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Antineoplastic Constituents from the Chemical Diversified Extract of Radix puerariae
Author(s) -
Zhang JianLong,
Xu Wei,
Zhou ZhenRu,
Li Juan,
Jiang LinLin,
Zhang XingXiao,
Jiang RenWang
Publication year - 2019
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201800408
Subject(s) - chemistry , radix (gastropod) , chemical constituents , traditional medicine , food science , botany , chromatography , biology , medicine
To enhance the structural diversity of isoflavonoids and provide more derivatives for the biological screening, a semisynthetic mixture was generated by diversification of the crude extract of Radix puerariae ( Pueraria montana var . lobata ) through the chemical reaction with hydrazine hydrate. Eleven 3,4‐diarylpyrazoles ( 1 – 11 ) and two 5‐phenyl‐6‐benzyldihydropyridazinones ( 12 and 13 ) were isolated from the semisynthetic mixture, and their structures were identified by spectroscopic methods in combination with X‐ray crystallographic analysis. Among them, nine compounds ( 5 – 13 ) were new derivatives. All the compounds were evaluated on the inhibitory activities against the prostate cancer cell lines LNCaP and PC3. Compounds 12 and 13 were found to exhibit much more potent inhibitory activities against the androgen dependent LNCaP cells than the androgen independent PC3 cells. Rapid synthesis of new 3,4‐diarylpyrazoles and two 5‐phenyl‐6‐benzyldihydropyridazinones with significant biological activity highlights the great potential of one‐pot combinatorial modification for the diversification of natural products.