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Synthesis and Biological Evaluation of Decursinol Derivatives as FoxO-1 Inhibitors in HepG2 Cells
주정호,정선화,유국현,천혜경 대한화학회 2019 Bulletin of the Korean Chemical Society Vol.40 No.8
Diabetes mellitus type 2 is caused by insulin resistance, often associated with increased hepatic gluconeogenesis. Forkhead box O-1 (FoxO-1) is known as a major transcription factor regulating hepatic gluconeogenesis, and the increased FoxO-1 expression and activity are mainly observed in type 2 diabetic patients. To discover new FoxO-1 inhibitors, the compounds were newly synthesized from decursinol, which is a molecule isolated from the Angelica gigas and proved to be safe. The compounds were evaluated for in vitro FoxO-1 inhibitory activity using FoxO-1 reporter assay in HepG2 cells. Among these, the compounds 2b and 2c exhibited FoxO-1 inhibitory activity with IC50 values of 98.9 and 123.7 ?M, respectively. Moreover, the blood glucose level reduction efficacy of synthesized compound 2b was found similar to that of glimepiride, a commercially available antidiabetic drug and used as a reference (21.6 vs. 21.4%), in alloxan-induced type 2 diabetes rats. These findings suggest that, the compound 2b has moderate inhibitory activity on FoxO-1 and possibly resulting in the amelioration of diabetic hyperglycemia.
Synthesis and In Vivo Evalution of Decursinol Derivatives as Antidiabetics
주정호,권호석,이재응,유국현 대한화학회 2017 Bulletin of the Korean Chemical Society Vol.38 No.9
There are currently no diabetes drugs that can reduce blood glucose without causing adverse secondary effects. In this study, we report the synthesis of various compounds derived from decursinol, a molecule isolated from Angelica gigas with proven safety. The blood glucose reduction efficacy of synthesized compound 11 was equivalent to that of glimepiride, a commercially available diabetes drug used as a reference (21.6% vs. 21.4%), which was confirmed in rat and mouse models of diabetes. Compound 11 is a nonsulfonyl urea class substance that is predicted to be highly effective in reducing blood glucose while having few adverse effects, indicating that it is potential candidate drug for diabetes treatment that circumvents the limitations of existing therapeutics.
Bruceantin 유사체의 전합성에 대한 연구 (Ⅰ)
주정호,최정진,김홍범,Ju, Jeong Ho,Choe, Jeong Jin,Kim, Hong Beom 대한화학회 1994 대한화학회지 Vol.38 No.1
Bruceantin유사체 전합성의 중요한 중간체인 ethyl $({\pm})$-8-oxo-10-oxa-l'H-spiro[1, 3]dioxolane-4,4'-tricyclo [9.2.1.0 1,6]dodec-6-ene-9-carboxylate (7)의 합성경로를 개발하였다. 시작물질로서 ethyl 2-cyclohexanonecarboxylate and methyl vinyl ketone을 사용하여, Robinson annulation, allylic oxidation등을 응용하였으며, regiospecific acylation and the formation of epoxy methano bridge 형성 반응 등이 연구되었다. Actalone (3)의 ketalization 반응에서 새로운 decarboethoxylation 반응을 발견하였으며, 이 반응을 이용하여 3차 알코올과 엔온을 가지고 있는 4,4a,5,6,7,8-Hexahydro-4a-hydroxy-2(3H)naphthalenone (14)를 합성하였다. The synthetic pathway of ethyl $({\pm})$-8-oxo-10-oxa-l'H-spiro[1, 3]dioxolane-4,4'-tricyclo [9.2.1.0 1,6]dodec-6-ene-9-carboxylate (7), an important intermediate for the total synthesis of bruceantin analogue, was developed. Ethyl 2-cyclohexanonecarboxylate and methyl vinyl ketone were employed as starting materials. Robinson annulation, allylic oxidation, regiospecific acylation and the formation of epoxy methano bridge ring were studied. 4,4a,5,6,7,8-Hexahydro-4a-hydroxy-2(3H)naphthalenone (14) was synthesized utilizing the unusual decarboethoxylation reaction discovered during ketalization of octalone (3).