Exploring the Anti-Diabetic Potential of Quercetagitrin through Dual Inhibition of PTPN6 and PTPN9

Gone, Geetanjali B.; Go, Geonhui; Nam, Gibeom; Jeong, Woojoo; Kim, Hyemin; Lee, Soah; Chung, Sang J.

doi:10.3390/nu16050647

Open AccessArticle

Exploring the Anti-Diabetic Potential of Quercetagitrin through Dual Inhibition of PTPN6 and PTPN9

by

Geetanjali B. Gone

^1,†,

Geonhui Go

^1,†,

Gibeom Nam

¹

,

Woojoo Jeong

¹,

Hyemin Kim

¹,

Soah Lee

^1,2,* and

Sang J. Chung

^1,2,*

¹

Department of Biopharmaceutical Convergence, Sungkyunkwan University, Suwon 16419, Republic of Korea

²

School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea

^*

Authors to whom correspondence should be addressed.

^†

These authors contributed equally to this work.

Nutrients 2024, 16(5), 647; https://doi.org/10.3390/nu16050647

Submission received: 29 January 2024 / Revised: 19 February 2024 / Accepted: 23 February 2024 / Published: 25 February 2024

(This article belongs to the Special Issue Nutritional Regulation of Plant Extracts on Human Health)

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Abstract

Protein tyrosine phosphatases (PTPs) are pivotal contributors to the development of type 2 diabetes (T2DM). Hence, directing interventions towards PTPs emerges as a valuable therapeutic approach for managing type 2 diabetes. In particular, PTPN6 and PTPN9 are targets for anti-diabetic effects. Through high-throughput drug screening, quercetagitrin (QG) was recognized as a dual-target inhibitor of PTPN6 and PTPN9. We observed that QG suppressed the catalytic activity of PTPN6 (IC₅₀ = 1 μM) and PTPN9 (IC₅₀ = 1.7 μM) in vitro and enhanced glucose uptake by mature C2C12 myoblasts. Additionally, QG increased the phosphorylation of adenosine monophosphate-activated protein kinase (AMPK) and insulin-dependent phosphorylation of Akt in mature C2C12 myoblasts. It further promoted the phosphorylation of Akt in the presence of palmitic acid, suggesting the attenuation of insulin resistance. In summary, our results indicate QG’s role as a potent inhibitor targeting both PTPN6 and PTPN9, showcasing its potential as a promising treatment avenue for T2DM.

Keywords: PTPN6; PTPN9; quercetagitrin; anti-diabetic; type 2 diabetes

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MDPI and ACS Style

Gone, G.B.; Go, G.; Nam, G.; Jeong, W.; Kim, H.; Lee, S.; Chung, S.J. Exploring the Anti-Diabetic Potential of Quercetagitrin through Dual Inhibition of PTPN6 and PTPN9. Nutrients 2024, 16, 647. https://doi.org/10.3390/nu16050647

AMA Style

Gone GB, Go G, Nam G, Jeong W, Kim H, Lee S, Chung SJ. Exploring the Anti-Diabetic Potential of Quercetagitrin through Dual Inhibition of PTPN6 and PTPN9. Nutrients. 2024; 16(5):647. https://doi.org/10.3390/nu16050647

Chicago/Turabian Style

Gone, Geetanjali B., Geonhui Go, Gibeom Nam, Woojoo Jeong, Hyemin Kim, Soah Lee, and Sang J. Chung. 2024. "Exploring the Anti-Diabetic Potential of Quercetagitrin through Dual Inhibition of PTPN6 and PTPN9" Nutrients 16, no. 5: 647. https://doi.org/10.3390/nu16050647

APA Style

Gone, G. B., Go, G., Nam, G., Jeong, W., Kim, H., Lee, S., & Chung, S. J. (2024). Exploring the Anti-Diabetic Potential of Quercetagitrin through Dual Inhibition of PTPN6 and PTPN9. Nutrients, 16(5), 647. https://doi.org/10.3390/nu16050647

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Exploring the Anti-Diabetic Potential of Quercetagitrin through Dual Inhibition of PTPN6 and PTPN9

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