Schmeller T, Latz-Brüning B, Wink M
Institut für Pharmazeutische Biologie, Universität Heidelberg, Germany.
Phytochemistry. 1997 Jan;44(2):257-66. doi: 10.1016/s0031-9422(96)00545-6.
The alkaloids berberine, palmatine and sanguinarine are toxic to insects and vertebrates and inhibit the multiplication of bacteria, fungi and viruses. Biochemical properties which may contribute to these allelochemical activities were analysed. Acetylcholine esterase, butyrylcholinesterase, choline acetyl transferase, alpha 1- and alpha 2-adrenergic, nicotinergic, muscarinergic and serotonin2 receptors were substantially affected. Sanguinarine appears to be the most effective inhibitor of choline acetyl-transferase (IC50 284 nM), while the protoberberines were inactive at this target. Berberine and palmatine were most active at the alpha 2-receptor (binding with IC50 476 and 956 nM, respectively). Furthermore, berberine and sanguinarine intercalate DNA, inhibit DNA synthesis and reverse transcriptase. In addition, sanguinarine (but not berberine) affects membrane permeability and berberine protein biosynthesis. In consequence, these biochemical activities may mediate chemical defence against microorganisms, viruses and herbivores in the plants producing these alkaloids.
生物碱小檗碱、巴马汀和血根碱对昆虫和脊椎动物有毒，并能抑制细菌、真菌和病毒的繁殖。分析了可能导致这些化感物质活性的生化特性。乙酰胆碱酯酶、丁酰胆碱酯酶、胆碱乙酰转移酶、α1和α2肾上腺素能、烟碱能、毒蕈碱能和5-羟色胺2受体均受到显著影响。血根碱似乎是胆碱乙酰转移酶最有效的抑制剂（IC50为284 nM），而原小檗碱在该靶点上无活性。小檗碱和巴马汀在α2受体上活性最高（结合IC50分别为476和956 nM）。此外，小檗碱和血根碱可嵌入DNA、抑制DNA合成和逆转录酶。此外，血根碱（而非小檗碱）会影响膜通透性，小檗碱会影响蛋白质生物合成。因此，这些生化活性可能介导了产生这些生物碱的植物对微生物、病毒和食草动物的化学防御。
