Apigenin and apigeninidin isolates from theSorghum bicolorleaf targets inflammation via cyclo‐oxygenase‐2 and prostaglandin‐E₂blockade

Abstract

JA fraction of SBL had the highest ratio of COX-2IC :COX-1IC whereas JE had the lowest ratio COX-2IC :COX-1IC . Interestingly, JE5 derived from JE showed a ratio of COX-2IC :COX-1IC while P8 derived from JE5 showed a dose-dependent reduction in COX-2IC :COX-1IC5 ratio and in PG-E production, which was more effective compared to ibuprofen. A dose-dependent reduction in RAW 264.7 macrophage cell proliferation was also observed in P8-treated cells. The phenolic compounds identified in P8 include apigenin and apigeninidin adducts which may explain the exceptional anti-inflammatory activity and efficacy in COX-2 targeting.

The Inhibitory Effect of Flavonoid Aglycones on the Metabolic Activity of CYP3A4 Enzyme

“…Residual activity of CYP3A4 after incubations with flavones apigenin, chrysin, chrysin dimethyl ether, and tangerine was 24%, 17%, 61%, and 42% ( Table 1 ). Apigenin has been well studied due to it positive effects in prevention of breast cancer, and positive effects on cardio myoblasts and pancreatic cells in pancreatitis [ 39 , 40 , 41 , 42 , 43 ]. At 1 µM concentration, decrease in activity of 76% for was observed apigenin.…”

Sorghum Grain: From Genotype, Nutrition, and Phenolic Profile to Its Health Benefits and Food Applications

“…This photochromic property can be potentially used to develop photochromic foods, such as color changeable candies, providing additional value and attractiveness to foods. Besides, as mentioned above, 3‐deoxyanthocyanidins are potent antioxidants and have anti‐inflammatory and anticancer activities (Awika et al., ; Makanjuola et al., ; Shih et al., ; Yang et al., ), so they could be added in food as therapeutic agents to prevent some chronic diseases. 3‐Deoxyanthocyanidins are promising natural and multifunctional colorants in the food system.…”

“…During inflammation, a number of pro‐inflammatory compounds such as interleukin (IL), cyclooxygenase (COX)‐2, tumor necrosis factor (TNF)‐α, and prostaglandin E2 (PG‐E2) are generated (Shim, Kim, Jang, Ko, & Kim, ). Many phenolic compounds from sorghum grain have been demonstrated to inhibit the production of these pro‐inflammatory compounds (Burdette, ; Funakoshi‐Tago, Nakamura, Tago, Mashino, & Kasahara, ; Makanjuola, Ogundaini, Ajonuma, & Dosunmu, ; Shim et al., ; Wölfle et al., ). For example, phenolic acids, such as gallic acid and ferulic acids, were reported to suppress the COX‐2 enzyme, and ferulic acid has been shown to inhibit the production of TNF‐α (Burdette, ).…”

Polyphenols in the treatment of autoimmune diseases

“…As for COX and LOX enzymes, flavones are predominantly COX inhibitors, whereas flavanols are preferentially LOX inhibitors [77]. Thus, flavonoids, such as luteolin, galangin, morin and apigenin exert notable COX inhibitory effects [78,79]. Flavanols, including quercetin, kaempferol, myricetin and morin, in turn, inhibit LOX enzymes [80].…”