دورية أكاديمية
Evidence of Insulin-Sensitizing and Mimetic Activity of the Sesquiterpene Quinone Avarone, a Protein Tyrosine Phosphatase 1B and Aldose Reductase Dual Targeting Agent from the Marine Sponge Dysidea avara
| العنوان: | Evidence of Insulin-Sensitizing and Mimetic Activity of the Sesquiterpene Quinone Avarone, a Protein Tyrosine Phosphatase 1B and Aldose Reductase Dual Targeting Agent from the Marine Sponge Dysidea avara |
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| المؤلفون: | Casertano, Marcello, Genovese, Massimo, Santi, Alice, Pranzini, Erica, Balestri, Francesco, Avunduk, Sibel |
| المساهمون: | MÜ, Sağlık Hizmetleri Meslek Yüksekokulu (Marmaris), Tıbbi Hizmetler Ve Teknikler Bölümü, orcid:0000-0002-3644-1516, Avunduk, Sibel |
| بيانات النشر: | MDPI |
| سنة النشر: | 2023 |
| مصطلحات موضوعية: | Marine natural products, Dysidea avara, avarone, Sesquiterpene‑type quinones |
| الوصف: | Type 2 diabetes mellitus (T2DM) is a complex disease characterized by impaired glucose homeostasis and serious long-term complications. First-line therapeutic options for T2DM treatment are monodrug therapies, often replaced by multidrug therapies to ensure that non-responding patients maintain target glycemia levels. The use of multitarget drugs instead of mono- or multidrug therapies has been emerging as a main strategy to treat multifactorial diseases, including T2DM. Therefore, modern drug discovery in its early stages aims to identify potential modulators for multiple targets; for this purpose, exploration of the chemical space of natural products represents a powerful tool. Our study demonstrates that avarone, a sesquiterpene quinone obtained from the sponge Dysidea avara, is capable of inhibiting in vitro PTP1B, the main negative regulator of the insulin receptor, while it improves insulin sensitivity, and mitochondria activity in C2C12 cells. We observe that when avarone is administered alone, it acts as an insulin-mimetic agent. In addition, we show that avarone acts as a tight binding inhibitor of aldose reductase (AKR1B1), the enzyme involved in the development of diabetic complications. Overall, avarone could be proposed as a novel natural hit to be developed as a multitarget drug for diabetes and its pathological complications. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 1999-4923 |
| العلاقة: | PHARMACEUTICS; Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı; Casertano, M.; Genovese, M.; Santi, A.; Pranzini, E.; Balestri, F.; Piazza, L.; Del Corso, A.; Avunduk, S.; Imperatore, C.; Menna, M.; Paoli, P. Evidence of Insulin-Sensitizing and Mimetic Activity of the Sesquiterpene Quinone Avarone, a Protein Tyrosine Phosphatase 1B and Aldose Reductase Dual Targeting Agent from the Marine Sponge Dysidea avara. Pharmaceutics 2023, 15, 528. https://doi.org/10.3390/pharmaceutics15020528Test; https://doi.org/10.3390/pharmaceutics15020528Test; https://hdl.handle.net/20.500.12809/10619Test; 15 |
| DOI: | 10.3390/pharmaceutics15020528 |
| الإتاحة: | https://doi.org/20.500.12809/10619Test https://doi.org/10.3390/pharmaceutics15020528Test https://hdl.handle.net/20.500.12809/10619Test |
| حقوق: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.F87E6DFE |
| قاعدة البيانات: | BASE |
Full Text Finder | تدمد: | 19994923 |
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| DOI: | 10.3390/pharmaceutics15020528 |