Calycosin

Calycosin, a naturally occurring isoflavonoid found predominantly in Astragalus membranaceus, has antioxidant, anti-inflammatory, and anti-apoptotic properties^[1]. By inhibiting the activation of NF-κB, Calycosin can reduce the production of pro-inflammatory cytokines (TNF-α, IL-1β, and IL-6), and alleviate the inflammatory response^[2]. Calycosin has been widely used to stabilize membrane structures, improve membrane integrity, and alleviate cellular oxidative damage^[3].

In vitro, Calycosin treatment for 24 hours significantly inhibited the viability of AGS, KATO-3, and MKN-28 cells, with IC₅₀ values of 47.18µM, 82.17µM and 71.93µM, respectively^[4]. Treatment with 80µM Calycosin for 48 hours significantly induced apoptosis in HT29 cells, accompanied by a decrease in the protein level of LC31 and an increase in the protein levels of LC3II and Beclin-1^[5]. Treatment with 100µM Calycosin for 24 hours significantly inhibited the IGF-1R signaling pathway in MDA-435 cells and reduced cell viability^[6].

In vivo, Calycosin treatment via oral administration at a dose of 50mg/kg daily for 10 days significantly alleviated the intestinal damage in mice induced by dextran sulfate sodium (DSS) and prevented the weight loss of the mice^[7]. Oral administration of Calycosin at a dose of 50mg/kg/day for 3 days significantly alleviated myocardial fibrosis and cardiac dysfunction following myocardial infarction in mice^[8].

References:
[1] Ahmed H S. Neuropharmacological effects of calycosin: a translational review of molecular mechanisms and therapeutic applications[J]. Naunyn-Schmiedeberg's Archives of Pharmacology, 2025, 398(10): 12891-12909.
[2] Gong G, Zheng Y, Yang Y, et al. Pharmaceutical values of calycosin: one type of flavonoid isolated from astragalus[J]. Evidence‐Based Complementary and Alternative Medicine, 2021, 2021(1): 9952578.
[3] Gao J Q, Liu Z J, Chen T, et al. Pharmaceutical properties of calycosin, the major bioactive isoflavonoid in the dry root extract of Radix astragali[J]. Pharmaceutical biology, 2014, 52(9): 1217-1222.
[4] Zhang Y, Zhang J Q, Zhang T, et al. Calycosin induces gastric cancer cell apoptosis via the ROS-mediated MAPK/STAT3/NF-κB pathway[J]. OncoTargets and therapy, 2021: 2505-2517.
[5] El‐kott A F, Al‐kahtani M A, Shati A A. Calycosin induces apoptosis in adenocarcinoma HT 29 cells by inducing cytotoxic autophagy mediated by SIRT 1/AMPK‐induced inhibition of Akt/mTOR[J]. Clinical and Experimental Pharmacology and Physiology, 2019, 46(10): 944-954.
[6] Chen J, Hou R, Zhang X, et al. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF-1R, p38 MAPK and PI3K/Akt pathways[J]. PloS one, 2014, 9(3): e91245.
[7] Chao L, Zheng P, Xia L, et al. Calycosin attenuates dextran sulfate sodium (DSS)-induced experimental colitis[J]. Iranian Journal of Basic Medical Sciences, 2017, 20(9): 1056.
[8] Chen G, Xu H, Xu T, et al. Calycosin reduces myocardial fibrosis and improves cardiac function in post-myocardial infarction mice by suppressing TGFBR1 signaling pathways[J]. Phytomedicine, 2022, 104: 154277.