Anticancer effect and structure-activity analysis of marine products isolated from metabolites of mangrove fungi in the South China Sea.
Marine-derived fungi provide plenty of structurally unique and biologically active secondary metabolites. We screened 87 marine products from mangrove fungi in the South China Sea for anticancer activity by MTT assay. 14% of the compounds (11/86) exhibited a potent activity against cancer in vitro. Importantly, some compounds such as compounds 78 and 81 appeared to be promising for treating cancer patients with multidrug resistance, which should encourage more efforts to isolate promising candidates for further development as clinically useful chemotherapeutic drugs. Furthermore, DNA intercalation was not involved in their anticancer activities, as determined by DNA binding assay. On the other hand, the structure-activity analysis indicated that the hydroxyl group was important for their cytotoxic activity and that bulky functional groups such as phenyl rings could result in a loss of biological activity, which will direct the further development of marine product-based derivatives.
Tao
Li-yang
LY
State Key Laboratory for Oncology in South China, Cancer Center, Sun Yat-Sen University, Guangzhou, 510060, China. sohutly@163.com
Zhang
Jian-ye
JY
Liang
Yong-ju
YJ
Chen
Li-ming
LM
Zhen
Li-sheng
LS
Wang
Fang
F
Mi
Yan-jun
YJ
She
Zhi-gang
ZG
To
Kenneth Kin Wah
KK
Lin
Yong-cheng
YC
Fu
Li-wu
LW
D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002681:China; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D005658:Fungi / Q000302:isolation & purification / Q000378:metabolism*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D043982:Rhizophoraceae / Q000382:microbiology*; D012623:Seawater; D013329:Structure-Activity Relationship; D013778:Tetrazolium Salts; D013844:Thiazoles
D000970:Antineoplastic Agents; D013778:Tetrazolium Salts; D013844:Thiazoles; C022616:thiazolyl blue