Role of natural P-gp inhibitor in the effective delivery for chemotherapeutic agents

Shah, Disha; AJAZUDDIN, .; Bhattacharya, Sankha

doi:10.1007/s00432-022-04387-2

Cited by 21 publications

(9 citation statements)

References 92 publications

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“…AS-IV can increase the sensitivity of tumor chemotherapeutic drugs. Several researchs demonstrated that chemotherapy resistance is mainly mediated by P-glycoprotein (P-gp) (Jiang et al, 2021;Shah et al, 2023). Inhibition of P-gp transporters and regulation of multidrug resistance (MDR) are important strategies for reversing MDR (Pilotto Heming et al, 2022).…”

Section: Enhancement Of Chemosensitivitymentioning

confidence: 99%

Astragaloside IV, as a potential anticancer agent

Xia

Li²,

Tang

et al. 2023

Front. Pharmacol.

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Cancer is a global intractable disease, and its morbidity and mortality are increasing year by year in developing countries. Surgery and chemotherapy are often used to treat cancer, but they result in unsatisfactory outcomes, such as severe side effects and drug resistance. With the accelerated modernization of traditional Chinese medicine (TCM), an increasing body of evidence has shown that several TCM components have significant anticancer activities. Astragaloside IV (AS-IV) is considered the main active ingredient of the dried root of Astragalus membranaceus. AS-IV exhibits various pharmacological effects, such as anti-inflammatory, hypoglycemic, antifibrotic, and anticancer activities. AS-IV possesses a wide range of activities, such as the modulation of reactive oxygen species-scavenging enzyme activities, participation in cell cycle arrest, induction of apoptosis and autophagy, and suppression of cancer cell proliferation, invasiveness, and metastasis. These effects are involved in the inhibition of different malignant tumors, such as lung, liver, breast, and gastric cancers. This article reviews the bioavailability, anticancer activity, and mechanism of AS-IV and provides suggestions for further research of this TCM.

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Section: Enhancement Of Chemosensitivitymentioning

confidence: 99%

Astragaloside IV, as a potential anticancer agent

Xia

Li²,

Tang

et al. 2023

Front. Pharmacol.

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“…The natural molecules most recently identified as potential inhibitors of P-gp are part of the fourth generation of inhibitors. These compounds such as flavonoids, alkaloids, terpenoids, and saponins [ 22 ] are able to perform a double mode of action on P-gp: they can interfere with its transcriptional expression and/or directly inhibit its function. These compounds can be substrates for P-gp and compete with anticancer agents to bind to the active site of the transporter (drug-binding pocket, DBP) and reduce drug efflux.…”

Section: Natural Inhibitors Of P-glycoprotein In Leukemiamentioning

confidence: 99%

“…P-gp inhibitors of plant origin, belonging to various classes of secondary metabolites, were identified. Several published reviews summarize the most relevant advances in plant-focused P-gp inhibition research in different tumor models [ 22 , 25 , 26 , 27 ]. There are many examples of the ability of natural molecules, as fourth-generation inhibitors, to modulate P-gp in leukemia tumor models ( Table 1 ).…”

Section: Natural Inhibitors Of P-glycoprotein In Leukemiamentioning

confidence: 99%

Natural Inhibitors of P-glycoprotein in Acute Myeloid Leukemia

Labbozzetta

Poma

Notarbartolo

2023

IJMS

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Acute myeloid leukemia (AML) remains an insidious neoplasm due to the percentage of patients who develop resistance to both classic chemotherapy and emerging drugs. Multidrug resistance (MDR) is a complex process determined by multiple mechanisms, and it is often caused by the overexpression of efflux pumps, the most important of which is P-glycoprotein (P-gp). This mini-review aims to examine the advantages of using natural substances as P-gp inhibitors, focusing on four molecules: phytol, curcumin, lupeol, and heptacosane, and their mechanism of action in AML.

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“…[17] However, the weaknesses of poor solubility and stability, and low oral bioavailability, affect its clinical application and limit its further development. [18,19] In recent years, there are an increasing number of reaches for improvements of its solubility and stability via alteration of its solid phase forms with BER chloride as reactant. [20,21] Nevertheless, solubility of BER was not significantly improved.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous Improvements of Physicochemical Properties and Anti‐Microbial Activity of Berberine via Forming Salt with Gallic Acid

Chen,

Yang,

Ren

et al. 2024

Cryst. Res. Technol.

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Implementing combination medication through crystal engineering technology receives increasing attention from researchers due to improvements in the clinical treatment effects as well as the physicochemical properties of the drug. Berberine (BER) is commonly used to treat gastroenteritis and bacterial diarrhea, with the problems of poor solubility and low oral bioavailability. Recently, it is found that gallic acid (GA) also has anti‐inflammatory and anti‐bacterial activities. Therefore, if the above‐mentioned two ingredients can be combined, it is possible to enhance the therapeutic effects and physicochemical properties of BER. Inspired by this, 8‐hydroxy‐7,8‐dihydroberberine (8H‐HBER) in this study is employed to react with gallic acid to yield BER gallate dihydrate (2BER‐2GA‐2 W). Furthermore, dissolution experiments demonstrate that the maximum apparent solubility (MAS) of 2BER‐2GA‐2 W in dilute hydrochloric acid solution medium (pH 1.2) has increased by 7 times compared to the commercial form of BER, because of avoiding the common‐ion effect. Moreover, 2BER‐2GA‐2 W has also obviously enhanced stability relative to the commercial form of BER. In addition, 2BER‐2GA‐2 W has a better inhibitory effect on Staphylococcus aureus (S. aureus) relative to the commercial form of BER. Hence, 2BER‐2GA‐2 W will be a promising solid‐state form of BER for its further development.

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Role of natural P-gp inhibitor in the effective delivery for chemotherapeutic agents

Cited by 21 publications

References 92 publications

Astragaloside IV, as a potential anticancer agent

Astragaloside IV, as a potential anticancer agent

Natural Inhibitors of P-glycoprotein in Acute Myeloid Leukemia

Simultaneous Improvements of Physicochemical Properties and Anti‐Microbial Activity of Berberine via Forming Salt with Gallic Acid

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