- The effect of oxidation on berberine-mediated CYP1 inhibition: Oxidation behavior and metabolite-mediated inhibition
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The protoberberine alkaloid berberine carries methylenedioxy moiety and exerts a variety of pharmacological effects, such as antiinflammation and lipid-lowering effects. Berberine causes potent CYP1B1 inhibition, whereas CYP1A2 shows resistance to the inh
- Lo, Sheng-Nan,Shen, Chien-Chang,Chang, Chia-Yu,Tsai, Keng-Chang,Huang, Chiung-Chiao,Wu, Tian-Shung,Ueng, Yune-Fang
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- Method for synthesizing benzophenanthridine and protoberberine alkaloids through modular diversity regulation and control
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The invention discloses a method for synthesizing benzophenanthridine and protoberberine alkaloids through modular diversity regulation and control. The method comprises the following steps: improving a substituent group of a high-iodine salt leaving group, generating pyridine alkyne under the action of relatively mild potassium tert-butoxide, and carrying out [4 + 2] cycloaddition reaction on the pyridine alkyne and diene to obtain polysubstituted isoquinoline ring precursor compounds. Ring opening and aromatization of the isoquinoline ring precursor are realized by developing a novel iridium-catalyzed cross-coupling method, polysubstituted isoquinoline ring compounds with connecting capacity are efficiently synthesized, and then the polysubstituted isoquinoline ring compounds are coupled with a high-activity polysubstituted cyclic boric acid to obtain 3-aryl isoquinoline high-grade intermediates. Through application of two different chemical principles, regulation and control of the 3-aryl isoquinoline high-grade intermediates are realized, and benzophenanthridine and protoberberine alkaloids are modularly, diversely and efficiently synthesized.
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Paragraph 0391-0396
(2021/05/29)
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