TY - JOUR
T1 - Cytotoxic constituents from Brazilian red propolis and their structure-activity relationship
AU - Li, Feng
AU - Awale, Suresh
AU - Tezuka, Yasuhiro
AU - Kadota, Shigetoshi
PY - 2008/5/15
Y1 - 2008/5/15
N2 - Several classes of flavonoids [flavanoids (1-10), flavonol (11), isoflavones (12-18), isoflavanones (19-22), isoflavans (23-26), chalcones (27-30), auronol (31), pterocarpans (32-37), 2-arylbenzofuran (38), and neoflavonoid (39)] and lignans (40-42) isolated from the MeOH extract of Brazilian red propolis were investigated for their cytotoxic activity against a panel of six different cancer cell lines including murine colon 26-L5 carcinoma, murine B16-BL6 melanoma, murine Lewis lung carcinoma, human lung A549 adenocarcinoma, human cervix HeLa adenocarcinoma, and human HT-1080 fibrosarcoma cell lines. Based on the observed results, structure-activity relationships were discussed. Among the tested compounds, 7-hydroxy-6-methoxyflavanone (3) exhibited the most potent activity against B16-BL6 (IC50, 6.66 μM), LLC (IC50, 9.29 μM), A549 (IC50, 8.63 μM), and HT-1080 (IC50, 7.94 μM) cancer cell lines, and mucronulatol (26) against LLC (IC50, 8.38 μM) and A549 (IC50, 9.9 μM) cancer cell lines. These activity data were comparable to those of the clinically used anticancer drugs, 5-fluorouracil and doxorubicin, against the tested cell lines, suggesting that 3 and 26 are the good candidates for future anticancer drug development.
AB - Several classes of flavonoids [flavanoids (1-10), flavonol (11), isoflavones (12-18), isoflavanones (19-22), isoflavans (23-26), chalcones (27-30), auronol (31), pterocarpans (32-37), 2-arylbenzofuran (38), and neoflavonoid (39)] and lignans (40-42) isolated from the MeOH extract of Brazilian red propolis were investigated for their cytotoxic activity against a panel of six different cancer cell lines including murine colon 26-L5 carcinoma, murine B16-BL6 melanoma, murine Lewis lung carcinoma, human lung A549 adenocarcinoma, human cervix HeLa adenocarcinoma, and human HT-1080 fibrosarcoma cell lines. Based on the observed results, structure-activity relationships were discussed. Among the tested compounds, 7-hydroxy-6-methoxyflavanone (3) exhibited the most potent activity against B16-BL6 (IC50, 6.66 μM), LLC (IC50, 9.29 μM), A549 (IC50, 8.63 μM), and HT-1080 (IC50, 7.94 μM) cancer cell lines, and mucronulatol (26) against LLC (IC50, 8.38 μM) and A549 (IC50, 9.9 μM) cancer cell lines. These activity data were comparable to those of the clinically used anticancer drugs, 5-fluorouracil and doxorubicin, against the tested cell lines, suggesting that 3 and 26 are the good candidates for future anticancer drug development.
KW - Brazilian red propolis
KW - Cytotoxic activity
KW - Flavonoids
KW - Structure-activity relationship
UR - http://www.scopus.com/inward/record.url?scp=43749087342&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2008.04.016
DO - 10.1016/j.bmc.2008.04.016
M3 - 学術論文
C2 - 18440233
AN - SCOPUS:43749087342
SN - 0968-0896
VL - 16
SP - 5434
EP - 5440
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 10
ER -
