Drug intelligence / Profile preview

α-hederin

Development stage
Preclinical
Modality
Small Molecules
01

Overview

α-Hederin is a naturally occurring pentacyclic triterpenoid saponin compound with the molecular formula C41H66O12 and a molar mass of 750.96 g/mol[6][8][10]. It is found in various plant sources including the seeds of Nigella sativa and leaves of Hedera helix (common ivy)[10]. α-Hederin exhibits significant pharmacological activities such as antitumor (anticancer), anti-inflammatory, spasmolytic (muscle relaxant), and anti-infective effects[1][2][3][4]. Its principal mechanism involves inhibiting tumor cell proliferation by inducing apoptosis (programmed cell death), arresting the cell cycle process in cancer cells[1], modulating multiple signaling pathways including JAK/STAT and PI3K/Akt/mTOR[3], affecting lipid metabolism and TGFβ pathways via regulation of vesicular miRNAs[5], and blocking small extracellular vesicle-mediated drug resistance transmission in cancer therapy. Preclinical studies have shown that α-hederin can enhance the efficacy of chemotherapeutic agents such as paclitaxel or 5-fluorouracil by sensitizing tumor cells to these drugs[4][5][10]. It has been studied for its potential use against breast cancer, lung cancer (including non-small cell lung cancer), colorectal cancer, liver cancer as well as for its general anti-infective properties.

Other names
alpha-hederinhelixinhederoside Ckoronaroside Anepalin2nepalin-2nepalin 2taurosideehederosidecTXB-Hederinalpha-hedersapindosideaakebosidestc
02

Targets

GPX4 (Glutathione peroxidase 4)CholesterolRhodopsin-like G protein-coupled receptor

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