Cytotoxic triterpenes from Antrodia camphorata and their mode of action in HT-29 human colon cancer cells

Abstract

Five lanostane (2, 3, 4, 6 and 8) and three ergostane-type (1, 5 and 7) triterpenes isolated from the fruiting bodies of Antrodia camphorata were evaluated for their in vitro cytotoxic data against various cancer cell types. The three zhankuic acids, 1, 5 and 7 displayed the most potent cytotoxic effect with an IC 50 value of 22.3-75.0 lM. The compound 3 was selectively cytotoxic in three colon cancer cell lines (HT-29, HCT-116 and SW-480) and a breast cancer model (MDA-MB-231), whereas 8 only showed its cytotoxicity against MDA-MB-231. None of these isolates was toxic to mammary epithelial (MCF10A) and primary foreskin fibroblast (HS68) cells, two human normal cell lines. The compounds 1, 5 and 7 were also demonstrated to induce apoptosis in HT-29 and SW-480 cells, as confirmed by sub-G1 cell cycle arrest. In HT-29 cells, the expression of apoptosis-associated proteins poly-(ADP-ribose) polymerase cleavage, Bcl-2 and procaspase-3 were suppressed by compounds 1, 5 and 7. A mixture containing 4 lM each of compounds 1, 5 and 7 also showed a synergistic cytotoxic effect in HT-29 cells.

Anticancer Effects of Taiwanofungus camphoratus Extracts, Isolated Compounds and its Combinational use

“…Supernatants were collected after 21 Induce apoptosis, 21 suppress the expression of apoptosisassociated proteins 43 Human leukemia HL 60 cells 21 21,25,43 1.8 25 Murine lymphocytic leukemia P-388 cells 25 22 centrifugation, and the same buffer was added to the precipitate for another 24 hours at 60 C. The supernatants of the two extractions were collected, and a 3.75-fold volume of 95% ethanol was added, precipitated at 4 C overnight, then spun, and the pellets were collected. The pellets were dried and resuspended in distilled water, dialyzed (molecular weight: 12,000e14,000 Da) against distilled water overnight at 4 C, and centrifuged to collect the supernatant as sulfated polysaccharides.…”

Multiple Molecular Targets of Antrodia camphorata: A Suitable Candidate for Breast Cancer Chemoprevention

“…Zhankuic acid and suphurenic acid showed significant cytotoxic effect to the human breast cancer cells MDA-MB-231 and MCF-7 with an IC 50 value of 25.1 and 89.2; and 57.8 and 357.0 µM, respectively. Indeed, sulphurenic acid is selectively cytotoxic to estrogennonresponsive MDA-MB-231 cells, and the only one compound that does not contain the diene structure with in the rings at position 7 and 9 and instead possesses a single double bond in the rings at the position 8 (Yeh et al, 2009). This result also provides another hallmark that cytotoxic effect of bioactive compounds also depends on structural activity relationship.…”

Effect of Chinese Herb Extract on the Formation of Triterpenoids in Shake-Flask Cultures of Antrodia cinnamomea

“…Various types of bioactive compounds from the fruiting bodies of A. cinnamomea have been identified, including triterpenoids, polysaccharide, steroids and sesquiterpene lactone [1,[3][4][5]. Apart from polysaccharide, triterpenoids were well recognized as potential anticancer agents due to their activity against growing tumors in the fruiting bodies of A. cinnamomea [1,3,[5][6][7][8]. Cultivated mycelium has been reported to exhibit similar anticancer effects with wild fruiting bodies [9][10][11][12][13].…”