Cajanus cajan – a source of PPARγ activators leading to anti-inflammatory and cytotoxic effects

Abstract

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.

Separation of six compounds from pigeon pea leaves by elution–extrusion counter‐current chromatography

“…13 C‐NMR (CDCl 3 , δ /ppm): 175.83 (‐COOH), 162.47 (C‐2), 162.32 (C‐4), 141.96 (C‐6), 137.31 (C‐1′), 131.97 (C‐C), 130.85 (C‐G), 130.39 (C‐F), 128.77 (C‐3′, 5′), 127.90 (C‐4′), 126.83 (C‐2′, 6′), 121.93 (C‐B), 116.80 (C‐3), 103.36 (C‐5), 103.08 (C‐1), 55.75 (‐OCH 3 ), 25.84 (C‐E), 22.12 (C‐A), 17.82 (C‐D). The above results were consistent with the literature and the compound was identified as cajaninstilbene acid.…”

“…13 C‐NMR (CDCl 3 , δ /ppm): 161.14 (C‐3), 156.86 (C‐1), 139.71 (C‐5), 137.07 (C‐1′), 129.42 (C‐4′), 128.71 (C‐3′, 5′), 128.32 (C‐A), 127.80 (C‐B), 126.60 (C‐2′, 6′), 105.94 (C‐6), 104.95 (C‐4), 101.00 (C‐2), 55.40 (‐OCH 3 ). The above results were consistent with the literature and the compound was identified as 3‐methoxy‐5‐(2‐phenylethenyl)‐phenol.…”

“…The compounds feature, highresolution MS, and 1-D NMR spectroscopy results were: 25.84 (C-E), 22.12 (C-A), 17.82 (C-D). The above results were consistent with the literature [30] and the compound was identified as cajaninstilbene acid.…”

Molecular targets of vitexin and isovitexin in cancer therapy: a critical review

“…Generally, flavone C‐ glycosides are structural analogues of natural estrogen and are thought to function like selective estrogen receptor modulators and therefore have anticancer effects against hormone‐related cancers. Vitexin and isovitexin have cytotoxic effects on breast (MCF‐7), prostate (PCO‐3), cervix (HeLa), and ovarian cancer (OVCAR) cells by inducing apoptosis via cleavage of PARP, upregulation of Bax, and downregulation of Bcl‐2 . This stimulation of apoptosis seems to be mediated by activation of caspases.…”

Cajaninstilbene Acid Ameliorates Cognitive Impairment Induced by Intrahippocampal Injection of Amyloid-β1–42 Oligomers

“…Cajaninstilbene acid (CSA), a main bioactive stilbene from pigeon pea [ Cajanus cajan (L.) Millsp.] leaves, possesses many bioactivities, including anti-bacterial (Kong et al, 2010), anti-tumor (Fu et al, 2015), anti-osteoporosis (Sun et al, 2019), anti-oxidative (Wu et al, 2011), anti-inflammatory (Patel and Bhutani, 2014; Huang et al, 2016; Schuster et al, 2016), and neuroprotective (Jiang et al, 2014; Liu et al, 2014a) effects. It is reported that stilbenes containing extract-fraction from Cajanus cajan (L.) leaves (sECC) ameliorated Aβ 25–35 -induced cognitive impairment (Ruan et al, 2009).…”