Apigenin and apigeninidin isolates from the Sorghum bicolor leaf targets inflammation via cyclo-oxygenase-2 and prostaglandin-E2 blockade.

Abstract

AIM:

This study evaluated the anti-inflammatory properties of a species of Sorghum bicolor leaf (SBL) grown in West Africa.

METHOD:

Cyclo-oxygenase (COX)-2:COX-1 selectivity assay was carried out by plating isolated peripheral blood mononuclear cells in culture medium with specific SBL fractions: crude extract (J), ethyl-acetate (JE) and aqueous (JA); secondary compounds from JE (JE5, JE6, JE7 and JE8); purified (P9) and semi-purified (P8) compounds from JE5 at 5-200 μg/mL for 1 hour. Test compounds and controls ibuprofen (50 μmol/L) and CAY10404 (1 μmol/L; 10 μmol/L) were added to two sets of plates, one without lipopolyshaccharide (LPS) and the other with LPS (1 μg/mL) for 24 hour. COX-2IC50 :COX-1IC50 ratio represented 50% inhibition of the activity of COX-2 to that of COX-1 using ibuprofen as control. In separate experiments the supernatant of P8 and P9-treated fractions of SBL and controls were plated with RAW 264.7 macrophage cells to measure prostaglandin (PG)-E2 production and cell proliferation activity.

RESULTS:

JA fraction of SBL had the highest ratio of COX-2IC50 :COX-1IC5041.214 whereas JE had the lowest ratio COX-2IC50 :COX-1IC501.161 . Interestingly, JE5 derived from JE showed a ratio of COX-2IC50 :COX-1IC500.495 while P8 derived from JE5 showed a dose-dependent reduction in COX-2IC50 :COX-1IC50 ratio and in PG-E2 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.

• Authors: Samira B L Makanjuola, Abiodun O Ogundaini, Louis C Ajonuma, Adedoyin Dosunmu
• Journal: International journal of rheumatic diseases (Int J Rheum Dis) Vol. 21 Issue 8 Pg. 1487-1495 (Aug 2018) ISSN: 1756-185X [Electronic] England
• PMID: 30146750 (Publication Type: Journal Article)
• Copyright: © 2018 Asia Pacific League of Associations for Rheumatology and John Wiley & Sons Australia, Ltd.

Chemical References

• Anthocyanins
• Cyclooxygenase 2 Inhibitors
• Membrane Proteins
• Apigenin
• apigeninidin
• Ptgs2 protein, mouse
• Cyclooxygenase 1
• Cyclooxygenase 2
• PTGS1 protein, human
• PTGS2 protein, human
• Ptgs1 protein, mouse
• Dinoprostone

Topics

• Animals
• Anthocyanins (isolation & purification, pharmacology)
• Apigenin (isolation & purification, pharmacology)
• Cell Proliferation (drug effects)
• Cyclooxygenase 1 (metabolism)
• Cyclooxygenase 2 (metabolism)
• Cyclooxygenase 2 Inhibitors (isolation & purification, pharmacology)
• Dinoprostone (metabolism)
• Leukocytes, Mononuclear (drug effects, enzymology)
• Macrophages (drug effects, enzymology)
• Membrane Proteins (metabolism)
• Mice
• Nigeria
• Phytotherapy
• Plant Leaves (chemistry)
• Plants, Medicinal
• RAW 264.7 Cells
• Signal Transduction (drug effects)
• Sorghum (chemistry)