Benidipine hydrochloride, a calcium channel blocker (CCB), inhibited SFTSV (Severe fever with thrombocytopenia syndrome virus) replication in vitro. Benidipine hydrochloride was revealed to inhibit virus infection through impairing virus internalization and genome replication[3]. Histopathologically neuroprotective effects of benidipine hydrochloride was seen in the cerebral cortex tissues. Benidipine hydrochloride can play a certain protective role in the cerebral I/R injury. The protective effect of this agent may be related to the improvement on the antioxidant capacity of brain tissue and the inhibition of overproduction of inflammatory cytokines[4]. Moreover, patients with hypertension have high plasma TBARS (thiobarbituric acid reactive substance), and benidipine hydrochloride decreases not only blood pressure but also oxidative stress in the clinical practice[5]. Benidipine has a more potent antihypertensive effect than cilnidipine and also a renoprotective effect, indicating the high usefulness of benidipine in hypertensive patients with diabetes[6]. Combination therapy with benidipine hydrochloride and candesartan cilexetil may contribute to the suppression of arteriosclerosis and may be useful for elderly hypertensive patients with diabetes mellitus[7].
Benidipine HCl/贝尼地平盐酸盐 细胞实验
Cell Line
Concentration
Treated Time
Description
References
GE1 cells
1, 10, 100, 1000, 10000 nM
12 hours
Promoted GE1 cell proliferation
Adv Wound Care (New Rochelle). 2019 Mar 1;8(3):108-117.
MC3T3-E1 cells
0.01, 0.10, 1.00 µM
21 days
To evaluate the effect of Benidipine on matrix mineralization in MC3T3-E1 cells, results showed that Benidipine significantly promoted extracellular matrix mineralization.
J Zhejiang Univ Sci B. 2021 May 15;22(5):410-420.
MLO-Y4 cells
0.1, 1, 10, 100, 1000, 10000 nM
24 hours
Promoted MLO-Y4 cell proliferation
Adv Wound Care (New Rochelle). 2019 Mar 1;8(3):108-117.
Huh7 cells
10 µM
24 hours
Benidipine HCl significantly inhibited HTNV replication in Huh7 cells
Front Pharmacol. 2022 Aug 29;13:940178.
A549 cells
6.552 µM
24 hours
Benidipine HCl significantly inhibited HTNV replication in A549 cells with an IC50 of 6.552 μM
Front Pharmacol. 2022 Aug 29;13:940178.
Rat aortic endothelial cells
10 nM
30 minutes
To investigate the effects of benidipine on LPC-induced suppression of [Ca2+]i increase in endothelial cells, results showed that benidipine inhibited LPC-induced suppression of [Ca2+]i increase
J Biomed Sci. 2009 Jun 26;16(1):57.
Vero cells
10 µM
36 hours
Benidipine hydrochloride showed the strongest inhibitory effect on SFTSV infection (>90%) at the concentration of 10 μM.
Cell Res. 2019 Sep;29(9):739-753.
HEK293T cells
1 µM
40 minutes
To investigate the inhibitory mechanism of Benidipine on CaV1.2 channels, cryo-EM structural analysis revealed that Benidipine is located in the DIII-DIV fenestration site, and its hydrophobic sidechain provides additional interactions with the channel subunit α1, supporting its inhibitory effects on both L-type and T-type voltage-gated calcium channels
Nat Commun. 2024 Mar 30;15(1):2772.
MC3T3-E1 cells
0.01, 0.10, 1.00 µM
48 hours
To evaluate the effect of Benidipine on the proliferation of MC3T3-E1 cells, results showed that Benidipine significantly promoted cell proliferation in a dose-dependent manner.
J Zhejiang Univ Sci B. 2021 May 15;22(5):410-420.
MC3T3-E1 cells
0.01, 0.10, 1.00 µM
7, 10, 14 days
To evaluate the effect of Benidipine on alkaline phosphatase (ALP) activity in MC3T3-E1 cells, results showed that Benidipine significantly increased ALP activity, especially at 10 and 14 days.
J Zhejiang Univ Sci B. 2021 May 15;22(5):410-420.
MRC5 normal human fibroblasts
10 µM
Benidipine selectively promotes the death of cigarette smoke-induced senescent lung cells
Aging (Albany NY). 2023 Dec 12;15(23):13581-13592.
Benidipine HCl/贝尼地平盐酸盐 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Wistar rats
MRONJ-like lesion model
Local injection
0.13 mg/kg, 1.3 mg/kg
Single injection, lasting two weeks
Promote healing of MRONJ-like lesions, reduce necrotic bone area, and promote new bone formation
Pharmaceuticals (Basel). 2022 Aug 18;15(8):1020
Sprague-Dawley rats
Myocardial ischemia/reperfusion model
Intravenous injection
10 mg/kg
Single dose, 10 minutes before reperfusion
Benidipine exerts its antiapoptotic effect by inhibiting the mitochondrial-mediated apoptotic pathway (but not the death receptor-mediated pathway), reducing myocardial apoptosis. Specifically, it decreased TUNEL-positive staining (8.4±1.2% vs 15.3±1.3%), reduced caspase-3 activity (1.94±0.25 vs 3.43±0.29), and inhibited mitochondrial cytochrome c release and caspase-9 activation. Additionally, benidipine enhanced ERK1/2 activity and prolonged its activation duration but had no significant effect on p38 MAPK.
Br J Pharmacol. 2004 Jun;142(4):627-34
C57BL/6 mice
SFTSV infection model
Intragastric administration
15 mg/kg
Twice a day for 7 days
Benidipine hydrochloride and nifedipine significantly reduced viral loads in spleen and serum, and alleviated SFTSV-induced pathogenesis.
Cell Res. 2019 Sep;29(9):739-753.
Rats
Tooth extraction socket model
Local injection
15 or 45 μg/kg
Single injection, lasting 28 days
Evaluated the effect of BD on bone and gingival healing at the extraction socket. Results showed BD significantly augmented bone volume and density, and also promoted epithelial wound healing.
Adv Wound Care (New Rochelle). 2019 Mar 1;8(3):108-117.
New Zealand white rabbits
Myocardial ischemia/reperfusion model
Intravenous injection
3 mg/kg or 10 mg/kg
Single dose, observed for 4 hours and 45 minutes
To investigate the effects of benidipine on myocardial infarct size, apoptosis, necrosis, and cardiac functional recovery in rabbits subjected to myocardial ischemia/reperfusion. Results showed that 10 mg/kg benidipine significantly reduced myocardial apoptosis (6.2 ±0.8% vs 12.2 ±1.1%), necrosis, and infarct size (20 ±2.3% vs 49 ±2.6%), and improved cardiac functional recovery. 3 mg/kg benidipine, without hemodynamic effects, still significantly reduced apoptosis but failed to reduce necrosis.
Br J Pharmacol. 2001 Feb;132(4):869-78
Sprague-Dawley rats
Sprague-Dawley rats
Oral
4 mg/kg
Single dose, aortas were isolated 90 minutes after administration
To investigate the protective effects of benidipine on LPC-induced impairment of endothelium-dependent relaxation, results showed that benidipine inhibited LPC-induced endothelial dysfunction
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