycemic intact mice. Four weeks after treatments of YGB: the changes on the body weight, food consumption, blood glucose levels, leptin and adiponectin contents were observed for monitoring the antiobese and antidiabetic effects of YGB. The effects were compared to those of CLA(conjugated linoleic acid) which improve type II diabetes and inhibit related obesity.

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Effect of a novel biphenyl compound, VMNS2e on ob/ob mice

Cited by 4 publications

References 44 publications

Discovery and evaluation of biphenyl derivatives of 2‐iminobenzimidazoles as prototype dual PTP1B inhibitors and AMPK activators with in vivo antidiabetic activity

Discovery and evaluation of biphenyl derivatives of 2‐iminobenzimidazoles as prototype dual PTP1B inhibitors and AMPK activators with in vivo antidiabetic activity

Effects of blue honeysuckle containing anthocyanin on anti-diabetic hypoglycemia and hyperlipidemia in ob/ob mice

Antiobese and Antidiabetic Effects of Yookmijihwang-tang-gamibang, a Traditional Polyherbal Formula on the Obese and Type II Diabetic C57BL/6JHam-ob/ob Mice

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