Effect of Gambogenic Acid on Cytochrome P450 1A2, 2B1 and 2E1, and Constitutive Androstane Receptor in Rats

Sun, Jing; Tang, Xiaozhu; Xu, Qianqian; Tao, Ge; Peng, Daiyin; Chen, Weidong

doi:10.1007/s13318-018-0477-7

Cited by 6 publications

(3 citation statements)

References 43 publications

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“…The cytochrome P450 (CYP450) superfamily is usually considered the most important phase I drug-metabolizing enzyme system. GNA increased the activity of liver CY-P1A2, CYP2E1, CYP2C, and CYP3A [86,87]. Therefore, when GNA is administered with other drugs, potential drug-drug interactions mediated by CYP1A2, CYP2E1, CYP2C, and CYP3A induction should be taken into consideration.…”

Section: Pharmacokinetic Study Of Gambogenic Acidmentioning

confidence: 99%

Unveiling Gambogenic Acid as a Promising Antitumor Compound: A Review

Mi,

Xing,

Zhang

et al. 2024

Planta Med

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Gambogenic acid is a derivative of gambogic acid, a polyprenylated xanthone isolated from Garcinia hanburyi. Compared with the more widely studied gambogic acid, gambogenic acid has demonstrated advantages such as a more potent antitumor effect and less systemic toxicity than gambogic acid according to early investigations. Therefore, the present review summarizes the effectiveness and mechanisms of gambogenic acid in different cancers and highlights the mechanisms of action. In addition, drug delivery systems to improve the bioavailability of gambogenic acid and its pharmacokinetic profile are included. Gambogenic acid has been applied to treat a wide range of cancers, such as lung, liver, colorectal, breast, gastric, bladder, and prostate cancers. Gambogenic acid exerts its antitumor effects as a novel class of enhancer of zeste homolog 2 inhibitors. It prevents cancer cell proliferation by inducing apoptosis, ferroptosis, and necroptosis and controlling the cell cycle as well as autophagy. Gambogenic acid also hinders tumor cell invasion and metastasis by downregulating metastasis-related proteins. Moreover, gambogenic acid increases the sensitivity of cancer cells to chemotherapy and has shown effects on multidrug resistance in malignancy. This review adds insights for the prevention and treatment of cancers using gambogenic acid.

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Section: Pharmacokinetic Study Of Gambogenic Acidmentioning

confidence: 99%

Unveiling Gambogenic Acid as a Promising Antitumor Compound: A Review

Mi,

Xing,

Zhang

et al. 2024

Planta Med

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show abstract

“…In this study, based on our previous research, a simplified cocktail approach was successfully applied to evaluate the effect of GNA on CYP2C and CYP3A in rats 21) . The LC-MS/MS method was validated by assessments of selectivity, accuracy, precision, matrix effect, recovery, and the stability profiles of the probe drugs.…”

Section: Effect Of Gna On Cyp Isoform Substratesmentioning

confidence: 99%

“…At present, limited information about GNA is available on CYP-mediated metabolism. We had studied the effect of GNA on CYP1A2, 2B1 and 2E1 in rats 21) . The 14-day administration of GNA significantly increased the mRNA and protein expression levels as well as the activity of CYP2E1.…”

Section: Chemical and Pharmaceutical Bulletin Advance Publicationmentioning

confidence: 99%

Anti-tumor Effect of Gambogenic Acid and Its Effect on CYP2C and CYP3A after Oral Administration

Sun

Pang

Tang

et al. 2023

CHEMICAL & PHARMACEUTICAL BULLETIN

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Gambogenic acid (GNA), which has a broad spectrum of anti-tumor activity, is considered as a potential anticancer ingredient. In this study, we examined the antitumor effect and the effect of GNA on cytochrome P450 and pregnane X receptor (PXR).In anti-tumor experiments, an A549 cells tumor-bearing nude mice model was established. Tumor weights and volumes were measured. Inhibition ratio (IR) was calculated. In a pharmacokinetic study, after intragastrical administration of GNA in rats, a cocktail method was adopted to evaluate the activities of CYP2C6, 2C11 and 3A1; RT-qPCR and WB assays were applied to evaluate the mRNA and protein expression levels, respectively. Compared with injection, oral administration also can inhibit tumor growth. Moreover, GNA increased the activities of CYP2C11 and CYP3A1 in the high-dose group as well as the mRNA and protein expression levels.The mRNA and protein expression levels of PXR were also slightly induced. Our study suggested that, oral administration of GNA was effective in inhibiting tumor growth in mice and could induced the activities of CYP2C and CYP3A in rats.

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Effect of gambogenic acid in attenuating diethylnitrosamine (DEN)-induced hepatocellular carcinoma in rat model

Zhang¹,

Yang

et al. 2023

Arabian Journal of Chemistry

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Effect of Gambogenic Acid on Cytochrome P450 1A2, 2B1 and 2E1, and Constitutive Androstane Receptor in Rats

Abstract: The obtained results suggest that the CYP1A2 and CYP2E1 enzymes could be induced in rats after treatment with GNA. Therefore, when GNA is administrated with other drugs, potential drug-drug interactions (DDI) mediated by CYP1A2 and CYP2E1 induction should be taken into consideration.

Cited by 6 publications

References 43 publications

Unveiling Gambogenic Acid as a Promising Antitumor Compound: A Review

Unveiling Gambogenic Acid as a Promising Antitumor Compound: A Review

Anti-tumor Effect of Gambogenic Acid and Its Effect on CYP2C and CYP3A after Oral Administration

Effect of gambogenic acid in attenuating diethylnitrosamine (DEN)-induced hepatocellular carcinoma in rat model

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