MARTINELLINE AND MARTINELLIC ACID, NOVEL G-PROTEIN LINKED RECEPTOR ANTAGONISTS FROM THE TROPICAL PLANT MARTINELLA-IQUITOSENSIS (BIGNONIACEAE)
MARTINELLINE AND MARTINELLIC ACID, NOVEL G-PROTEIN LINKED RECEPTOR ANTAGONISTS FROM THE TROPICAL PLANT MARTINELLA-IQUITOSENSIS (BIGNONIACEAE)
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DOI：
10.1021/ja00130a005
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发表时间：
1995-06-28
影响因子：
15
通讯作者：
VARGA, SL
中科院分区：
文献类型：
--
作者：
WITHERUP, KM;RANSOM, RW;VARGA, SL
从伊基托马丁尼（Martinella iquitosensis）根的有机提取物中分离得到两种新的吡咯喹啉生物碱：马丁尼碱（martinelline，1）和马丁尼酸（martinellicacid，2）。在南美洲，两种马丁属物种作为眼部药物的民族植物学用途可能部分由1的存在和较小程度的2解释;本研究涉及1和2的缓激肽（BK）B-1和B-2受体拮抗剂活性以及1对组胺能、α（1）-肾上腺素能和毒蕈碱受体的亲和力。1和2代表迄今报道的唯一天然存在的非肽BK拮抗剂。还评价了这些化合物的抗菌潜力、细胞毒性和裂解活性。
Two novel pyrroloquinoline alkaloids, martinelline (1) and martinellic acid (2), were isolated from an organic extract of Martinella iquitosensis roots. The ethnobotanical use of the two Martinella species as an eye medication in South America may be explained in part by the presence of 1 and to a lesser extent 2; this study relates the bradykinin (BK) B-1 and B-2 receptor antagonist activity of 1 and 2 as well as the affinity of 1 for histaminergic, alpha(1)-adrenergic, and muscarinic receptors. 1 and 2 represent the only naturally occurring nonpeptide BK antagonists reported to date. The antibiotic potential, cytotoxicity, and lytic activity were also evaluated for these compounds.