Different AhR binding sites of diterpenoid ligands from Andrographis paniculata caused differential CYP1A1 induction in primary culture in mouse hepatocytes

Chatuphonprasert, Waranya; Remsungnen, Tawun; Nemoto, Nobuo; Jarukamjorn, Kanokwan

doi:10.1016/j.tiv.2011.09.004

Cited by 6 publications

(6 citation statements)

References 52 publications

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“…This result suggests that the constituents of APE, at least the andrographolide, act as the activator of PXR and AhR. A computational docking analysis showed that andrographolide binds to AhR with the ligand posing binding energy similar to beta-naphthoflavone (−10.77 versus −9.96 kcal/mol) [51]. Moreover, coincident changes in the DNA-binding activity of AhR and PXR and the mRNA and protein levels of CYP1A1/2, CYP2C6/11, and CYP3A2 in the present study (Figures 3(a) and 3(b)) suggest that APE and andrographolide increase the activity of ethoxyresorufin O -deethylation, methoxyresorufin O -demethylation, diclofenac 4-hydroxylation, and testosterone 6 β -hydroxylation (Table 3) in rat liver at the transcriptional level.…”

Section: Discussionmentioning

confidence: 99%

Andrographis paniculataExtract and Andrographolide Modulate the Hepatic Drug Metabolism System and Plasma Tolbutamide Concentrations in Rats

Chen

Huang

Liu

et al. 2013

Evidence-Based Complementary and Alternative Medicine

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Andrographolide is the most abundant terpenoid of A. paniculata which is used in the treatment of diabetes. In this study, we investigated the effects of A. paniculata extract (APE) and andrographolide on the expression of drug-metabolizing enzymes in rat liver and determined whether modulation of these enzymes changed the pharmacokinetics of tolbutamide. Rats were intragastrically dosed with 2 g/kg/day APE or 50 mg/kg/day andrographolide for 5 days before a dose of 20 mg/kg tolbutamide was given. APE and andrographolide reduced the AUC0–12 h of tolbutamide by 37% and 18%, respectively, compared with that in controls. The protein and mRNA levels and enzyme activities of CYP2C6/11, CYP1A1/2, and CYP3A1/2 were increased by APE and andrographolide. To evaluate whether APE or andrographolide affected the hypoglycemic action of tolbutamide, high-fat diet-induced obese mice were used and treated in the same manner as the rats. APE and andrographolide increased CYP2C6/11 expression and decreased plasma tolbutamide levels. In a glucose tolerance test, however, the hypoglycemic effect of tolbutamide was not changed by APE or andrographolide. These results suggest that APE and andrographolide accelerate the metabolism rate of tolbutamide through increased expression and activity of drug-metabolizing enzymes. APE and andrographolide, however, do not impair the hypoglycemic effect of tolbutamide.

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Section: Discussionmentioning

confidence: 99%

Andrographis paniculataExtract and Andrographolide Modulate the Hepatic Drug Metabolism System and Plasma Tolbutamide Concentrations in Rats

Chen

Huang

Liu

et al. 2013

Evidence-Based Complementary and Alternative Medicine

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“…Furthermore, A. paniculata and its major compounds are able to inhibit the CYP2C isoform (CYP2C9, 2C11, 2C19), and CYP 2D6, as shown in Table 3 . On the other hand, some studies have revealed that the alcoholic extract and andrographolide can induce activities in the CYP1A1 and CYP2B isozyme, both in vitro and in vivo ([ 188 , 189 , 190 , 191 ]). In phase II drug metabolism, it was found that both the ethanolic and methanolic extracts, including andrographolide and the derivatives, showed the inhibition of UDP-glucuronyltransferases or the UGT isoforms (UGT1A3, UGT1A8, UGT2B7, UGT1A1, UGT1A6, UGT1A7, and UGT1A10) [ 192 , 193 , 194 ].…”

Section: Resultsmentioning

confidence: 99%

A Comprehensive Review of Andrographis paniculata (Burm. f.) Nees and Its Constituents as Potential Lead Compounds for COVID-19 Drug Discovery

Intharuksa

Arunotayanun²,

Yooin

et al. 2022

Molecules

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The COVID-19 pandemic has intensively disrupted global health, economics, and well-being. Andrographis paniculata (Burm. f.) Nees has been used as a complementary treatment for COVID-19 in several Asian countries. This review aimed to summarize the information available regarding A. paniculata and its constituents, to provide critical points relating to its pharmacological properties, safety, and efficacy, revealing its potential to serve as a source of lead compounds for COVID-19 drug discovery. A. paniculata and its active compounds possess favorable antiviral, anti-inflammatory, immunomodulatory, and antipyretic activities that could be beneficial for COVID-19 treatment. Interestingly, recent in silico and in vitro studies have revealed that the active ingredients in A. paniculata showed promising activities against 3CLpro and its virus-specific target protein, human hACE2 protein; they also inhibit infectious virion production. Moreover, existing publications regarding randomized controlled trials demonstrated that the use of A. paniculata alone or in combination was superior to the placebo in reducing the severity of upper respiratory tract infection (URTI) manifestations, especially as part of early treatment, without serious side effects. Taken together, its chemical and biological properties, especially its antiviral activities against SARS-CoV-2, clinical trials on URTI, and the safety of A. paniculata, as discussed in this review, support the argument that A. paniculata is a promising natural source for drug discovery regarding COVID-19 post-infectious treatment, rather than prophylaxis.

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“…A. paniculata extract ↑ mouse hepatic CYP1A1 and CYP2B [31] Andrographolide ↑ CYP1A1 and CYP1A2 mRNA expression levels [32] Andrographolide ↑ CYP1A1 and CYP1B1 mRNA expression [33] A. paniculata 60% ethanol extract or andrographolide ↓ CYP3A, CYP2C9 in vitro and CYP2C11 in vivo [34,35] Andrographolide plus 3-MC synergistically ↑ CYP1 family gene in male B6 mice [36] 14-deoxy-11,12-didehydroandrographolide and andrographolide ↓ CYP1A2, CYP2D6 and CYP3A4 expression in HepG2 cells [37] A. paniculata ethanol and methanol extracts ↓ CYP3A4, CYP2C9; andrographolide ↓ CYP3A4 [38] Andrographolide and 14-deoxy-11,12-didehydroandrographolide co-treatment with BNF ↑ CYP1A1 expression; but, neoandrographolide co-treatment with BNF ↓ CYP1A1 expression [39] Andrographolide (1, 10, 100 M) ↓ CYP3A4 mRNA and protein levels in Caco-2 cells [40] 3. Modulate GSH content…”

Section: Act As Cyps Inducersmentioning

confidence: 99%

“…Molecular docking analysis data supported that andrographolide and 14-deoxy-11,12didehydroandrographolide induced CYP1A1 expression or co-treatment with CYP1A1 inducer (-naphthoflavone, BNF) showed a synergistic increase expression of CYP1A1. In contrast, neoandrographolide suppressed BNF induced CYP1A1 expression [39]. Qiu et al study the herb-drug interactions in combination therapy.…”

Section: The Role Of a Paniculata As Cyps Inducersmentioning

confidence: 99%

Hepatoprotective Diterpenoids Isolated from Andrographis paniculata

Chao¹,

Lin²

2012

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Andrographis paniculata (Burm.f.) Nees (Acanthaceae), a plant widely used as traditional herbal medicine in many countries, has drawn attention of the researchers in recent years. Its major constituents are diterpenoids and flavonoids. This article reviews the anti-hepatotoxic effects of A. paniculata extract and derivative compounds, such as andrographolide, the major active compound, most studied for its bioactivities. Neoandrographolide shows anti-inflammatory and anti-hepatoxic properties. 14-deoxy-11,12-didehydroandrographolide and 14-deoxyabdrographolide have immunostimulatory, anti-atherosclerotic, and anti-hepatotoxic activities. The hepatoprotective activities include (1) inhibiting carbontetrachloride (CCl4), tert-butylhydroperoxide (t-BHP)-induced hepatic toxicity, (2) acting as cytochrome P450 enzymes (CYPs) inducers, (3) modulating glutathione (GSH) content, (4) influence glutathione S-transferase (GSTP) activity and phosphatidylinositol-3-kinase/Akt (PI3k/Akt) pathway, (5) synergistic effect with anti-cancer drugs induced apoptosis contributing to the bioactivities of A. paniculata extracts and isolated bioactive compounds. The articles reviewed suggest that the above compounds could be candidates for research and development as potential hepatoprotective drugs

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Different AhR binding sites of diterpenoid ligands from Andrographis paniculata caused differential CYP1A1 induction in primary culture in mouse hepatocytes

Cited by 6 publications

References 52 publications

Andrographis paniculataExtract and Andrographolide Modulate the Hepatic Drug Metabolism System and Plasma Tolbutamide Concentrations in Rats

Andrographis paniculataExtract and Andrographolide Modulate the Hepatic Drug Metabolism System and Plasma Tolbutamide Concentrations in Rats

A Comprehensive Review of Andrographis paniculata (Burm. f.) Nees and Its Constituents as Potential Lead Compounds for COVID-19 Drug Discovery

Hepatoprotective Diterpenoids Isolated from <i>Andrographis paniculata</i>

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Different AhR binding sites of diterpenoid ligands from Andrographis paniculata caused differential CYP1A1 induction in primary culture in mouse hepatocytes

Cited by 6 publications

References 52 publications

Andrographis paniculataExtract and Andrographolide Modulate the Hepatic Drug Metabolism System and Plasma Tolbutamide Concentrations in Rats

Andrographis paniculataExtract and Andrographolide Modulate the Hepatic Drug Metabolism System and Plasma Tolbutamide Concentrations in Rats

A Comprehensive Review of Andrographis paniculata (Burm. f.) Nees and Its Constituents as Potential Lead Compounds for COVID-19 Drug Discovery

Hepatoprotective Diterpenoids Isolated from &lt;i&gt;Andrographis paniculata&lt;/i&gt;

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Hepatoprotective Diterpenoids Isolated from <i>Andrographis paniculata</i>