Pectolinarigenin

Pectolinarigenin, as a flavonoids compound, which can be isolated from the aerial parts of C. chanroenicum has been displayed biologic activities such as anti-inflammation and anti-allergy[1]. It also repressed cancer growth in vitro, including lung cancer, breast cancer and colorectal adenocarcinoma[2].

In vitro, pectolinarigenin inhibited significantly the growth of the SK-HEP-1 liver cancer cells and exhibited an IC50 of 10 µM, while against normal cells the cytotoxic effects were much less pronounced[3]. In vitro experiment it demenstrated that Pectolinarigenin at 10 µM obviously inhibited ROS accumulation after 24 h-treatment in HepG2 cells and also increased protein expression of NQO-1 and AKR1B10[4]. In vitro, 30 µM pectolinarigenin treatment suppressed melanin biosynthesis without cytotoxicity in melan-a cells[5]. Pectolinarigenin also reduced the lipid contents in vitro[6]. Treatment with 40 µM pectolinarigenin in A375 cells and in B16 cells increased >6-fold and 10-fold apoptotic rate compared with the respective untreated control groups[7].

In vivo, 10 mg/kg pectolinarigenin in mice could activate the Nrf2/ARE pathway and induced antioxidant enzymes as the same manner as the results from HepG2 cells[4]. In vivo efficacy test it shown that mice were administrated pectolinarigenin (20 mg/kg/2 days and 50 mg/kg/2 days) intraperitoneally blocked STAT3 activation and disturbed tumor growth and metastasis with superior pharmacodynamic properties[8]. In vivo test it exhibited that mice were administrated with 25 mg/kg/d orally for 7 days or 14 days effectively ameliorated kidney injury and tubulointerstitial fibrosis after unilateral ureteral obstruction (UUO) surgery[9].

References:

[1] H. Lim, et al. Anti-inflammatory activity of pectolinarigenin and pectolinarin isolated from Cirsium chanroenicum Biol. Pharm. Bull., 31 (2008), pp. 2063-2067.

[2] M. Bonesi, et al. In vitro biological evaluation of novel 7-O dialkylaminoalkyl cytotoxic pectolinarigenin derivatives against a panel of human cancer cell lines Bioorg. Med. Chem. Lett., 18 (2008), pp. 5431-5434.

[3] Liu S, et al. Pectolinarigenin flavonoid exhibits selective anti-proliferative activity in cisplatin-resistant hepatocellular carcinoma, autophagy activation, inhibiting cell migration and invasion, G2/M phase cell cycle arrest and targeting ERK1/2 MAP kinases. J BUON. 2020 Jan-Feb;25(1):415-420.

[4] Shiraiwa M, et al. Pectolinarigenin Induces Antioxidant Enzymes through Nrf2/ARE Pathway in HepG2 Cells. Antioxidants (Basel). 2022 Mar 30;11(4):675.

[5] Lee S, et al. Pectolinarigenin, an aglycone of pectolinarin, has more potent inhibitory activities on melanogenesis than pectolinarin. Biochem Biophys Res Commun. 2017;493:765-772.

[6] Zhang Y, Wan C, Song Z, Meng W, Wang S, Lan Z. Pectolinarigenin reduces the expression of sterol regulatory element-binding proteins and cellular lipid levels. Biosci Biotechnol Biochem. 2022 Aug 24;86(9):1220-1230.

[7] Deng Y, et al. Pectolinarigenin inhibits cell viability, migration and invasion and induces apoptosis via a ROS-mitochondrial apoptotic pathway in melanoma cells. Oncol Lett. 2020 Oct;20(4):116.

[8] Zhang T, et al. Pectolinarigenin acts as a potential anti-osteosarcoma agent via mediating SHP-1/JAK2/STAT3 signaling. Biomed Pharmacother. 2022 Sep;153:113323.

[9] Li Y, et al. Natural flavonoid pectolinarigenin alleviated kidney fibrosis via inhibiting the activation of TGFβ/SMAD3 and JAK2/STAT3 signaling. Int Immunopharmacol. 2021 Feb;91:107279.