Psoralen, an ingredient from Fructus Psoraleae, intercalates with DNA, inhibiting DNA synthesis and cell division and showing anticancer activity. Psoralen exhibits a wide range of biological properties, including anti-cancer, antioxidant, antidepressant, anticancer, antibacterial, and antiviral, et al[3]. Psoralen may function to inhibit breast cancer cell growth in the bone microenvironment and regulate the function of osteoblasts and osteoclasts in tumor-bearing mice[4]. When the rats were pretreated with psoralen (20 mg/kg/day for 10 days), the system exposure of anastrozole would be increased significantly[5]. The acute oral median lethal dose of psoralen in ICR mice was determined to be 1,673 mg/kg. Psoralen inhibited the viability of normal human liver L02 cells in vitro by inducing S-phase arrest. In addition, psoralen in both the mouse livers and L02 cells upregulated cyclin E1 and p27 protein levels[6]. Psoralen could induce hepatotoxicity by enhanced liver-to-body weight ratio and alterations of serum alanine aminotransferase (ALT), aspartate aminotransferase (AST) and total cholesterol after administration for 3 days. In addition, histopathological examinations also indicated the hepatotoxicity induced by psoralen[7]. Chronic exposure to low-level of psoralen causes a disturbance in alanine metabolism, glutamate metabolism, urea cycle, glucose-alanine cycle, ammonia recycling, glycine, and serine metabolism pathways[8].
Psoralen/补骨脂素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Caco-2 cells
50 µM
2 hours
To investigate the effects of psoralen on the transport of anastrozole in the Caco-2 cell transwell model. Results showed that psoralen increased the absorption of anastrozole and decreased its efflux by inhibiting P-gp activity.
Pharm Biol. 2018 Dec;56(1):433-439
Rat skin
2.0% (w/v)
24 hours
Evaluate the permeability of psoralen through the skin, showing that the skin deposition of psoralen from the optimized ethosome formulation (ES2) was 6.56-fold higher than that from the tincture.
Int J Nanomedicine. 2014 Jan 23;9:669-78
RAW 264.7 macrophages
62.5, 125, 250 µM
24 hours
To evaluate the effect of psoralen derivatives on the viability of RAW 264.7 cells, showing no significant differences at concentrations up to 250 μM.
Int J Mol Sci. 2022 May 22;23(10):5813.
Rat chondrocytes
0.01, 0.1, 1, 10, 100 µM
24, 48, 72 hours
Psoralen increased chondrocyte viability in a dose- and time-dependent manner, promoting chondrocyte proliferation.
Int J Mol Med. 2017 Nov;40(5):1377-1384
SMMC7721 hepatoma cells
20–80 µM
24–72 hours
Psoralen inhibited proliferation of SMMC7721 in a dose- and time-dependent manner, and promoted apoptosis.
Biol Res. 2019 Jul 5;52(1):34
Human synoviocytes
1-100 µM
3 days
PSO significantly reversed TNF-α induced up-regulation of MMP13 and ILs synoviocytes in a dose-dependent manner (1 to 20 µM).
Int J Biol Sci. 2019 Jan 1;15(1):229-238
Rat chondrocytes
1-100 µM
3 days
PSO (10 µM) activated cartilaginous specific ECM expression along with up-regulation of proliferative genes at transcriptional levels.
Int J Biol Sci. 2019 Jan 1;15(1):229-238
HepG2 hepatoma cells
10–80 µM
72 hours
Psoralen had little effect on HepG2 cell proliferation.
Biol Res. 2019 Jul 5;52(1):34
Rat liver microsomes
2 mM
30 minutes
To investigate the effects of psoralen on the metabolic stability of anastrozole in rat liver microsomes. Results showed that psoralen significantly decreased the intrinsic clearance rates of anastrozole.
Pharm Biol. 2018 Dec;56(1):433-439
Plasmid DNA
0.1-900 µM
30-90 minutes
To investigate the effect of psoralen combined with UVA light on plasmid DNA. Results showed that psoralen alone was not toxic, but when combined with UVA light, DNA single-strand breaks increased, leading to a reduction in supercoiled conformation.
Int J Mol Sci. 2022 Dec 3;23(23):15233
Rat chondrocytes
1 µM
48 hours
Psoralen promoted chondrocyte proliferation by activating the Wnt/β-catenin signaling pathway, upregulating the expression of Wnt-4, Frizzled-2, β-catenin, and cyclin D1, and downregulating GSK-3β expression.
Int J Mol Med. 2017 Nov;40(5):1377-1384
Human primary chondrocytes
12 μg/mL
5 days
To verify that psoralen inhibits chondrocyte inflammation via an estrogen-like effect. Results showed that psoralen promoted the expression of estrogen target genes CTSD, PGR, and TFF1 and decreased the expression of inflammation-related genes TNF-α, IL-1β, and IL-6.
Aging (Albany NY). 2022 Aug 24;14(16):6716-6726
L02 hepatocytes
10–80 µM
72 hours
10–40 μM psoralen had little effect on L02 cell proliferation, while 80 μM psoralen inhibited L02 cell proliferation.
Biol Res. 2019 Jul 5;52(1):34
HepG2.2.15 cells
126.4 µM (IC50)
8 days
Evaluate the inhibitory effect of psoralen on HBV replication, showing that psoralen inhibits HBV replication in a concentration-dependent manner.
Virol Sin. 2022 Apr;37(2):256-265
FaDu cells
0.1-900 µM
90 minutes
To investigate the effect of psoralen combined with UVA light on the survival of FaDu cells. Results showed that psoralen alone was not cytotoxic, but when combined with UVA light, cell damage increased depending on psoralen concentration and irradiation time.
Int J Mol Sci. 2022 Dec 3;23(23):15233
Psoralen/补骨脂素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Human
Graft-versus-host disease (GVHD) patients
Extracorporeal photopheresis (ECP)
0.9 μM 8-MOP
10-15 minutes
To study the effect of ECP treatment on Akt phosphorylation in T-lymphocytes from GVHD patients, results showed significantly decreased Akt phosphorylation post-treatment.
J Biol Chem. 2016 Nov 18;291(47):24364-24376
SD rats
MIA-induced osteoarthritis model
Intra-articular injection
1 mg/kg
Daily for 1 week, and once every three days for another 1 week
Following six weeks of PSO treatments to articular cartilage osteoarthritis, compared to MIA-induced group, the appearance and physiological structure of articular cartilage was more integrated with greatly organized chondrocytes and abundant cartilage matrix.
Int J Biol Sci. 2019 Jan 1;15(1):229-238
New Zealand rabbits
OA animal model induced by anterior cruciate ligament transection (ACLT)
Joint cavity injection
1 mg/mL, 0.1 mL/kg
Once a week, total of 5 times
To verify the therapeutic effect of psoralen on rabbit OA. Results showed that the psoralen group had less cartilage tissue destruction, decreased OARSI scores, increased subchondral bone mineral density (BMD), trabecular thickness and number, and decreased trabecular separation.
Aging (Albany NY). 2022 Aug 24;14(16):6716-6726
Male Sprague Dawley rats
Rat skin model
Topical administration
2.0% (w/v)
Single dose, continued for 10 hours
Evaluate the release of psoralen from ethosomes in vivo using microdialysis, showing significantly higher drug concentration in the skin compared to the tincture.
Int J Nanomedicine. 2014 Jan 23;9:669-78
Male Sprague-Dawley rats
No specific model
Oral gavage
20 mg/kg/day
Once daily for 10 days
To investigate the effects of psoralen pretreatment on the pharmacokinetics of anastrozole in rats. Results showed that psoralen significantly increased the systemic exposure of anastrozole.
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