Pharmacognosy Department, Faculty of Pharmacy, Misr University for Science & Technology (MUST), 6th October City, Egypt.
Chemistry of Tannins Department, National Research Center, Dokki, Cairo, 12622, Egypt.
J Pharm Biomed Anal. 2021 Feb 5;194:113804. doi: 10.1016/j.jpba.2020.113804. Epub 2020 Nov 26.
Plants of the genus Pulicaria (family: Asteraceae) are widely used in central Asia and the Middle East for treatment of different human diseases. Ultra performance liquid chromatography coupled to high resolution mass spectrometry (UPLC/MS) was utilized to establish the metabolic profiles of two Pulicaria species: P. crispa and P. incisa. 122 metabolites were identified including flavonoids (37), phenolic acids (22), sesquiterpenes (17), diterpenes (7), and fatty acids (27), with enrichment in methoxylated flavonoids (20), caffeoylquinic acid conjugates (14) xanthane sesquiterpenes (9) and hydroxylated fatty acids (20) in both Pulicaria species. The metabolite profile of P. incisa was characterized by the presence of tri- and tetra-methoxylated flavonoids while xanthane sesquiterpenes were the main chemical markers of P. crispa. Additionally, a novel sesquiterpene acid (dihydropulicaric acid) was annotated in both species based on its MS fragments. Antioxidant activity for P. crispa and P. incisa methanol extracts was assessed in vitro based on DPPH and ABTS assays and further in vivo using chlorpromazine intoxicated rat model. Results revealed that P. incisa extract was more effective in inhibiting both DPPH and ABTS free radicals (IC 0.36 and 0.52 mg/mL, respectively) than P. crispa (IC 0.51 and 0.73 mg/mL). In the animal model, antioxidant activity of P. incisa (20 mg/kg/day) was also slightly higher causing a 55 % reduction in MDA levels and 65 % increase in GSH activity compared to untreated animals. Furthermore, both extracts showed a hepatoprotective effect as revealed by improvement in levels of serum biomarkers of liver functions: total bilirubin, alanine transaminase (ALT) and aspartate transaminase (AST) comparable to silymarin at 25 mg/kg/day. These findings were also supported by the preserved integrity of the hepatic tissues of animals receiving either extracts at a dose of 20 mg/kg b.wt. The present study reveals for the potential antioxidant and hepatoprotective effects for Pulicaria in relation to its bioactive metabolites.
属植物的 Pulicaria （菊科）在中亚和中东地区被广泛用于治疗不同的人类疾病。超高效液相色谱与高分辨质谱联用（UPLC/MS）被用于建立两个 Pulicaria 物种的代谢图谱：P. crispa 和 P. incisa。鉴定出 122 种代谢产物，包括黄酮类化合物（37）、酚酸（22）、倍半萜（17）、二萜（7）和脂肪酸（27），其中富含甲氧基化黄酮类化合物（20）、咖啡酰奎宁酸衍生物（14）、大戟烷倍半萜（9）和羟基化脂肪酸（20）。P. incisa 的代谢产物图谱的特点是存在三甲基和四甲基化的黄酮类化合物，而大戟烷倍半萜则是 P. crispa 的主要化学标志物。此外，根据其 MS 片段，在两个物种中都注释了一种新的倍半萜酸（二氢 pulicaric 酸）。基于 DPPH 和 ABTS 测定，评估了 P. crispa 和 P. incisa 甲醇提取物的体外抗氧化活性，并进一步在氯丙嗪中毒大鼠模型中进行了体内评估。结果表明，P. incisa 提取物在抑制 DPPH 和 ABTS 自由基方面比 P. crispa 更有效（IC 0.36 和 0.52 mg/mL）。在动物模型中，P. incisa（20 mg/kg/天）的抗氧化活性也略高，与未处理的动物相比，MDA 水平降低了 55%，GSH 活性增加了 65%。此外，两种提取物都表现出肝保护作用，表现为改善肝功能血清生物标志物的水平：总胆红素、丙氨酸转氨酶（ALT）和天冬氨酸转氨酶（AST）与 25 mg/kg/天的水飞蓟素相当。这一发现也得到了以下事实的支持：在 20 mg/kg 体重剂量下，两种提取物都能保持动物肝组织的完整性。本研究揭示了 Pulicaria 与其生物活性代谢物的潜在抗氧化和肝保护作用。
