Isosakuranetin

Isosakuranetin is a flavanone that has been found in Citrus species and has diverse biological activities.^{1,2,3,4,5,6,7} It inhibits calcium uptake induced by pregnenolone sulfate (PregS; Item No. 21004) in HEK293 cells expressing mouse transient receptor potential melastatin 3 (TRPM3; IC₅₀ = 50 nM).¹ Isosakuranetin is selective for TRPM3 over TRPM1, TRPM8, and TRP vanilloid-related 1 (TRPV1) when used at a concentration of 10 μM. In vivo, isosakuranetin (2 mg/kg) increases latency to first pain-related response in mice in a hot plate test and reduces the number and duration of PregS-induced nocifensive responses, such as paw licking, shaking, or lifting, in mice. It also reduces systolic blood pressure in spontaneously hypertensive rats when administered at a dose of 10 mg/kg.² Isosakuranetin (20 µM) inhibits UV-B-induced matrix metalloproteinase-1 (MMP-1) expression by 90% in HaCaT human keratinocyte cells, as well as phosphorylation of ERK1/2 when used at a concentration of 50 µM.³ It blocks hydrogen peroxide-induced increases in reactive oxygen species (ROS), intracellular calcium concentration, caspase-3 activity, and JNK phosphorylation, as well as decreases in catalase activity, in PC12 cells when used at a concentration of 0.8 µM.⁴ Isosakuranetin also has antibacterial and trypanocidal activity against M. tuberculosis, C. neoformans, and T. cruzi.^5,6,7

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1. Straub, I., Krügel, U., Mohr, F., et al. Flavanones that selectively inhibit TRPM3 attenuate thermal nociception in vivo. Mol. Pharmacol. 84(5), 736-750 (2013).

2. Maruyama, H., Sumitou, Y., Sakamoto, T., et al. Antihypertensive effects of flavonoids isolated from brazilian green propolis in spontaneously hypertensive rats. Biol. Pharm. Bull. 32(7), 1244-1250 (2009).

3. Jung, H., Lee, E.H., Lee, T.H., et al. The methoxyflavonoid isosakuranetin suppresses UV-B-induced matrix metalloproteinase-1 expression and collagen degradation relevant for skin photoaging. Int. J. Mol. Sci. 17(9), E1449 (2016).

4. Hwang, S.-L., and Yen, G.-C. Modulation of Akt, JNK, and p38 activation is involved in citrus flavonoid-mediated cytoprotection of PC12 cells challenged by hydrogen peroxide. J. Agric. Food Chem. 57(6), 2576-2582 (2009).

5. Suksamrarn, A., Chotipong, A., Suavansri, T., et al. Antimycobacterial activity and cytotoxicity of flavonoids from the flowers of Chromolaena odorata. Arch. Pharm. Res. 27(5), 507-511 (2004).

6. da Silva Filho, A.A., de Sousa, J.P., Soares, S., et al. Antimicrobial activity of the extract and isolated compounds from Baccharis dracunculifolia D. C. (Asteraceae). Z. Naturforsch. C. 63(1-2), 40-46 (2008).

7. da Silva Filho, A.A., Pires Bueno, P.C., Gregório, L.E., et al. In-vitro trypanocidal activity evaluation of crude extract and isolated compounds from Baccharis dracunculifolia D.C. (Asteraceae). J. Pharm. Pharmacol. 56(9), 1195-1199 (2004).