Potential metabolism determinants and drug–drug interactions of a natural flavanone bavachinin

Li, Xin-Qiang; Xing, Haizhou; Qin, Z. H.; Yang, Jing; Wang, Peile; Zhang, Xiaojian; Yao, Zhihong; Yao, Xin‐Sheng

doi:10.1039/d0ra06961b

Cited by 4 publications

(2 citation statements)

References 58 publications

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“…As a general assumption, drugs under in vitro screening are of potential drugability with high potency/excellent activity when the IC 50 is up to 1 μM; when the IC 50 is between 1 and 20 μM the compound is considered to have good activity alone [ 156 ]. Considering that bavachinin can only achieve PPAR-γ agonistic function, its main mechanism of action, at an EC 50 value of 0.74 μM for PPAR-γ, it is likely that this toxic side effect will occur at higher doses of bavachinin or when there is a preexisting background of liver disease or co-consumption of other molecules that affect liver function and metabolism [ 157 ]. Wang et al (2018) produced bavachinin-loaded nanoparticles by an emulsion-solvent evaporation technique.…”

Section: Controlled Flavonoid Release Systems In Asthma Treatmentmentioning

confidence: 99%

Therapeutic Potential of Controlled Delivery Systems in Asthma: Preclinical Development of Flavonoid-Based Treatments

et al. 2022

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Asthma is a chronic disease with increasing prevalence and incidence, manifested by allergic inflammatory reactions, and is life-threatening for patients with severe disease. Repetitive challenges with the allergens and limitation of treatment efficacy greatly dampens successful management of asthma. The adverse events related to several drugs currently used, such as corticosteroids and β-agonists, and the low rigorous adherence to preconized protocols likely compromises a more assertive therapy. Flavonoids represent a class of natural compounds with extraordinary antioxidant and anti-inflammatory properties, with their potential benefits already demonstrated for several diseases, including asthma. Advanced technology has been used in the pharmaceutical field to improve the efficacy and safety of drugs. Notably, there is also an increasing interest for the application of these techniques using natural products as active molecules. Flavones, flavonols, flavanones, and chalcones are examples of flavonoid compounds that were tested in controlled delivery systems for asthma treatment, and which achieved better treatment results in comparison to their free forms. This review aims to provide a comprehensive understanding of the development of novel controlled delivery systems to enhance the therapeutic potential of flavonoids as active molecules for asthma treatment.

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Section: Controlled Flavonoid Release Systems In Asthma Treatmentmentioning

confidence: 99%

Therapeutic Potential of Controlled Delivery Systems in Asthma: Preclinical Development of Flavonoid-Based Treatments

et al. 2022

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“…HDIs pose a significant public health concern due to the complex nature of medicinal herbs, often leading to severe adverse events [11]. For instance, bavachinin, a flavonoid commonly used to treat bone diseases, has demonstrated inhibitory effects on metabolic enzymes, including cytochrome P450s (CYPs) [13]. Screening for potential HDIs early in medicinal herb development is crucial to ensure safety and market entry.…”

Section: Introductionmentioning

confidence: 99%

An In Silico-Guided Approach for Assessing Herb-Drug Interaction Potential: A Case Study with Cudrania tricuspidata Leaf Extracts

Seo,

Kwak,

Cho

et al. 2024

Planta Med

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Cudrania tricuspidata leaf extracts (CLEs) have long been utilized as traditional oriental medicines across Asian countries like Korea, China, and Japan. These extracts are renowned for their therapeutic benefits in addressing inflammation, tumors, obesity, and diabetes, maintaining their status as a pivotal folk remedy. Given the rising trend of combining medicinal herbs with conventional medications, it is imperative to explore the potential herb-drug interactions (HDIs). However, there is a dearth of research on evaluating the HDIs of CLEs. Also, the intricate chemical composition of medicinal herbs presents methodological hurdles in establishing causal relationships between their constituents and HDIs. To overcome these challenges, a combined in silico and in vitro workflow was developed and effectively applied to evaluate the potential HDI of CLEs along with the associated chemical factors. In vitro CYP inhibition assays, CLEs exhibited potent inhibition of CYP1A2 and CYP2C8, with quercetin, kaempferol, and their glycosides identified as the major constituents. In silico analysis based on the prediction tools (ADMETlab2.0 and pkCSM) identified key contributors to CYP inhibition, quercetin and kaempferol. Additionally, molecular docking (MD) analysis validated the binding of ligands (quercetin and kaempferol) to proteins (CYP1A2 and CYP2C8). These findings suggest that CLEs could inhibit CYP1A2 and CYP2C8, aiding in understanding the HDI potential of CLEs for safe clinical application. Furthermore, this approach can be broadly applied to study HDIs of various medicinal herbs, enhancing their therapeutic benefits and reducing adverse reactions by considering chemical profiles relevant to HDI potential in herbal preparations.

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Multi-technology integrated network pharmacology-based study on phytochemicals, active metabolites, and molecular mechanism of Psoraleae Fructus to promote melanogenesis

Yu,

Wang,

et al. 2024

Journal of Ethnopharmacology

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Potential metabolism determinants and drug–drug interactions of a natural flavanone bavachinin

Abstract: Metabolism, efflux transport and drug–drug interactions of bavachinin.

Cited by 4 publications

References 58 publications

Therapeutic Potential of Controlled Delivery Systems in Asthma: Preclinical Development of Flavonoid-Based Treatments

Therapeutic Potential of Controlled Delivery Systems in Asthma: Preclinical Development of Flavonoid-Based Treatments

An In Silico-Guided Approach for Assessing Herb-Drug Interaction Potential: A Case Study with Cudrania tricuspidata Leaf Extracts

Multi-technology integrated network pharmacology-based study on phytochemicals, active metabolites, and molecular mechanism of Psoraleae Fructus to promote melanogenesis

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