หัวเรื่อง:ไม่มีชื่อไทย (ชื่ออังกฤษ : Synthesis and Cytotoxicity Studies of Polyhydroxysterols and Their Sulfate Analogs)
ผู้เขียน:
Potjamarn Bunyathaworn, 
ดร.บุญส่ง คงคาทิพย์, ศาสตราจารย์เกียรติคุณ
, ดร.งามผ่อง คงคาทิพย์, ศาสตราจารย์เกียรติคุณ
สื่อสิ่งพิมพ์:pdf
Abstract
The six new polyhydroxy steroids, 3?, 20(S)-dihydroxy-5?-cholest-24-ene (19), 3?, 20(S)- dihydroxy-5?-cholestane (20), 3?, 20(S), 24-trihydroxy-5?-cholestane (23), 2?, 3?, 20(S)-trihydroxy- 5?-cholestane (29), 2?, 3?, 20(S)-trihydroxy-5?-cholest-24-ene (31), 2?, 3?, 20(S), 24-tetrahydroxycholestane (37) and the sulfate derivative 21 were synthesized from tigogenin. Antitumor activity against two tumor cell lines (lung cancer NCI-H187 and oral cancer KB) was evaluated. Compound 23 containing trihydroxy groups at the C-3, C-20 and C-24 positions showed strong activity against both NCI-H187 and KB cells (IC50 2.11 and 5.39 ?g/mL). The 3, 20-dihydroxy steroid 19 showed strong activity against NCI-H187 (IC50 4.24 ?g/mL) but was weakly active against KB (IC50 39.12 ?g/mL) whereas the analog 20 which has a saturated side chain showed moderate activity against KB (IC50 20.51 ?g/mL) and was inactive against the NCI-H187 cell line. Surprisingly, the sulfate derivative of 20, compound 21, was inactive to both tested cells. Compounds 29 and 31, having vicinal dihydroxy groups in ring A at C-2, C- 3 as well as a hydroxyl group at the C-20 position, showed similar activity against NCI-H187 (IC50 9.08 and 9.59 ?g/mL) but for the KB cell, only 31 showed strong activity (IC50 10.14 ?g/mL) whereas 29 was inactive. The analogue compound 37, which has an extra hydroxyl group at C-24, was inactive against both tested cell lines.