Affinisine

Affinisine is an indole alkaloid present in Alstonia macrophylla and Tabernaemontana catharinensis. Affinisine induces apoptosis, cell cycle arrest and reduces cell viability in melanoma cells. Affinisine can be used in studies related to cancers such as melanoma, glioma and breast cancer^[1][2][3]. In Vitro:Affinisine (compound 14) (up to 30 μg/mL; 72 h) was not evaluated in cytotoxicity or multidrug resistance reversal assays using Vincristine (HY-N0488A)-sensitive KB/S, Vincristine-resistant KB/VJ300, or Vincristine-resistant KB/VJ300 cells co-treated with 0.1 μg/mL Vincristine^[1].
Affinisine (5-100 μg/mL; 24-48 h) inhibits viability of A375, WM1366, and SK-MEL-28 human melanoma cells in a dose- and time-dependent manner, with the lowest 48 h IC₅₀ of 32.86 μg/mL in WM1366 cells, and shows selectivity over normal CCD-1059Sk skin cells^[2].
Affinisine (compound 3) (48 h) moderately inhibits the growth of U251, NCI-ADR/RES, 786-0, and HT-29 human tumor cell lines after 48 h of incubation, with GI₅₀ values ranging from 8.3 μM to 9.5 μM, and shows a selectivity index of at least 1.5 relative to non-tumor HaCat keratinocytes^[3].
Affinisine (57-65 μg/mL for A375; 32-45 μg/mL for WM1366; 46-55 μg/mL for SK-MEL-28; 48 h) induces apoptosis in A375, WM1366, and SK-MEL-28 human melanoma cells after 48 h of treatment, with the highest apoptotic rate (87.16%) observed in A375 cells treated with 65 μg/mL^[2].
Affinisine (57-65 μg/mL for A375; 32-45 μg/mL for WM1366; 46-55 μg/mL for SK-MEL-28; 48 h) induces G₂/M phase arrest in A375 human melanoma cells and G₀/G₁ phase arrest in WM1366 human melanoma cells after 48 h of treatment, but does not affect cell cycle progression in SK-MEL-28 human melanoma cells^[2].