Cytotoxic Evaluation of Compounds Isolated from the Aerial Parts of Hedyotis pilulifera and Methanol Extract of Inonotus obliquus

Abstract

The aim of this study was to evaluate the inhibitory activity of compounds isolated from the aerial parts of Hedyotis pilulifera (Pit.) T.N.Ninh toward selected cancer cell lines. The isolated compounds were identified by analyzing their nuclear magnetic resonance spectral data and physical properties, and comparison of these with reported data. The sulforhodamine B assay was used for the cytotoxic evaluation of isolates. Among twenty-one compounds isolated from H. pilulifera, compounds 2, 3, and 4 showed moderate inhibitory effect on MCF-7 with IC 50 values of 63.5, 59.4, and 52.7 µg/mL, respectively, while the other compounds exhibited no effect (IC 50 values > 100 µg/mL). Further investigation using HT29, LU-1, HL-60, KB, Hep G2, and SK-Mel2 cancer cell lines showed the moderate cytotoxic activity of compound 3 (IC 50 values ranging from 51.7 to 78.3 µg/mL) to all cells, while compound 4 showed selective effect only against HL-60 cells (IC 50 61.5 µg/mL). This is the first report of cytotoxic activity of pomolic acid 3β-acetate (3) toward all tested cancer cell lines, and also the first report of cytotoxicity of rotungenic acid (4) against LU-1, HL-60, KB, Hep G2, and SK-Mel2 cancer cell lines. The methanol extract of chaga mushroom {Inonotus obliquus (Ach. ex Pers.) Pilát} exhibited the strongest cytotoxic effects against HL-60 and LU-1 (32.2 and 38.0 µg/mL, respectively), and modest cytotoxic effects against SW480 (41.3 µg/mL), HepG2 (51.3 µg/mL), KB (57.0 µg/mL), and LNCaP (57.7 µg/mL). We conclude that compounds 3 and 4 from H. pilulifera may be useful in further investigation for anticancer agent discovery and chaga could be used as a natural anticancer remedy against promyelocytic leukemia and lung adenocarcinoma.

Ursane and 24‐Noroleanane‐Type Triterpenoids with Anti‐HIV Activity from the Twigs and Leaves of Antirhea chinensis

“…Compounds 3, 5, and 11 displayed weak inhibitory effects on the growth of human breast cancer cell lines (MCF-7), human colorectal adenocarcinoma (HT-29), and/or HepG2 cells, while compounds 6 and 7 were inactive toward MCF-7 cells. [10,16,21]…”

“…Compounds 1 and 2 were also tested for cytotoxic activities against the human promyelocytic leukemia (HL‐60) and liver hepatocellular carcinoma (HepG2) cells, and neither of them was active. Compounds 3 , 5 , and 11 displayed weak inhibitory effects on the growth of human breast cancer cell lines (MCF‐7), human colorectal adenocarcinoma (HT‐29), and/or HepG2 cells, while compounds 6 and 7 were inactive toward MCF‐7 cells [10,16,21] …”

The Phytochemical Profile and Anticancer Activity of Anthemis tinctoria and Angelica sylvestris Used in Estonian Ethnomedicine

“…The same study of ethnomedicinal traditions in cancer therapy [ 2 ] also showed the use of chaga mushroom ( Inonotus obliquus ), chamomile ( Chamomilla recutita ), marigold ( Calendula officinalis ), and Scots pine ( Pinus sylvestris ), which have been previously studied in the context of possible anti-cancer effects in vitro. The methanolic chaga muchroom extract exhibited the strongest cytotoxic effects against promyelocytic leukemia cells (HL-60) and lung adenocarcinoma (LU-1, 32.2 and 38.0 μg/mL, respectively), and modest cytotoxic effects against colon adenocarcinoma (SW480), liver hepatocellular carcinoma (HepG2), oral epidermoid carcinoma (KB), and prostate cancer (LNCaP, 41.3–57.7 μg/mL) [ 24 ]. The cytotoxic activity of methanolic extract of chamomile ( Chamomilla recutita ) flowers on SK-MEL-2 (melanoma cells, IC 50 value 40.7 μg/mL) was approximately twofold higher than on KB cells (IC 50 value 71.4 μg/mL).…”

Comparative Analyses of Bioactive Compounds in Inonotus obliquus Conks Growing on Alnus and Betula

“…In Estonian ethnomedicine, the conks of I. obliquus have been a popular folk anti-cancer remedy [ 19 ]. As was shown in the in vitro studies, the methanol extract of I. obliquus conks growing in Estonia exhibited the strongest cytotoxic effects against promyelocytic leukaemia and lung adenocarcinoma cells (the IC 50 values were 32.2 and 38.0 μg/mL, respectively), and modest cytotoxic effects (41.3–57.7 μg/mL) against the cells of colon adenocarcinoma, liver hepatocellular carcinoma, oral epidermoid carcinoma, and prostate cancer cells [ 16 ].…”

“…The triterpene and steroid compounds of these conks have demonstrated hepatoprotective, hypoglycemic, antifungal, antioxidant, and anti-inflammatory properties; in addition, they can regulate cholesterol biosynthesis [ 12 ]. In summary, I. obliquus is characterized as a promising natural material of biologically active substances against cancer and for immunotherapy [ 9 , 12 , 13 , 14 , 15 , 16 , 17 , 18 ].…”