Romero-Estrada Antonio, Maldonado-Magaña Amalia, González-Christen Judith, Bahena Silvia Marquina, Garduño-Ramírez María Luisa, Rodríguez-López Verónica, Alvarez Laura
Centro de Investigaciones Químicas-IICBA, Universidad Autónoma del Estado de Morelos, Avenida Universidad 1001, Chamilpa, Cuernavaca, Morelos, 62209, Mexico.
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Avenida Universidad 1001, Chamilpa, Cuernavaca, Morelos, 62209, Mexico.
BMC Complement Altern Med. 2016 Oct 26;16(1):422. doi: 10.1186/s12906-016-1397-1.
Bursera copallifera (Burseraceae) releases a resin known as "copal ancho" which has been used, since pre-Colombian times, as ceremonially burned incense and to treat tooth ache, tumors, arthritis, cold, cough, and various inflammatory conditions; however, its anti-inflammatory potential is poorly studied. The aim of the present study was to isolate, quantify, and to investigate the anti-inflammatory activity of triterpene compounds isolated from the copal resin of B. copallifera.
The constituents present in the total resin of B. copallifera were obtained by successive chromatographic procedures, and quantitative analysis was performed by High Performance Liquid Chromatography (HPLC). Anti-inflammatory effects of the isolated triterpenes were investigated to determine their inhibitory effects on phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced edema in mice, viability and nitric oxide (NO) production inhibition on lipopolysaccharide (LPS)-activated RAW 264.7 macrophages, and inhibition of cyclooxygenase (COX)-1, COX-2 and secretory Phospholipase A (sPLA) activities in vitro.
Quantitative phytochemical analysis of the copal resin showed the presence of six pentacyclic triterpenes of which, 3-epilupeol (59.75 % yield) and α-amyrin (21.1 % yield) are the most abundant. Among the isolated triterpenes, 3-epilupeol formiate (Inhibitory Concentration 50 % (IC) = 0.96 μmol), α.amyrin acetate (IC = 1.17 μmol), lupenone (IC = 1.05 μmol), and 3-epilupeol (IC = 0.83 μmol) showed marked inhibition of the edema induced by TPA in mice. α-amyrin acetate and 3-epilupeol acetate, at 70 μM, also inhibited the activity of COX-2 by 62.85 and 73.28 % respectively, while α-amyrin and 3-epilupeol were the best inhibitors of the production of NO in LPS-activated RAW 264.7 cells with IC values of 15.5 and 8.98 μM respectively, and did not affected its viability. All compounds moderately inhibited the activity of PLA.
This work supports the folk use of B. copallifera and provides the basis for future investigations about the therapeutic use of this resin in treating inflammation.
伯氏裂榄（橄榄科）会分泌一种名为“墨西哥柯巴脂”的树脂，自前哥伦布时代以来，它就被用作仪式焚香，还用于治疗牙痛、肿瘤、关节炎、感冒、咳嗽及各种炎症；然而，其抗炎潜力的研究较少。本研究的目的是从伯氏裂榄的柯巴脂中分离、定量并研究三萜类化合物的抗炎活性。
通过连续色谱法获得伯氏裂榄总树脂中的成分，并用高效液相色谱法（HPLC）进行定量分析。研究分离出的三萜类化合物的抗炎作用，以确定它们对佛波酯12 - O -十四酰佛波醇-13 -乙酸酯（TPA）诱导的小鼠水肿的抑制作用、对脂多糖（LPS）激活的RAW 264.7巨噬细胞活力和一氧化氮（NO）产生的抑制作用，以及在体外对环氧合酶（COX）-1、COX - 2和分泌型磷脂酶A（sPLA）活性的抑制作用。
对柯巴脂进行的植物化学定量分析表明，其中存在六种五环三萜，其中3 -表羽扇豆醇（产率59.75%）和α-香树脂醇（产率21.1%）含量最高。在分离出的三萜类化合物中，甲酸3 -表羽扇豆酯（半数抑制浓度（IC）= 0.96 μmol）、乙酸α-香树脂酯（IC = 1.17 μmol）、羽扇豆酮（IC = 1.05 μmol）和3 -表羽扇豆醇（IC = 0.83 μmol）对TPA诱导的小鼠水肿有显著抑制作用。乙酸α-香树脂酯和乙酸3 -表羽扇豆酯在70 μM时，对COX - 2活性的抑制率分别为62.85%和73.28%，而α-香树脂醇和3 -表羽扇豆醇是LPS激活的RAW 264.7细胞中NO产生的最佳抑制剂，IC值分别为15.5和8.98 μM，且不影响其活力。所有化合物均适度抑制了PLA的活性。
本研究支持了伯氏裂榄在民间的用途，并为该树脂在治疗炎症方面的治疗用途的未来研究提供了依据。
