Andrographolide inhibits the expression and metabolic activity of cytochrome P450 3A4 in the modified Caco-2 cells

Qiu, Feng; Hou, Xiao-Long; Takahashi, Kyoko; Chen, Lixia; Azuma, Jun-ichi; Kang, Ning

doi:10.1016/j.jep.2011.09.002

Cited by 17 publications

(15 citation statements)

References 36 publications

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“…These studies further confirm the inhibitory influence of BA and AD on CYP3A activity. The present investigations are in accordance with the earlier in vitro studies of BA or AD metabolic inhibition on CYP3A4 enzyme in rat and human liver microsomes (Frank and Unger, 2006;Pekthong et al, 2008;Qiu et al, 2012). The increase in hypoglycemic action by concomitant administration of glyburide with BA or AD was more in diabetic rats than when the drugs were used singly and with the control group, which suggests the enhancement of glucose reduction capacity of glyburide in diabetic rats along with BA or AD.…”

Section: Discussionsupporting

confidence: 91%

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Pharmacokinetic and Pharmacodynamic Interaction of Boswellic Acids and Andrographolide with Glyburide in Diabetic Rats: Including Its PK/PD Modeling

Samala

Veeresham

2016

Phytotherapy Research

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The effect of boswellic acids (BA) and andrographolide (AD) on the pharmacokinetics and pharmacodynamics of glyburide in normal as well as in streptozotocin-induced diabetic rats was studied. In normal and diabetic rats, the combination of glyburide with BA or AD increased significantly (p < 0.01) all the pharmacokinetic parameters, such as Cmax, AUC0-n, AUCtotal, t1/2, and mean residence time, and decreased the clearance, Vd, markedly as compared with the control group. In rat liver, microsomes BA and AD have shown CYP3A4 inhibitory activity significantly (p < 0.01), compared with the vehicle group. The increase in hypoglycemic action by concomitant administration of glyburide with BA or AD was more in diabetic rats than when the drugs were used singly and with the control group, which suggests the enhancement of glucose reduction capacity of glyburide in diabetic rats along with BA or AD. In PK/PD modeling of BA and AD with glyburide, the predicted PK and PD parameters are in line with the observed PK and PD parameters. The results revealed that BA and AD led to the PK/PD changes because of glyburide-increased bioavailability and because of the inhibition of CYP3A4 enzyme. In conclusion, add-on preparations containing BA or AD may increase the bioavailability of glyburide, and hence the dose should be monitored.

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Section: Discussionsupporting

confidence: 91%

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic and Pharmacodynamic Interaction of Boswellic Acids and Andrographolide with Glyburide in Diabetic Rats: Including Its PK/PD Modeling

Samala

Veeresham

2016

Phytotherapy Research

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“…One herb can sometimes have multiple impacts in terms of adverse reactions. As an example, oral intake of andrographolide extracted from Andrographis paniculata likely leads to reduced metabolic activity of intestinal CYP3A4 (54) and induces nephrotoxicity associated with activation of oxidative and endoplasmic reticulum stress (55).…”

Section: General Adverse Reactions To Chmmentioning

confidence: 99%

Chinese herbal medicine for acute upper respiratory tract infections and reproductive safety: A systematic review

Huang

Pan

Zhou

et al. 2019

BST

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“…Standardized extracts of A. paniculata have been in common use in Scandinavia to treat and prevent the common cold for several decades (Gabrielian et al, 2002). AG has a number of interesting biological activities, including potential interactions with the immune system (Calabrese et al, 2000) and with cytochrome P450 enzymes (Qiu et al, 2012;Chien et al, 2010;Jarukamjorn et al, 2010;Pekthong et al, 2009). Several rat male fertility studies are available on either A. paniculata or AG which give conflicting results.…”

Section: Example Risk Assessmentmentioning

confidence: 99%

Towards a non-animal risk assessment for anti-androgenic effects in humans

Dent

Carmichael

Jones

et al. 2015

Environment International

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Toxicology testing is undergoing a transformation from a system based on high-dose studies in laboratory animals to one founded primarily on in vitro methods that evaluate changes in normal cellular signalling pathways using human-relevant cells or tissues. We review the tools and approaches that could be used to develop a non-animal safety assessment for anti-androgenic effects in humans, with a focus on the molecular initiating events (MIEs) that human disorders indicate critical for normal functioning of the hypothalamus-pituitary-testicular (HPT) axis. In vitro test systems exist which can be used to characterize the effects of test chemicals on some MIEs such as androgen receptor antagonism, inhibition of steroidogenic enzymes or 5α-reductase inhibition. When used alongside information describing the pharmacokinetics of a specific chemical exposure, these could be used to inform a pathways-based safety assessment. However, some parts of the HPT axis such as events occurring in the hypothalamus or pituitary are not well represented by accepted in vitro methods. In vitro tools to characterize perturbations in these events need to be developed before a fully integrated model of the HPT axis can be described. Knowledge gaps also exist which prevent us from using in vitro data to predict the type and severity of in vivo effect(s) that could arise from a given level of in vitro anti-androgenic activity. This means that more work is needed to reliably link an MIE with an adverse outcome. However, especially for chemicals with low anti-androgenic activity, human exposure data can be used to put in vitro mode of action data into context for risk-based safety decision-making.

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Andrographolide inhibits the expression and metabolic activity of cytochrome P450 3A4 in the modified Caco-2 cells

Cited by 17 publications

References 36 publications

Pharmacokinetic and Pharmacodynamic Interaction of Boswellic Acids and Andrographolide with Glyburide in Diabetic Rats: Including Its PK/PD Modeling

Pharmacokinetic and Pharmacodynamic Interaction of Boswellic Acids and Andrographolide with Glyburide in Diabetic Rats: Including Its PK/PD Modeling

Chinese herbal medicine for acute upper respiratory tract infections and reproductive safety: A systematic review

Towards a non-animal risk assessment for anti-androgenic effects in humans

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