From:  Potential of guggulsterone, a farnesoid X receptor antagonist, in the prevention and treatment of cancer

Potential of GS and its derivatives in the prevention and treatment of cancer

CancerModelCombinationMechanismReferences
Brain tumorIn vitrorBMECs-↓P-gp, ↑P-gp ATPase[134]
In vitroA172, U87MG,
T98G		SANT-1↑Caspase-3, -9, ↑cytochrome c, ↑Bax, ↑IκBα,
↓pIκKα/β, ↓NF-κB, ↓Ras, ↓p-STAT3, ↑ERK,
↓c-Myc		[140]
Breast cancerIn vitroMCF-7IR↓NF-κB, ↓ERα, ↓IGF-1Rβ, ↑p21
↑Radiosensitivity		[172]
In vitroMCF-7/DOXDOX↑Apoptosis, ↓drug-transport activity,
↓MRP1		[174]
In vitroMDA-MB-231,
MCF-7		-↑Apoptosis, ↑Caspase-3, ↓β-Catenin, ↓TCF,
↓c-Myc, ↓Cyclin D1, ↓survivin		[128]
In vitroMCF-7-↓MMP-9, ↓p65/p50, ↓IκBα, ↓IKKαβ,
↓IKK/IκB/NF-κB axisA		[117]
In vitroMCF-7-↓MMP-9, ↓AP-1, ↓MAPK, ↓ERK, ↓JNKB[117]
In vivoBALB/c miceDOX↓Tumor growth, ↓Bcl-2, ↓P-gp[138]
In vitroMDA-MB-231Bex & DOX↑Apoptosis, ↓BCRP, ↓MDR proteins[141]
CRCIn vitroHT-29-↓STAT3, ↓ARNT, ↓VEGF, ↓MMP-2, -9[110]
In vitroHT-29-↓Procaspase-9, -3, ↓Bcl-2, ↓cIAP-1
↑Fas, ↑caspase-8, ↑p-JNK, ↑p-cJun, ↑tBid		[72]
In vivonu/nu mice-↓Tumor growth[72]
In vitroHT-29IR↓IGF-1Rβ, ↓NF-κB, ↑p21, ↑γH2AX[172]
In vitroH508, SNU-C4,
HT-29		-↓FXR, ↑EGFR, ↑Src, ↑ERK-1/2[177]
In vitroHCT-116-↑p-53, ↓NF-κB, ↓Bcl-2, ↓cIAP-1, ↓survivin[126]
CCAIn vitroSk-ChA-1,
Mz-ChA-1		-↑Caspase-9, -3, -8, ↑PARP, ↓Bcl-2,
↓survivin		[111]
In vitroHuCC-T1, RBE-↑Caspase-9, -3, -8, ↑DR5, ↑tBid, ↓Bid,
↑p-JNK1/2, ↑p-p38, ↑p-ERK1/2, ↑P-eIF2α, ↑BiP, ↑GRP78, ↑CHOP		[130]
Esophageal cancerIn vitroBE-derived cells-↑Apoptosis, ↑Caspase-3[105]
In vitroBic-1-↓CDX2[113]
In vitroTE-3-↓Cell proliferation[179]
TE-12, SKGT-4,
SKGT-5		-↓FXR, ↓RAR-β2, ↓COX-2, ↓MMP-9,
↑Caspase-9, -3, -8
In vivonu/nu mice-↓Tumor growth[179]
In vitroSKGT-4, SKGT-5,
TE-3, TE-12		Amiloride↓Cell viability, ↑apoptosis[180]
In vivonu/nu nude miceAmiloride↓Tumor formation, ↓growth[180]
In vitroOE33, OE19-↓IκBα, ↓COX-2, ↓CDX-2, ↓PGE2[115]
GBCIn vitroTGBC1, TGBC2-↓NF-κB p65, ↓MMP-2, ↓VEGF-C[139]
In vitroTGBC1, TGBC2Gemcitabine↓NF-κB p65[139]
Haematological malignanciesIn vitroKBM-5-↓NF-κB, ↑Caspase, ↑PARP cleavage
↑TNF-induced apoptosis		[65]
In vitroU937-↓ΔΨm, ↓p-ERK, ↑ROS, ↑HO-1, ↓GSH[202]
In vitroU937-↓Cyclin D1, ↓cdc2, ↓Bfl-1, ↓XIAP, ↓cFLIP,
↓survivin, ↓Bcl-xL, ↓Bcl-2, ↓COX-2, ↓c-Myc,
↓IL-6, ↓IL-1β, ↓TNF,↑p21, ↑p27, ↑caspase-8, -9, -3,↑PARP, ↑BiD, ↑Bax, ↑cytochrome c, ↑JNK, ↓PI3K/Akt		[112]
In vitroU266-↓STAT3, ↓c-Src, ↓p-JAK2, ↑SHP-1,
↓Bcl-2, ↓Bcl-xL, ↓Mcl-1, ↓cyclin D1,
↑Caspase-3, ↑PARP		[109]
In vitroMM.1S-↓STAT3[109]
In vitroK562/DOX-↓P-gp, ↓MDR[135]
HCCIn vitroHep3B-↑CHOP, ↑DR5, ↑ROS, ↑BiP, ↑p-IRE1,
↑p-JNK, ↑p-PERK, ↑eIF-2α, ↑ATF4		[142]
In vitroHep3BTRAIL↓mtTMPt, ↑ Caspase-9, -3, -8, ↑PARP, ↓Bcl-2[142]
In vitroHepG2-↓Bcl-2, ↑Bax, ↓TGF-β1, ↓VEGF, ↑TNF-α[125]
In vitroHepG2R-↓COX-2, ↓P-gp[137]
In vitroPLC/PRF/5RDOX↓COX-2, ↓P-gp, ↓PGE2, ↓MDR[137]
In vitroHuH-7-↓EMT, ↓NR0B2, ↓CDH2 (N-cadherin)[106]
HNCIn vitroSCC4-↓STAT3[109]
In vitroPCI-37a,
UM-22b,
1483		-↓STAT-3, ↓HIF-1α[108]
In vivoNude mice-↑Apoptosis, ↓STAT-3[108]
In vitroSCC4-↓Cyclin-D1, ↓XIAP, ↓Mcl-1, ↓c-Myc,
↓Survivin, ↑caspase-9, -3, -8, ↑Fas/CD95, ↑Bax/Bcl2,		[133]
In vitroSCC4, HSC2-↓PI3K/Akt, ↓GSK3β, ↓PDK1, ↓p-Raf, ↓pS6,
↓p-Bax, ↓p-Bad		[66]
In vitroSCC4, HSC2-↓p-IκBα, ↓NF-κB p65, ↓COX-2, ↓IL-6,
↓p-STAT-3, ↓VEGF		[123]
Lung cancerIn vitroH1299-↓NF-κB, ↓IκBα, ↓IKK, ↓COX-2, ↓MMP-9,
↓VEGF, ↓Cyclin D1, ↓c-Myc, ↓cIAP1, ↓XIAP,
↓Bfl-1, ↓Bcl-2, ↓TRAF1, ↓cFLIP, ↓survivin		[65]
Pancreatic cancerIn vitroMIAPaCa-2,
Panc-1		Gemcitabine↓Bcl-2, ↓p-Akt, ↓NF-κB, ↑Bax, ↑p-JNK[211]
In vivoBALB/c
Nude Mice		Gemcitabine↓NF-κB, ↓Akt, ↓Bcl-2, ↑JNK[211]
In vitroCD18/HPAF,
Capan1		-↓XIAP, ↓Bcl2, ↓Cyclin D1, ↑BAD, ↑Bax,
↓MUC4, ↑Caspase-3, ↓JAK/STAT,
↓Src/FAK		[67]
In vitroMIAPaCa2,
PANC-1		-↓FXR[209]
In vitroPC-swIR↓IGF-1Rβ, ↓NF-κB[172]
In vitroPANC-1-↓Aktc[210]
PCIn vitroPC-3-↓Bcl-2, ↓Bcl-xL, ↑Bax, ↑Bak, ↑caspase-9, -3, -8[94]
In vitroPC-3, LNCaP-↑JNK1/2, ↑p38 MAPK, ↑ERK1/2[131]
In vitroDU145,
HUVEC		-↓VEGF, ↓G-CSF, ↓IL-17, ↓MMP-2,
↓p-Akt, ↓VEGF-R2,		[218]
In vivoDU145 cells
implanted
nude mice		-↓VEGF-R2, ↓factor VIII, ↓CD31[218]
Skin cancerIn vivoSENCAR mice-↓Skin edema, ↓hyperplasia, ↓ODC activity,
↓COX-2, ↓iNOS, ↓MAPKs, ↓NF-κB, ↓IKKα, ↓IκBα		[124]
In vitroB16/F10 mouse
melanoma		-↓Melanogenesis, ↓tyrosinase, ↓TRP-1
↓TRP-2, ↓MITF		[219]
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A Cis-GS; B Trans-GS; C GS derivatives, GSD1 & GSD7; AP-1: activator protein 1; Bex: Bexarotene; BiP: binding immunoglobulin protein; cIAP-1: cellular inhibitor of apoptosis protein 1; HIF-1α: hypoxia-inducible factor 1alpha; IL-6: interleukin-6; iNOS: inducible nitric oxide synthase; MM: multiple myeloma; MMP-2: matrix metalloproteinase-2; mtTMPt: mitochondrial transmembrane potential; ODC: ornithine decarboxylase; STAT-3: signal transducer and activator of transcription 3; tBid: truncated Bid