College of Pharmacy, Yeungnam University, Gyongsan 712-749, Korea.
Phytother Res. 2009 Nov;23(11):1531-6. doi: 10.1002/ptr.2791.
Hyperpigmentation disorders such as freckles and senile lentigines in the skin are associated with abnormal accumulation of melanin pigments. In this study, two lignan constituents were isolated from Saururus chinensis Baill (Saururaceae) as inhibitors of cellular melanin production by bioassay-guided fractionations. The active constituents were manassantin A and B that dose-dependently inhibited melanin production in alpha-melanocyte stimulating hormone (alpha-MSH)-activated melanoma B16 cells with IC(50) values of 13 nm and 8 nm, respectively. Arbutin as a positive control exhibited an IC(50) value of 96 microm on alpha-MSH-induced melanin production. Further, manassantin A inhibited forskolin- or 3-isobutyl-1-methylxanthine (IBMX)-induced melanin production with IC(50) values of 14 nm or 12 nm, respectively. Manassantin A decreased cellular amounts of IBMX-inducible tyrosinase protein but could not affect the catalytic activity of cell-free tyrosinase, a key enzyme in the biosynthetic pathway of melanin pigments. Finally, this study could provide a pharmacological potential of S. chinensis in hyperpigmentation disorders.
皮肤的色素沉着紊乱，如雀斑和老年斑，与黑色素色素的异常积累有关。在这项研究中，从三白草科 Saururus chinensis Baill（三白草科）中分离出两种木脂素成分，作为细胞黑色素生成的抑制剂，通过生物测定指导的分级分离。活性成分是马纳萨汀 A 和 B，它们分别以剂量依赖的方式抑制 α-促黑素细胞激素（α-MSH）激活的黑色素瘤 B16 细胞中的黑色素生成，IC（50）值分别为 13nm 和 8nm。熊果苷作为阳性对照，对 α-MSH 诱导的黑色素生成的 IC（50）值为 96µM。此外，马纳萨汀 A 分别以 14nm 或 12nm 的 IC（50）值抑制福司可林或 3-异丁基-1-甲基黄嘌呤（IBMX）诱导的黑色素生成。马纳萨汀 A 降低了 IBMX 诱导的酪氨酸酶蛋白的细胞含量，但不能影响细胞游离酪氨酸酶的催化活性，酪氨酸酶是黑色素生物合成途径中的关键酶。最后，本研究可为三白草在色素沉着紊乱中的药理学潜力提供依据。
