orientin and pinostrobin

Cajanus cajan is an important legume crop in the human diet in many parts of the world. Due to its pharmacological properties, C. cajan is, moreover, used in traditional medicine for treating skin diseases, diabetes, inflammatory disorders and various other dysfunctions. In this study, we focused on the role of peroxisome proliferator-activated receptor gamma (PPARγ) as a potential therapeutic target of Cajanus cajan and its main compounds for the treatment of cancer, inflammation and inflammation-related disorders. The anti-inflammatory potential of C. cajan and its bioactive compounds and their cytotoxicity on the human cervical adenocarcinoma cell line HeLa, the human colorectal adenocarcinoma cell line CaCo-2 and the human breast adenocarcinoma cell line MCF-7 were elucidated. C. cajan and its compounds exerted significant anti-inflammatory activity on lipopolysaccharide-stimulated macrophages, showed good cytotoxic effects on the 3 different cancer cell lines and proved PPARγ activity in vitro. The main active compounds were orientin, pinostrobin and vitexin. Cajaninstilbene acid and pinosylvin monomethylether were identified as novel PPARγ activators. Based on these data, C. cajan provides excellent beneficial medicinal attributes and may be used as a potential food or a pharmaceutical supplement.

Topics: Anti-Inflammatory Agents; Antineoplastic Agents, Phytogenic; Apigenin; Breast Neoplasms; Caco-2 Cells; Cajanus; Colorectal Neoplasms; Diet; Female; Flavanones; Flavonoids; Glucosides; HeLa Cells; Humans; MCF-7 Cells; Phytotherapy; Plant Extracts; PPAR gamma; Uterine Cervical Neoplasms

Antioxidant activities of the aqueous and ethanol extracts of pigeonpea [Cajanus cajan (L.) Millsp.] leaves, as well as petroleum ether, ethyl acetate, n-butanol and water fractions and the four main compounds separated from the ethanol extract, i.e. cajaninstilbene acid (3-hydroxy-4-prenylmethoxystilbene-2-carboxylic acid), pinostrobin, vitexin and orientin, were examined by a DPPH radical-scavenging assay and a beta-carotene-linoleic acid test. In the DPPH system, the antioxidant activity of the ethanol extracts was superior to that of the aqueous extracts, with IC(50) values were 242.01 and 404.91 microg/mL, respectively. Among the four fractions, the ethyl acetate one showed the highest scavenging activity, with an IC(50) value of 194.98 microg/mL. Cajaninstilbene acid (302.12 microg/mL) and orientin (316.21 microg/mL) showed more efficient radical-scavenging abilities than pinostrobin and vitexin. In the beta-carotene-linoleic acid test, the inhibition ratio (%) of the ethyl acetate fraction (94.13%+/-3.41%) was found to be the highest, being almost equal to the inhibition capacity of the positive control BHT (93.89%+/-1.45%) at 4 mg/mL. Pinostrobin (>500 microg/mL) and vitexin (>500 microg/mL) showed insignificant antioxidant activities compared with cajaninstilbene (321.53 microg/mL) and orientin (444.61 microg/mL). In general, the ethyl acetate fraction of the ethanol extract showed greater activity than the main compounds in both systems, such results might be attributed to the synergistic effects of the components. The antioxidant activities of all the tested samples were concentration-dependent. Based on the results obtained, we can conclude that the pigeonpea leaf extracts may be valuable natural antioxidant sources and are potentially applicable in both medicine and the healthy food industry.

Topics: Antioxidants; Apigenin; Cajanus; Flavanones; Flavonoids; Glucosides; Inhibitory Concentration 50; Plant Extracts; Plant Leaves; Solvents