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Table 1 Anticancer activity of GS in in vitro experimental model and underlying molecular targets

From: Potential therapeutic targets of Guggulsterone in cancer

Cancer Type Model/System Molecular Targets References
Pancreatic cancer Human pancreatic cancer cell lines ↓FXR reduced ↓ NF-κB, ↓Cyclin D1, ↓Bcl-2, ↓XIAP↓MPP9, ↓STAT3, ↓FAK, ↓Src, p-AKT,c-June, ↑Caspase-3,↑Bax [33, 38, 39]
Head and Neck cancer Head and neck carcinoma cell line ↓ PI3-kinase/AKT, ↑Bax, ↑Bad [88]
Esophagael cancer Esophageal adenocarcinoma cell lines ↓caudal type homeobox 2,↓Cox2,↓NFkB, ↓FXR, ↓ RAR-β2, ↑caspase-8,caspase-9,caspase-3 [47, 48]
Colon cancer Colon cancer cell line ↓cIAP-1, ↓cIAP-2, ↓Bcl-2, ↓STAT3, ↓VEGF, ↑truncated Bid, ↑Fas, ↑p-JNK, ↑p-c-Jun [50, 51]
Breast cancer Breast cancer cell lines ↓cyclin D1, ↓C-myc, ↓survivin, ↓TCF-4, ↓IKK/NF-κB, ↓MAPK/AP-1, ↓MMP-9 ↓ [34, 89]
Prostate cancer Prostate cancer cell lines ↑caspase-9, ↑caspase-8, ↑caspase-3, ↑Bax
Bcl-2 and Bcl-xL
Hepatocellular carcinoma Hepatocellular carcinoma cell lines TGF-β1, VEGF, Bcl-2,↑Bax,
[83, 85]
Hematological malignancies Leukemic cell lines ↓Bfl-1/A1, ↓XIAP, ↓cFLIP, ↓Bcl-2, ↓BclXL, ↓survivin
↑caspase 8, ↑bid cleavage, ↑cytochrome c release, ↑caspase 9, ↑ caspase 3, ↑ PARP cleavage.