11 November 2024 : Review article
Comprehensive Insights into Arecoline Hydrobromide: Pharmacology, Toxicity, and Pharmacokinetics
Wuyou Gao1ABDEF, Yujia He1BEF, Yuping Zhang1EF, Minghao Sun1DF, Yanping Sun1ABDEFG*DOI: 10.12659/MSM.945582
Med Sci Monit 2024; 30:e945582
Table 1 Summary of biological activities of arecoline hydrobromide.
| Pharmacological effects | Types | Cell lines/model | Doses | Effects/mechanisms | Reference |
|---|---|---|---|---|---|
| Acaricidal activity | In vitro | Cattle tick | 0.1, 0.5, 1.5, 2.5, 5, 7.5, 10 and 12.5 mg/mL | Larvae numbers (↓); Tick number, egg weight, and hatching capability (↓); SOD (↓), GST (↓), NOS (↑), MAO (↓), AChE (↓) | []17 |
| In vivo | Cattle tick -infected calves | 12.5 mg/mL | Tick number (↓); Total erythrocyte count (↑), neutrophil count (↑), monocyte count (↑) | []18 | |
| Treatment of rheumatoid arthritis | In vitro | Rheumatoid arthritis fibroblast-like synoviocytes (RA-FLSs) | 0, 12.5, 25, 50, 75, and 100 μg/ml | Cell viability (↓); DNA replication (↓);CDK1, cyclin A2, and cyclin B1 (↓);Cell apoptosis (↑); Bcl-2 (↓);Cell migration and invasion abilities (↓); PI3K/AKT pathway | []1 |
| In vivo | Collagen-induced arthritis (CIA) mice | 60 mg/kg, i.p. | Joint swelling, arthritis inflammation, cartilage degradation, bone erosion (↓) | []1 | |
| Potassium channel inhibitory activity | In vitro | Human embryonic kidney (HEK) 293 cells | 1.0, 10, and 100 μmol/L | hERG K+ current (↓) | []24 |
| In vivo | Jejunum muscle cells in W/Wv | 10, 10, 10, and 10 M | Jejunum smooth muscle contraction frequency (↑) | []25 | |
| Reproductive protection | In vivo | Experimentally induced type 1 diabetic rats | 10 mg/kg, i.p. | Serum insulin (↑), blood glucose (↓);Liver glycogen content (↑);Testosterone (↑); Serum FSH and LH (↑); Recovering Leydig cell ultrastructure; Fructose and sialic acid (↑); Expression of PDX-1 and GLUT-2 (↑) | []29 |
| Protective effect of gastric ulcer | In vivo | Alcohol-induced gastric ulcer rat model, acetic acid-induced gastric ulcer rat model | 4.41, 8.82 and 17.64 mg/kg, i.g. | Free acid, total acid, and activity of pepsin in stomach (↓);Ulcer index (↓) | []35 |
| In vivo | Stress gastric ulcer mouse model | 9, 18 and 36 mg/kg, i.g. | Ulcer index (↓) | []35 | |
| Regulation of CYP2B expression | In vivo | Wistar rats | 4, 20 and 100 mg/kg, i.g. | mRNA expression of hepatic CYP2B1 (↑), activity of hepatic CYP2B1/2 (↑);Protein content of hepatic endonuclear CAR (↑) | []39 |
| Regulation of mRNA expression of hepatorenal transporters | In vivo | Wistar rats | 0.8, 4 and 20 mg/kg, i.g. | mRNA expression of hepatic OCT2, OAT2, OCTN2, OATP1A1, OATP1A4, OATP2B1, MRP2, and MDR1A, and renal MRP2, BCRP, and MDR1A (↓);mRNA expression of renal OCTN2, OATP1A1, OATP1A4, and MRP5 (↑) | []41 |
| ↑ – improve or promote; ↓ – inhibit or reduce. | |||||