Northeast Biotechnology Network - Ph.D. Program, Federal University of Ceará, Brazil.
School of Dentistry, Federal University of Ceará, Sobral, Ceará, Brazil.
Arch Oral Biol. 2020 Sep;117:104816. doi: 10.1016/j.archoralbio.2020.104816. Epub 2020 Jun 10.
Many species of theBauhinia genus have been widely used in folk medicine as analgesic, anti-inflammatory and antioxidant agents. (-)-Fisetinidol palmitate is a semi-syntetic flavonoid obtained from the ethanolic extract of the stem of Bauhinia pulchella. This study aimed to evaluate the antiresorptive effect of the semi-syntetic (-)-fisetinidol palmitate in ligature-induced periodontitis in rats. Also, it evaluated the mechanism of action of (-)-fisetinidol palmitate and its toxicity.
Periodontitis was inducedvia a nylon thread ligature (3.0) around the second upper left molars. Rats were treated (oral gavage) once a day for 11 days with (-)-fisetinidol palmitate (0.01 or 0.1 mg/kg) or saline vehicle.
(-)-Fisetinidol palmitate (0.1 mg/kg) reduced alveolar bone loss, increased bone alkaline phosphatase (BALP), superoxide dismutase (SOD), and catalase (CAT) activity; also, it decreased IL1-β, IL-8/CINC-1, nitrite/nitrate levels and myeloperoxidase activity. (-)-Fisetinidol palmitate reduced the mRNA levels of IL1-β, IL-6, RANK, and RANK-L, while it increased the OPG ones. No statistical differences (P > 0.05) were observed in the transaminases (ALT, AST) and Total Alkaline Phosphatase (TALP) levels among groups.
(-)- CONCLUSIONS: Fisetinidol palmitate did not result in any signs of toxicity and had anti-resorptive effects in a pre-clinical trial of periodontitis, showing antioxidant activity with the involvement of the RANK/RANKL/OPG pathway.
许多猪腰豆属物种在民间医学中被广泛用作镇痛药、消炎药和抗氧化剂。(-)-非瑟酮醇棕榈酸酯是一种半合成类黄酮,从猪腰豆茎的乙醇提取物中获得。本研究旨在评估半合成(-)-非瑟酮醇棕榈酸酯在结扎诱导的大鼠牙周炎中的抗吸收作用。此外,还评估了(-)-非瑟酮醇棕榈酸酯的作用机制及其毒性。
通过将尼龙线(3.0)结扎在第二左上磨牙周围来诱导牙周炎。大鼠每天用(-)-非瑟酮醇棕榈酸酯(0.01 或 0.1mg/kg)或生理盐水载体经口灌胃治疗 11 天。
(-)-非瑟酮醇棕榈酸酯(0.1mg/kg)减少牙槽骨丧失,增加骨碱性磷酸酶(BALP)、超氧化物歧化酶(SOD)和过氧化氢酶(CAT)活性;还降低了 IL1-β、IL-8/CINC-1、亚硝酸盐/硝酸盐水平和髓过氧化物酶活性。(-)-非瑟酮醇棕榈酸酯降低了 IL1-β、IL-6、RANK 和 RANK-L 的 mRNA 水平,而增加了 OPG 的 mRNA 水平。各组间谷丙转氨酶(ALT、AST)和总碱性磷酸酶(TALP)水平无统计学差异(P>0.05)。
(-)结论:非瑟酮醇棕榈酸酯在牙周炎的临床前试验中没有导致任何毒性迹象,具有抗吸收作用,表现出抗氧化活性,涉及 RANK/RANKL/OPG 途径。