Determination of isobavachalcone in rat plasma by LC–MS/MS and its application to a pharmacokinetic study

Ma, Tao; Nie, Li-Juan; Li, Hongmei; Huo, Qiang; Zhang, Yuxin; Wu, Cheng‐Zhu

doi:10.1016/j.jpba.2014.12.023

Cited by 12 publications

(9 citation statements)

References 17 publications

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“…be linked to suboptimal dosing as well as to its pharmacokinetics, knowing that ISO has a half-life of~6 h in rats 73 . However, we have observed as a general pattern that autophagy induction with non-toxic agents is not sufficient to inhibit tumor growth of established tumors in mice.…”

Section: Discussionmentioning

confidence: 99%

Isobacachalcone induces autophagy and improves the outcome of immunogenic chemotherapy

Tian

Durand

et al. 2020

Cell Death Dis

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A number of natural plant products have a long-standing history in both traditional and modern medical applications. Some secondary metabolites induce autophagy and mediate autophagy-dependent healthspan- and lifespan-extending effects in suitable mouse models. Here, we identified isobacachalcone (ISO) as a non-toxic inducer of autophagic flux that acts on human and mouse cells in vitro, as well as mouse organs in vivo. Mechanistically, ISO inhibits AKT as well as, downstream of AKT, the mechanistic target of rapamycin complex 1 (mTORC1), coupled to the activation of the pro-autophagic transcription factors EB (TFEB) and E3 (TFE3). Cells equipped with a constitutively active AKT mutant failed to activate autophagy. ISO also stimulated the AKT-repressible activation of all three arms of the unfolded stress response (UPR), including the PERK-dependent phosphorylation of eukaryotic initiation factor 2α (eIF2α). Knockout of TFEB and/or TFE3 blunted the UPR, while knockout of PERK or replacement of eIF2α by a non-phosphorylable mutant reduced TFEB/TFE3 activation and autophagy induced by ISO. This points to crosstalk between the UPR and autophagy. Of note, the administration of ISO to mice improved the efficacy of immunogenic anticancer chemotherapy. This effect relied on an improved T lymphocyte-dependent anticancer immune response and was lost upon constitutive AKT activation in, or deletion of the essential autophagy gene Atg5 from, the malignant cells. In conclusion, ISO is a bioavailable autophagy inducer that warrants further preclinical characterization.

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Section: Discussionmentioning

confidence: 99%

Isobacachalcone induces autophagy and improves the outcome of immunogenic chemotherapy

Tian

Durand

et al. 2020

Cell Death Dis

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“…Dimethyl sulfoxide (DMSO), 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT), z-VAD-FMK, Nec-1, CQ, and 4,6-diamidino-2-phenyl indole (DAPI) were purchased from Sigma-Aldrich (St. Louis, MO, USA). IBC was isolated from the seeds of P. corylifolia , and its purity was higher than 96.5% as indicated by HPLC analysis [ 42 ]. Bavachin, isobavachin, bavachinin, isoliquiritigenin, shikonin, and paclitaxel were purchased from Yuanye Biological Technology (Shanghai, China).…”

Section: Methodsmentioning

confidence: 99%

Isobavachalcone Induces Multiple Cell Death in Human Triple-Negative Breast Cancer MDA-MB-231 Cells

Gao

Chen

et al. 2022

Molecules

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Standardized treatment guidelines and effective drugs are not available for human triple-negative breast cancer (TNBC). Many efforts have recently been exerted to investigate the efficacy of natural compounds as anticancer agents owing to their low toxicity. However, no study has examined the effects of isobavachalcone (IBC) on the programmed cell death (PCD) of human triple-negative breast MDA-MB-231 cancer cells. In this study, IBC substantially inhibited the proliferation of MDA-MB-231 cells in concentration- and time-dependent manners. In addition, we found that IBC induced multiple cell death processes, such as apoptosis, necroptosis, and autophagy in MDA-MB-231 cells. The initial mechanism of IBC-mediated cell death in MDA-MB-231 cells involves the downregulation of Akt and p-Akt-473, an increase in the Bax/Bcl-2 ratio, and cleaved caspases-3 induced apoptosis; the upregulation of RIP3, p-RIP3 and MLKL induced necroptosis; as well as a simultaneous increase in LC3-II/I ratio induced autophagy. In addition, we observed that IBC induced mitochondrial dysfunction, thereby decreasing cellular ATP levels and increasing reactive oxygen species accumulation to induce PCD. These results suggest that IBC is a promising lead compound with anti-TNBC activity.

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“…Moreover, as a flavonoid, corylifolinin demonstrates poor intestinal permeability and reduced bioavailability (Xing et al, 2022). Research by (S. N. T. Ma et al, 2015) 2020) explored sex-related differences in the pharmacokinetics of corylifolinin in rats, uncovering variations in corylifolinin metabolism between genders, with males displaying a higher metabolic efficiency compared to females (Z. X.…”

Section: Absorption Of Corylifolininmentioning

confidence: 99%

Advances on resources, biosynthesis pathway, bioavailability, bioactivity, and application of corylifolinin

Chen,

Li,

Hussain

et al. 2024

Future Postharvest and Food

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Corylifolinin, also known as isobavachalcone, is a flavonoid compound isolated from the seeds of Psoralea corylifolia L. With a rich array of biological activities, corylifolinin has emerged as a versatile therapeutic agent. It has demonstrated notable antioxidant, anti‐inflammatory, anti‐tumor, anti‐bacterial, and anti‐viral properties. Moreover, corylifolinin holds promise in enhancing liver function, cardiovascular health, and providing neuroprotection. Its applications span a range of medical conditions, including hepatitis, cardiovascular disease, tumors, and inflammation. Herein, this comprehensive review delves into various aspects of corylifolinin, encompassing its sources, biosynthetic pathways, biotransformation, physicochemical properties, absorption, assimilation, metabolism, and excretion. It explores the molecular mechanisms underlying its diverse bioactivities in cellular and animal models. Furthermore, we present insights into clinical trials, human studies, toxicological profiles, safety considerations, marketed products, and patents related to corylifolinin. This compilation aims to serve as a valuable reference for both the development and clinical application of corylifolinin‐based therapies.

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Determination of isobavachalcone in rat plasma by LC–MS/MS and its application to a pharmacokinetic study

Cited by 12 publications

References 17 publications

Isobacachalcone induces autophagy and improves the outcome of immunogenic chemotherapy

Isobacachalcone induces autophagy and improves the outcome of immunogenic chemotherapy

Isobavachalcone Induces Multiple Cell Death in Human Triple-Negative Breast Cancer MDA-MB-231 Cells

Advances on resources, biosynthesis pathway, bioavailability, bioactivity, and application of corylifolinin

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