Benserazide hydrochloride is commonly used in Parkinson's disease and is an inhibitor of peripheral aromatic L-amino acid decarboxylase (AADC). Benserazide reduces the central AADC activity in the striatum of rats with nigrostriatal denervation, which leads to changes in the metabolism of exogenous L-DOPA[2]. Benserazide hydrochloride (BH) and Levodopa (LD) individually and in combination (BH + LD) (25 μM; 0 hour, 12 hours, 24 hours and 168 hours; SH-SY5Y) treatment inhibit protein aggregation and have the ability to minimise the amyloid-induced cytotoxicity in human neuroblastoma cell line. Benserazide hydrochloride and LD both can act as efficient inhibitors of the formation of cytotoxic HSA aggregates, and the inhibitory effects are more pronounced when both of these drugs are added simultaneously[3]. Under dopaminergic nigrostriatal denervation, treatment with L-DOPA/BE ameliorated colonic motility through a normalization of myenteric cholinergic neurotransmission, along with an improvement of colonic inflammation[4].
Benserazide HCI/盐酸苄丝肼 细胞实验
Cell Line
Concentration
Treated Time
Description
References
LoVo
3 μM, 10 μM, 30 μM, 100 μM
48 hours
Did not inhibit LoVo cell proliferation
Pharmacol Res. 2016 Nov;113(Pt A):18-37.
HT29
3 μM, 10 μM, 30 μM, 100 μM
48 hours
Inhibited HT29 cell proliferation, cytotoxic at 100 μM
Pharmacol Res. 2016 Nov;113(Pt A):18-37.
HCT116
10 μM, 30 μM, 100 μM
48 hours
Inhibited HCT116 cell proliferation, completely at 30 μM
Pharmacol Res. 2016 Nov;113(Pt A):18-37.
Enterococcus faecalis
1.5 mM
24 hours
To evaluate the inhibitory effects of human AADC inhibitors on PEA production in En. faecalis. Benserazide significantly inhibited PEA production in En. faecalis.
Gut Microbes. 2022 Jan-Dec;14(1):2128605.
LO2 cells
0-500 μM
48 hours
Evaluate the cytotoxicity of Benserazide on LO2 cells, showing IC50 value >500 μM
J Exp Clin Cancer Res. 2017 Apr 20;36(1):58.
HCT116 cells
0-500 μM
48 hours
Evaluate the cytotoxicity of Benserazide on HCT116 cells, showing IC50 value of 181.4 ± 11.5 μM
J Exp Clin Cancer Res. 2017 Apr 20;36(1):58.
SW480 cells
0-500 μM
48 hours
Evaluate the cytotoxicity of Benserazide on SW480 cells, showing IC50 value of 143.0 ± 7.0 μM
J Exp Clin Cancer Res. 2017 Apr 20;36(1):58.
Benserazide HCI/盐酸苄丝肼 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
CB-17/SCID mice
SW480 cells xenograft model
Intraperitoneal injection
300 and 600 mg/kg
Once daily for 16 days
Evaluate the inhibitory effect of Benserazide on tumor growth, showing significant suppression at 300 and 600 mg/Kg doses, reducing tumor size and weight by 30.1% and 60.3% respectively
J Exp Clin Cancer Res. 2017 Apr 20;36(1):58.
Nude mice
Human colon cancer cell xenograft model
Subcutaneous injection
50 mg/kg/day
Once daily for the duration of the experiment
Prevented tumor growth
Pharmacol Res. 2016 Nov;113(Pt A):18-37.
Mice
Mouse pain models
Intraperitoneal (i.p.) or intracerebroventricular (i.c.v.) injection
1 mg/kg (i.p.) or 25 μg/mouse (i.c.v.)
Single administration
To investigate the effect of benserazide on L-DOPS-induced antinociception. Results showed that systemic benserazide (i.p.) did not affect the antinociceptive effect of L-DOPS, while i.c.v. benserazide significantly suppressed the antinociceptive effect of L-DOPS.
Br J Pharmacol. 1994 Feb;111(2):503-8
Mice
Parkinsonian mouse model
Subcutaneous injection
15 mg/kg
Once daily for 2 weeks
To inhibit the breakdown of L-dopa in the periphery and evaluate its effect on abnormal involuntary movements (AIMs). Results showed that AIMs developed similarly in α6(-/-) and wildtype mice with combined L-dopa and benserazide treatment, but declined to ~50% in α6(-/-) mice with continued treatment.
Neuropharmacology. 2012 Sep;63(3):450-9
Rat
Healthy rats
Intraperitoneal injection
15 mg/kg bodyweight
Single dose, PET scans performed 1 hour after injection
To evaluate the impact of peripheral aromatic L-amino acid decarboxylase (AADC) inhibition on brain uptake. Results showed that brain uptake of 3-L-[18F]FPhe was significantly increased with benserazide pretreatment, while 3-D-[18F]FPhe was unaffected.
Cancers (Basel). 2021 Nov 30;13(23):6030
Mice
6-hydroxydopamine (6-OHDA)-induced hemiparkinsonian model
Intraperitoneal injection
12 mg/kg
Once daily for 10 days
To evaluate the effect of Benserazide in combination with L-DOPA on dyskinesia in a Parkinson's disease mouse model. Results showed that Benserazide combined with L-DOPA alleviated dyskinetic symptoms.
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