Drug intelligence / Profile preview

actein

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Actein is a natural triterpenoid glycoside, specifically a 9,19-cyclobutane triterpenoid, isolated from *Cimicifuga spp.* (e.g., *Cimicifuga foetida*, *Actaea racemosa L.*, also known as black cohosh). It has demonstrated diverse pharmacological activities, including anti-cancer effects against various malignancies such as breast cancer, oral squamous cell carcinoma, colorectal cancer, non-small cell lung cancer, multiple myeloma, and bladder cancer. Its anti-cancer mechanisms involve inhibiting cell proliferation, inducing apoptosis, and modulating key signaling pathways like PI3K/Akt/mTOR, Ras/Raf/MAPK, and FoxO1. Beyond oncology, actein shows promise in metabolic disorders, ameliorating atherosclerosis by upregulating ABCG1 and LXR, and combating obesity through AMPK activation and white fat browning. It has also been investigated for its potential in treating COPD and osteoporosis by influencing bone and cartilage metabolism.

02

Targets

CASP3 (Caspase-3)CASP8 (Caspase-8)CASP9 (Caspase-9)CDK2 (Cyclin-dependent kinase 2)ABCG1 (ATP-binding cassette sub-family G member 1)AMPK (Adenosine monophosphate–activated protein kinase)BAX (Apoptosis regulator BAX)CDK (CDK family)EGFR (Epidermal growth factor receptor)FOXO1 (Forkhead box protein O1)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)ISG15 (Interferon-stimulated gene 15 protein)NeuraminidaseJNK (Mitogen-activated protein kinase kinase kinase family)NR1H3 (Liver X receptor beta)MMP12 (Macrophage Metalloelastase)NF-κBPARP (PARP family)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)MAPK3 (Mitogen-activated protein kinase 1)TAGLN2 (Transgelin-2)mTOR (Mammalian target of rapamycin kinase)

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