Canh Pham Em, Van Doan Vien, Le Thi Tuong Vi, Van Ngo Cuong, Vo Van Lenh
Faculty of Pharmacy, Hong Bang International University, 700000, Ho Chi Minh City, Viet Nam.
Faculty of Pharmacy, Lac Hong University, 810000, Dong Nai Province, Viet Nam.
Heliyon. 2024 Sep 29;10(19):e38634. doi: 10.1016/j.heliyon.2024.e38634. eCollection 2024 Oct 15.
(VA) leaves contain many potential active ingredients and exhibit diverse pharmacological activities. The antihypertensive, anti-inflammatory, and analgesic effects of VA crude and fraction extracts were carried out using Swiss albino mice models. VAE is considered safe to be administered due to LD being greater than 10,000 mg/kg body weight. A dose-dependent increase in antihypertensive, anti-inflammatory, and analgesic activities was observed in both VAE and fractions, similar to the reference drugs. The antihypertensive effect of the VAE 2.0 (2000 mg/kg, SBP: ↓26.05 %, DBP: ↓34.51 %) was nearly equivalent to Captopril (100 mg/kg, SBP: ↓30.28 %, DBP: ↓40.71 %) with no statistically significant difference (p > 0.05). The VAE 1.0 (1000 mg/kg), and EA 30 (30 mg/kg) showed potent anti-inflammatory activity when reducing the total edematous paw volume significantly (p < 0.01) by ↓65.58 %, and ↓69.34 %, respectively, similar to Ibuprofen (7.5 mg/kg, ↓67.03 %). Besides, VAE (>500 mg/kg), and W 400 (water, 400 mg/kg) fraction extracts showed a potent analgesic effect equivalent to Para 50 (paracetamol 50 mg/kg) for the highest protection (>65 %) against the acetic acid-induced writhing after 35 min. Moreover, cepharanthine, cynaroside, and vernoniosides of VA leaf extract exhibited the highest affinity (>10 kcal/mol) in anti-inflammatory and analgesic targets (iNOS and COX-2) and antihypertensive targets (ACE and β adrenoreceptor). Therefore, the crude and fraction extracts of VA leaves from the percolation method and bioactive metabolites are a potential source that can be developed into antihypertensive, anti-inflammatory, and analgesic agents in herbal medicine.
长春花（VA）叶含有许多潜在的活性成分，并具有多种药理活性。使用瑞士白化小鼠模型对VA粗提物和馏分提取物的降压、抗炎和镇痛作用进行了研究。由于半数致死量大于10000mg/kg体重，长春花提取物（VAE）被认为给药安全。在VAE及其馏分中均观察到降压、抗炎和镇痛活性呈剂量依赖性增加，与参比药物相似。VAE 2.0（2000mg/kg，收缩压：下降26.05%，舒张压：下降34.51%）的降压效果与卡托普利（100mg/kg，收缩压：下降30.28%，舒张压：下降40.71%）几乎相当，无统计学显著差异（p>0.05）。VAE 1.0（1000mg/kg）和乙醇提取物30（30mg/kg）在显著降低足爪总水肿体积（p<0.01）时分别下降65.58%和69.34%，显示出较强的抗炎活性，与布洛芬（7.5mg/kg，下降67.03%）相似。此外，VAE（>500mg/kg）和水提取物400（水，400mg/kg）馏分提取物在35分钟后对乙酸诱导的扭体表现出与对乙酰氨基酚50（对乙酰氨基酚50mg/kg）相当的强效镇痛作用，最高保护率（>65%）。此外，长春花叶提取物中的粉防己碱、木犀草苷和斑鸠菊苷在抗炎和镇痛靶点（诱导型一氧化氮合酶和环氧化酶-2）以及降压靶点（血管紧张素转换酶和β肾上腺素受体）中表现出最高亲和力（>10kcal/mol）。因此，通过渗漉法得到的长春花叶粗提物和馏分提取物以及生物活性代谢物是一种有潜力的来源，可开发成草药中的降压、抗炎和镇痛剂。
