Phillygenin is an active ingredient from Forsythia with many medicinal properties, such as antioxidant, reducing blood lipid, inhibition of low density lipoprotein oxidation .
Phillygenin (Forsythigenol) is an active ingredient from Forsythia with many medicinal properties, such as antioxidant, reducing blood lipid, inhibition of low density lipoprotein oxidation. PHI (Phillygenin) attenuates CCl4(10% carbon tetrachloride)-induced liver fibrosis partly via modulating inflammation and gut microbiota[3]. PHI inhibited the inflammation and apoptosis of pulmonary epithelial cells by activating PPARγ signaling via downregulating MMP8[4]. Phillygenin inhibited the growth of SH-1-V1 cells and exhibited an IC50 of 6 µM. Phillygenin inhibited in vitro and in vivo cancer cell growth in drug-resistant human esophageal cancer cells, and these effects were mediated via apoptosis, ROS generation, mitochondrial membrane potential loss, and activation of the NF-kB signalling pathway[5]. PHI could inhibit the proliferation, migration, and EMT (epithelial-mesenchymal transition) of pancreatic cancer cells (PANC-1 and SW1990) and induce its apoptosis[6].
179068-02-1 PHCCC
Phillygenin/连翘脂素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Rat cerebrocortical nerve terminals (synaptosomes)
5-30 µM
10 minutes
Phillygenin suppressed 4-AP-induced glutamate release in a concentration-dependent manner with an IC50 value of 17 µM.
Biomedicines. 2024 Feb 22;12(3):495
HEK 293T cells
20 and 40 µM
24 hours
PHI significantly promoted TGR5 activation (Fig. 7H) and elevated intracellular cAMP levels in HEK 293T cells (Fig. 7I).
J Pharm Anal. 2025 Jan;15(1):101042
NCM460 cells
20 and 40 µM
24 hours
PHI treatment enhanced the expression of tight junction proteins (ZO-1, E-cadherin, and occludin) and suppressed fibrosis markers (N-cadherin, α-SMA, and MMP9) and apoptosis marker (cleaved caspase-3).
J Pharm Anal. 2025 Jan;15(1):101042
VSC4.1 cells
0, 25, 50, 100 μg/mL
24 hours
To evaluate the effect of PHI on VSC4.1 neuronal cell apoptosis. Results showed that PHI pretreatment partially mitigated the morphological changes induced by LPS-activated microglia and significantly increased the expression of Bcl-xL protein.
J Orthop Translat. 2024 Aug 8;48:133-145
BV2 cells
0, 12.5, 25, 50, 100, 200, 400 μg/mL
24 hours
To evaluate the effect of PHI on BV2 cell viability. Results showed that PHI did not exert significant toxic effects on microglia at concentrations below 100 μg/mL.
J Orthop Translat. 2024 Aug 8;48:133-145
Primary murine chondrocytes
5, 10, 20, 40 µM
24 hours
To evaluate the effect of PHI on IL-1β-induced inflammation and ECM degradation. Results showed PHI dose-dependently suppressed pro-inflammatory cytokines (iNOS, COX-2, IL-6, TNF-α) and reduced ECM degradation (inhibited MMP-13 and ADAMTS5, increased Collagen II and Aggrecan).
J Orthop Translat. 2023 May 4;41:1-11
Gastric cancer cell BGC823
100 µg/ml
24 hours
Evaluate the toxicity of Phillygenin on gastric cancer cells
Front Microbiol. 2022 Apr 28;13:863624
Gastric epithelial cell (GES)-1
100 µg/ml
24 hours
Evaluate the toxicity of Phillygenin on gastric epithelial cells
Front Microbiol. 2022 Apr 28;13:863624
BGC823
100 μg/mL
24 hours
To detect the cytotoxicity of PHI-Der on BGC823 cells, results showed survival rates above 90% at 100 μg/mL concentration.
Front Microbiol. 2023 May 19;14:1071603
GES-1
100 μg/mL
24 hours
To detect the cytotoxicity of PHI-Der on GES-1 cells, results showed survival rates above 90% at 100 μg/mL concentration.
Front Microbiol. 2023 May 19;14:1071603
BEAS-2B cells
12.5, 25 and 50 µg/ml
24 hours
To evaluate the effect of PHI on LPS-induced inflammation and apoptosis in BEAS-2B cells. Results showed that PHI treatment suppressed LPS-induced inflammation and apoptosis.
Mol Med Rep. 2021 Nov;24(5):775
Rat hepatocytes
193.0 ± 47.6 µM
8 hours
Inhibited IL-1β-induced NO production and reduced iNOS mRNA and proinflammatory gene (e.g., Tnf and Il1r1) mRNA levels
To evaluate the oral bioavailability of PG-SMEDDS, the results showed that PG-SMEDDS significantly improved the absorption and bioavailability of PG (relative bioavailability was 587.77%).
Pharmaceutics. 2020 Feb 3;12(2):130
C57BL/6 mice
DMM-induced osteoarthritis model
Intragastric administration
20 mg/kg/d
Once daily for 8 weeks
To assess the protective effect of PHI on OA progression in DMM model. Results demonstrated PHI significantly improved cartilage erosion and proteoglycan loss, reduced OARSI scores, and alleviated OA progression via activating Nrf2 and inhibiting NF-κB pathway.
J Orthop Translat. 2023 May 4;41:1-11
C57BL/6J mice
DSS-induced chronic colitis
Oral
25, 50, and 100 mg/kg
Once daily for 30 days
PHI treatment significantly alleviated the symptoms of chronic colitis in mice, including body weight loss, disease activity index scores, colon shortening, splenomegaly, oxidative stress, and inflammatory response. PHI treatment also ameliorated the reduction of tight junction proteins, fibrosis, apoptosis, and intestinal stem cell activity.
J Pharm Anal. 2025 Jan;15(1):101042
C57BL/6 mice
Acute gastritis mouse model
Intragastric administration
28 mg/kg and 7 mg/kg
Once a day for 3 consecutive days
Evaluate the antibacterial effect of Phillygenin in vivo
Front Microbiol. 2022 Apr 28;13:863624
C57BL/6 mice
Acute gastritis model
Oral
28 mg/kg and 7 mg/kg
Once daily for 3 consecutive days
To evaluate the in vivo therapeutic effect of PHI-Der on H. pylori infection, results showed that PHI-Der significantly inhibited the colonization of H. pylori, reduced the inflammatory response, and promoted the repair of inflammatory damage.
Front Microbiol. 2023 May 19;14:1071603
Sprague-Dawley rats
Severe acute pancreatitis (SAP) model
Intraperitoneal injection
30 mg/kg
Single dose, lasting 12 hours
To investigate the mechanism by which PHI rescues impaired autophagy flux by modulating the PI3K/Akt/mTOR signaling pathway in SAP rats. Results showed reduced serum amylase and lipase levels, decreased pancreatic pathology scores, and improved autophagy-related protein expression after PHI intervention.
Int J Immunopathol Pharmacol. 2024 Jan-Dec;38:3946320241309260
Sprague Dawley rats
Spinal cord injury model
Intraperitoneal injection
50 mg/kg
Immediately after injury, continued for 7 days
To evaluate the effect of PHI on inflammatory response, neuronal apoptosis, axonal regeneration, and motor function recovery after spinal cord injury. Results showed that PHI significantly inhibited the inflammatory response and neuronal apoptosis, promoted axonal regeneration, and improved motor function recovery.
J Orthop Translat. 2024 Aug 8;48:133-145
C57BL/6 mice
DSS-induced acute ulcerative colitis
Oral
60 and 20 mg/kg
Throughout the whole experiment
PHI was able to maintain body weight, reduce DAI and mortality, restore the intestinal mucosal barrier, and inhibit cytokine secretion. PHI reduces macrophage infiltration into colon tissue.
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