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Cytotoxic steroids from Monascus purpureus-fermented rice
Xiao-Ya Shang1, Jin-Jie Li, Ming-Tao Liu
1Beijing Union University, Beijing Key Laboratory of Bioactive Substances and Functional Foods, 197# Beitucheng West Road, Haidian District, Beijing 100191, PR China. shangxiaoya@ygi.edu.cn
Two novel steroids from Monascus purpureus-fermented rice exhibit potent cytotoxic activity against lung and ovarian cancer cell lines. These compounds, along with two known steroids, were isolated and characterized, demonstrating significant potential in cancer research.
Area of Science:
- Natural Products Chemistry
- Medicinal Chemistry
- Pharmacology
Background:
- Monascus purpureus-fermented rice is a source of bioactive compounds.
- Steroids are a class of molecules with diverse biological activities.
- Cancer remains a major global health challenge, necessitating the discovery of new therapeutic agents.
Purpose of the Study:
- To isolate and characterize novel steroid compounds from Monascus purpureus-fermented rice.
- To evaluate the cytotoxic and anticancer activities of the isolated compounds.
Main Methods:
- Bioassay-guided fractionation of an EtOH extract.
- Structure elucidation using HRESIMS, 1D and 2D NMR.
- Determination of absolute stereochemistry by single-crystal X-ray crystallography and Circular Dichroism (CD).
- Cytotoxicity assays against lung adenocarcinoma (A549) and human ovarian cancer (A2780) cell lines.
Main Results:
- Isolation of two new steroids (compounds 1 and 2) and two known steroids (compounds 3 and 4).
- Compound 1, a unique steroid with a conjugated triene ketone system and a fused furan ring, showed potent cytotoxicity (IC50 = 0.08 μM against A549).
- Compounds 1 and 2 also demonstrated moderate activity against A2780 cells (IC50 = 2.8 and 5.1 μM, respectively).
Conclusions:
- Monascus purpureus-fermented rice yields structurally novel steroids with significant cytotoxic potential.
- Compound 1 represents a unique steroid scaffold with promising anticancer properties.
- Further investigation into these steroids may lead to the development of new cancer therapeutics.