Effect of Tinospora cordifolia aqua-alcoholic extract on pharmacokinetic of Glibenclamide in rat: An herb-drug interaction study

Sahu, Rajanikanta; Ahmed, Tausif; Sangana, Ramchandra R.; Punde, Ravindra; Subudhi, Bharat Bhusan

doi:10.1016/j.jpba.2018.01.010

Cited by 19 publications

(10 citation statements)

References 16 publications

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“…Because phytocompounds of extracts often have holistic properties, the contribution from other components cannot be ruled out. These data partly explain the potential of TCE to inhibit the metabolic activity of CYP2D6 and CYP3A4 …”

Section: Resultsmentioning

confidence: 72%

Tinospora cordifolia Extract Enhances Dextromethorphan Bioavailability: Implications for Alzheimer’s Disease

Majhi,

Sayyad,

Gaur

et al. 2024

ACS Omega

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Tinospora cordifolia (Willd.) Miers (Menispermaceae) is a traditional rejuvenator and a conventional medicine used to manage oxidative stress-related diseases, including those associated with the central nervous system. Decreased dextromethorphan (DEM) metabolism is necessary for high bioavailability and application against Alzheimer’s disease (AD). Since T. cordifolia stem extract (TCE) can potentially inhibit several metabolic enzymes, it can also enhance dextromethorphan bioavailability. This study investigates the potential of TCE to improve DEM’s bioavailability and efficacy for the management of AD. In silico analysis was carried out to find the inhibition potential of phytocomponents of T. cordifolia for CYP2D6 and CYP3A4. The LC-MS method was revalidated for the analysis of DEM and metabolite dextrorphan (DEX) in the presence of quinidine (QN). The ratio of DEM to DEX was estimated with varying doses of TCE following pharmacokinetic analysis. Network pharmacology analysis was carried out to understand the complementary potential of phytocomponents. This was further validated in the scopolamine-induced dementia model through behavioral and histopathological analyses. TCE (100 mg/kg) for 14 days increased the DEM to DEX ratio by 2.8-fold compared to QN treatment. While T max was comparable to that of QN treatment at this dose (100 mg/kg) of TCE, it increased significantly at the higher dose (400 mg/kg) of TCE pretreatment. All other pharmacokinetic parameters were also enhanced at this dose with a 4.7-fold increase in DEM/DEX compared with QN. Network pharmacology analysis indicated the ability of TCE to target multiple factors associated with AD. Furthermore, it improved spatial memory and reduced hyperactivity in rodents better than the combination of QN and DEM.

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Section: Resultsmentioning

confidence: 72%

Tinospora cordifolia Extract Enhances Dextromethorphan Bioavailability: Implications for Alzheimer’s Disease

Majhi,

Sayyad,

Gaur

et al. 2024

ACS Omega

Self Cite

View full text Add to dashboard Cite

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“…Pre-treatment with a low dose of Andrographis paniculata extract increases theophylline elimination due to the induction of CYP1A2, whereas a high dose of A. paniculata decreases theophylline elimination due to the inhibition of CYP1A2, respectively [72]. In the case of co-administration of Tinospora cordifolia aqueous-alcoholic extract and glibenclamide, only high doses (400 mg/kg) T. cordifolia aqueous alcoholic extract, not low doses (100 mg/kg), increased the oral bioavailability of glibenclamide due to the reduced clearance via CYP 2C9, 2D6 and 3A4 in rats [73].…”

Section: Multifaceted Factors In Study Designs (Eg Administration mentioning

confidence: 99%

Multifaceted Factors Causing Conflicting Outcomes in Herb-Drug Interactions

Choi

Chin

2020

Pharmaceutics

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Metabolic enzyme and/or transporter-mediated pharmacokinetic (PK) changes in a drug caused by concomitant herbal products have been a primary issue of herb and drug interactions (HDIs), because PK changes of a drug may result in the alternation of efficacy and toxicity. Studies on HDIs have been carried out by predictive in vitro and in vivo preclinical studies, and clinical trials. Nevertheless, the discrepancies between predictive data and the clinical significance on HDIs still exist, and different reports of HDIs add to rather than clarify the confusion regarding the use of herbal products and drug combinations. Here, we briefly review the underlying mechanisms causing PK-based HDIs, and more importantly summarize challenging issues, such as dose and treatment period effects, to be considered in study designs and interpretations of HDI evaluations.

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“…This pharmacokinetic study results are also backed by the CYP inhibition and metabolism study where the extract has been reported to inhibit CYP2C9 activity (IC 50 < 0.1 mg/ml), however the extract also inhibited CYP2C19, 2D6 and 1A2 enzymes (IC 50 < 1 mg/ml). The study proposed that the bioavailability of glibenclamide, being a CYP2C9 substrate could be high in clinical conditions when concomitantly administered with Tinospora cordifolia extract for an extended period (Sahu et al, ). A two‐phase randomized crossover clinical study in healthy male subjects was performed to deteremine CYP inhibition potential of berberine in humans.…”

Section: Herbs With An Established Potential For Hdi With Drugs Of Otmentioning

confidence: 99%

Herb–drug interaction studies of herbs used in treatment of cardiovascular disorders—A narrative review of preclinical and clinical studies

Shaikh

Thomas

Chitlange

2020

Phytotherapy Research

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About 70% of the world population is currently using medicinal herbs as complementary or alternative medicine, which is increasing at a tremendous pace in both developed and developing countries in the last two decades (World Health Organization Medicines Strategy 2002–2005). This increase in consumer demand of medicinal herbs continues despite the rarity of scientific data to establish their safety and efficacy profile. Its popularity is also attributed to several factors, including easy availability, cost effectiveness leading to better purchasing power and general perception that they are safe. Herbs are often administered concomitantly with therapeutic drugs for the treatment of major ailments, raising the potential for herb–drug interactions (HDIs). The major pathways postulated for HDIs involves the cytochrome P450 (CYP450)‐mediated inhibition or induction and transport and efflux proteins. In our review, we highlight frequently used herbal medicines for the treatment of cardiovascular disorders (CVD), their established HDIs studied using in vitro tools and in vivo pharmacokinetic and pharmacodynamic assays and case reports. Herbs have been divided into different sections on the basis of availability of HDI data in relevance to cardiovascular drugs: herbs reported to interact with cardiac drugs, herbs yet to be reported for interaction with drugs of any class and herbs reported to interact with drugs of other therapeutic category but not with cardiac drugs. The amount of active phytoconstituents present in the selected herbs and their extent of bioavailability are also mentioned. This review can serve as a quick reference database for physicians and health care professionals involved in CVD treatment, aimed at maximizing clinical outcomes with reduction in adverse and toxic effects.

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Effect of Tinospora cordifolia aqua-alcoholic extract on pharmacokinetic of Glibenclamide in rat: An herb-drug interaction study

Cited by 19 publications

References 16 publications

Tinospora cordifolia Extract Enhances Dextromethorphan Bioavailability: Implications for Alzheimer’s Disease

Tinospora cordifolia Extract Enhances Dextromethorphan Bioavailability: Implications for Alzheimer’s Disease

Multifaceted Factors Causing Conflicting Outcomes in Herb-Drug Interactions

Herb–drug interaction studies of herbs used in treatment of cardiovascular disorders—A narrative review of preclinical and clinical studies

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