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马兜铃属植物的研究III. 印度马兜铃根中具有生育调节活性成分的分离与生物学评价

Studies on Aristolochia III. Isolation and biological evaluation of constituents of Aristolochia indica roots for fertility-regulating activity.

作者信息

Che C T, Ahmed M S, Kang S S, Waller D P, Bingel A S, Martin A, Rajamahendran P, Bunyapraphatsara N, Lankin D C, Cordell G A

出版信息

J Nat Prod. 1984 Mar-Apr;47(2):331-41. doi: 10.1021/np50032a017.

DOI:10.1021/np50032a017
PMID:6539809
Abstract

An ethanol extract of Aristolochia indica roots decreased fertility in both rats and hamsters when administered postcoitally (days 1-10 and 1-6, respectively). Petroleum ether (A), CHCl3 (B), and aqueous (C) fractions, tested similarly in rats, were inactive and/or toxic. Partition of fraction B afforded non-acidic (D) and acidic (E) fractions. Savinin (1), isolated from fraction D and not previously reported from the Aristolochiaceae , was inactive when administered postcoitally to rats. Aristolochic acid-I (2), reported previously from A. indica and isolated from fraction E, was inactive when administered postcoitally to rats and toxic when administered postcoitally to hamsters. (12S)-7,12- Secoishwaran -12-ol (3), previously reported from A. indica and isolated from fraction A, did not interrupt pregnancy when administered to mice on day 6 of pregnancy. Four additional compounds, aristolic acid (4) [prepared from aristolochic acid-I (2)], methyl aristolate (5) [prepared by methylating aristolic acid (4)], and cis- and trans-p-coumaric acid (both oblate commercially), were similarly tested in mice and found to be inactive. Aristolic acid (4), and the cis- and trans-p-coumaric acids also were inactive when administered postcoitally (days 1-10) to rats. Seven compounds reported previously from A. indica were also isolated, as were a new naphthoquinone, aristolindiquinone (6) (fraction E), and magnoflorine (fraction C).

摘要

印度马兜铃根的乙醇提取物在交配后给药时(分别在大鼠和仓鼠中为第1 - 10天和第1 - 6天)可降低生育能力。在大鼠中进行类似测试的石油醚(A)、氯仿(B)和水相(C)部分无活性和/或有毒。B部分的分离得到了非酸性(D)和酸性(E)部分。从D部分分离出的萨维宁(1),此前马兜铃科中未有报道,在大鼠交配后给药时无活性。此前从印度马兜铃中报道并从E部分分离出的马兜铃酸 - I(2),在大鼠交配后给药时无活性,而在仓鼠交配后给药时有毒。(12S)-7,12 - 断异细辛 - 12 - 醇(3),此前从印度马兜铃中报道并从A部分分离出,在妊娠第6天给小鼠给药时不会中断妊娠。另外四种化合物,马兜铃酸(4)[由马兜铃酸 - I(2)制备]、马兜铃酸甲酯(5)[通过甲基化马兜铃酸(4)制备]以及顺式和反式对香豆酸(均为市售扁圆形),在小鼠中进行了类似测试,发现无活性。马兜铃酸(4)以及顺式和反式对香豆酸在大鼠交配后给药(第1 - 10天)时也无活性。还分离出了此前从印度马兜铃中报道的七种化合物,以及一种新的萘醌,马兜铃二醌(6)(E部分)和木兰碱(C部分)。

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