Indole alkaloid compounds as melanogenesis promoters and uses thereof

摘要

Provided are indole alkaloid compounds of formula I, for example, pubescine, and the use of such compounds and compositions thereof to promote (e.g., enhance) melanogenesis and pigmentation.;
Also provided are plant extracts containing a compound of formula I, for example, pubescine, and the use of such a plant extract to promote (e.g., enhance) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.

主权项

1. A method for increasing the melanin content in a mammalian subject in need thereof, comprising administering to said mammal a melanin content-increasing amount of i) an indole alkaloid compound; or ii) a plant extract containing pubescine;
wherein the indole alkaloid compound is according to formula I: wherein X is O or CR5; R1 is selected from the group consisting of hydrogen, hydroxy, substituted or unsubstituted (C1-C6) alkyl, and substituted or unsubstituted (C1-C6) alkoxy; R2 is selected from the group consisting of hydrogen, hydroxy, substituted or unsubstituted (C1-C6) alkyl, substituted or unsubstituted acyloxy, and substituted or unsubstituted (C1-C6) alkoxy; R3 is selected from the group consisting of hydrogen, hydroxy, substituted or unsubstituted (C1-C6) alkyl, substituted or unsubstituted acyloxy, substituted or unsubstituted (C1-C6) alkoxy, carboxy, substituted or unsubstituted alkoxycarbonyl, and substituted or unsubstituted amido; R4 is selected from the group consisting of hydroxy, substituted or unsubstituted (C1-C6) alkyl, substituted or unsubstituted (C1-C6) alkoxy, and halo; R5 is selected from the group consisting of hydrogen, hydroxy, substituted or unsubstituted (C1-C6) alkyl, substituted or unsubstituted acyloxy, substituted or unsubstituted (C1-C6) alkoxy; n is 0, 1, 2, 3, or 4; and the dotted bond is a single or a double bond; or pharmaceutically acceptable salts, solvates, stereo isomers, tautomers, isotopic variants or prodrugs thereof.