Furan-Aspidospermine dimer or pharmaceutically acceptable salt thereof, and preparation method, use and pharmaceutical composition

• Main Authors: Simeng Zhao, Guisheng Zhong, Meifen Bao, Yang Yu, Xianghai Cai
• Format: Patent
• Language: English
• Published: 19.10.2022
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A furan-aspidospermine dimer of formula I or a pharmaceutically acceptable salt thereof is provided: wherein R1 and R1' are independently selected from hydrogen, hydroxyl and C1-6 alkyloxy; n is 0-4; R2, R2' and R2'' are selected from hydrogen, C1-6 alkyl; R3 and R3' are selected from hydrogen, hydroxyl and =O; R4 is selected from hydrogen and hydroxyl; R5 has no substituent or is =O; A-B is selected from -CH2CH2, -CH=CH-, -HOCH-CHOH-, -CH2-CHOH- or an epoxide; and the pharmaceutically acceptable salt is selected from an organic salt or an inorganic salt substituted at positions R2' and R2''. The organic salt may be a tartrate, citrate, formate, acetate or oxalate. The inorganic salt may be a hydrochloride, hydrobromide, nitrate, sulfate or phosphate. A preparation method of the furan-aspidospermine dimer comprising the steps: conducting leaching, extraction and gradient elution on a plant selected from the genus Ervatamia and genus Melodinus is provided. A pharmaceutical composition comprising the furan-aspidospermine dimer or pharmaceutically acceptable salt thereof is provided. The furan-aspidospermine dimer or a pharmaceutically acceptable salt thereof can activate an immune response by increasing a proportion of T lymphocytes and enhance a function of the immune response.