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Calotropis gigantea stem bark extract
- Development stage
- Preclinical
- Lead developer
- Naresuan University
- Modality
- Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intraperitoneal
01
Overview
Calotropis gigantea stem bark extract is a botanical extract derived from the stem bark of the Calotropis gigantea plant, commonly known as giant calotrope. It is being investigated for its potential anti-cancer, anti-angiogenic, and gut microbiota-modulating properties. Research, primarily conducted by Naresuan University and Thammasat University in Thailand, has demonstrated that the extract (particularly its dichloromethane fraction, CGDCM) induces apoptosis in various cancer cell lines, including hepatocellular carcinoma (HepG2) and colorectal cancer (HCT116, HT-29), through mechanisms involving reactive oxygen species (ROS) generation, mitochondrial membrane potential reduction, and ATP synthesis inhibition. In vivo studies in HepG2-xenograft mouse models have shown that the extract suppresses tumor growth, inhibits tumor angiogenesis (by downregulating HIF-1α, VEGF, VEGFR-2, and other angiogenic factors), and selectively reprograms the gut microbiota to restore liver-gut microbial balance.
- Other names
- C. gigantea stem bark extractCalotropis gigantea (L.) Dryand. stem bark extract
02
Targets
EGFR (Epidermal growth factor receptor)HIF1A (Hypoxia-inducible factor 1-alpha)ATP1A (Sodium/potassium-transporting ATPase)VEGFA (Vascular endothelial growth factor A)VEGFR2 (Vascular endothelial growth factor receptor 2)
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