Anti-Inflammatory Effect of Licochalcone A via Regulation of ORAI1 and K+ Channels in T-Lymphocytes

Hong, Phan Thi Lam; Kim, Hee Jin; Jo, Sungwoo; Kim, Woo Kyun; Namkung, W.; Nam, Joo Hyun

doi:10.3390/ijms221910847

Cited by 15 publications

(13 citation statements)

References 43 publications

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“…As can be observed in Figure 6, during the first timepoints, all of the Lico-A NPs and free Lico-A showed statistically significant differences against the control group (p < 0.001). This may be due to the potent Lico-A anti-inflammatory capacity previously reported by other groups and demonstrated here for ocular applications [64,65]. Among all the formulations, Lico-A PLGA-PEG-B6 NPs presented significantly increased anti-inflammatory activity compared to the other formulations and free Lico-A (Figure 7).…”

Section: Anti-inflammatory Therapeutic Efficacy Of Licochalcone-a Fun...supporting

confidence: 64%

Development of Peptide Targeted PLGA-PEGylated Nanoparticles Loading Licochalcone-A for Ocular Inflammation

et al. 2022

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Licochalcone-A is a natural compound with anti-inflammatory properties. However, it possesses low water solubility, making its application for the treatment of ocular inflammation difficult. To overcome this drawback, biodegradable nanoparticles incorporating Licochalcone-A have been developed. Additionally, to avoid fast clearance and increase cellular internalization into the ocular tissues, PLGA nanoparticles have been functionalized using PEG and cell penetrating peptides (Tet-1 and B6). To optimize the formulations, a factorial design was carried out and short-term stability of the nanoparticles was studied. Moreover, morphology was also observed by transmission electron microcopy and in vitro drug release was carried out. Ocular tolerance of the formulations was ensured in vitro and in vivo and anti-inflammatory therapeutic efficacy was also assessed. Surface functionalized nanoparticles loading Licochalcone-A were developed with an average size below 200 nm, a positive surface charge, and a monodisperse population. The formulations were non-irritant and showed a prolonged Licochalcone-A release. Despite the fact that both Licochalcone-A Tet-1 and B6 functionalized nanoparticles demonstrated to be suitable for the treatment of ocular inflammation, B6 targeted nanoparticles provided greater therapeutic efficacy in in vivo assays.

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Section: Anti-inflammatory Therapeutic Efficacy Of Licochalcone-a Fun...supporting

confidence: 64%

Development of Peptide Targeted PLGA-PEGylated Nanoparticles Loading Licochalcone-A for Ocular Inflammation

et al. 2022

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“…Nevertheless, the complete summary of the Kv1.3 inhibiting properties of this compound and its derivatives is clearly presented in Table 1 in [ 57 ]. Considering other chalcones, recent studies show that also Licochalcone A is effective in blocking the Kv1.3 channel [ 33 ]. Only the concentration of

was enough to reduce the ion channel activity by half.…”

Section: Kv Channelsmentioning

confidence: 99%

Flavonoids as Modulators of Potassium Channels

Richter

Trybek

Delfino

et al. 2023

IJMS

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Potassium channels are widely distributed integral proteins responsible for the effective and selective transport of K+ ions through the biological membranes. According to the existing structural and mechanistic differences, they are divided into several groups. All of them are considered important molecular drug targets due to their physiological roles, including the regulation of membrane potential or cell signaling. One of the recent trends in molecular pharmacology is the evaluation of the therapeutic potential of natural compounds and their derivatives, which can exhibit high specificity and effectiveness. Among the pharmaceuticals of plant origin, which are potassium channel modulators, flavonoids appear as a powerful group of biologically active substances. It is caused by their well-documented anti-oxidative, anti-inflammatory, anti-mutagenic, anti-carcinogenic, and antidiabetic effects on human health. Here, we focus on presenting the current state of knowledge about the possibilities of modulation of particular types of potassium channels by different flavonoids. Additionally, the biological meaning of the flavonoid-mediated changes in the activity of K+ channels will be outlined. Finally, novel promising directions for further research in this area will be proposed.

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“…LA inhibited ORAI1, Kv1.3, and KCa3.1 channels and significantly inhibited the production and secretion of IL-2 in T cells induced by CD3 and CD28 antibodies in vivo . Overall, LA may offer an effective therapeutic strategy for inflammation-related immune diseases ( Phan et al, 2021 ).…”

Section: Anti-inflammation Activities Of Lamentioning

confidence: 99%

Role of Licochalcone A in Potential Pharmacological Therapy: A Review

Xie

Jiang

et al. 2022

Front. Pharmacol.

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Licochalcone A (LA), a useful and valuable flavonoid, is isolated from Glycyrrhiza uralensis Fisch. ex DC. and widely used clinically in traditional Chinese medicine. We systematically updated the latest information on the pharmacology of LA over the past decade from several authoritative internet databases, including Web of Science, Elsevier, Europe PMC, Wiley Online Library, and PubMed. A combination of keywords containing “Licochalcone A,” “Flavonoid,” and “Pharmacological Therapy” was used to help ensure a comprehensive review. Collected information demonstrates a wide range of pharmacological properties for LA, including anticancer, anti-inflammatory, antioxidant, antibacterial, anti-parasitic, bone protection, blood glucose and lipid regulation, neuroprotection, and skin protection. LA activity is mediated through several signaling pathways, such as PI3K/Akt/mTOR, P53, NF-κB, and P38. Caspase-3 apoptosis, MAPK inflammatory, and Nrf2 oxidative stress signaling pathways are also involved with multiple therapeutic targets, such as TNF-α, VEGF, Fas, FasL, PI3K, AKT, and caspases. Recent studies mainly focus on the anticancer properties of LA, which suggests that the pharmacology of other aspects of LA will need additional study. At the end of this review, current challenges and future research directions on LA are discussed. This review is divided into three parts based on the pharmacological effects of LA for the convenience of readers. We anticipate that this review will inspire further research.

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Anti-Inflammatory Effect of Licochalcone A via Regulation of ORAI1 and K+ Channels in T-Lymphocytes

Cited by 15 publications

References 43 publications

Development of Peptide Targeted PLGA-PEGylated Nanoparticles Loading Licochalcone-A for Ocular Inflammation

Development of Peptide Targeted PLGA-PEGylated Nanoparticles Loading Licochalcone-A for Ocular Inflammation

Flavonoids as Modulators of Potassium Channels

Role of Licochalcone A in Potential Pharmacological Therapy: A Review

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