PDF(Pubmed)
Abstract：
Labdanum resin or \"gum\" can be obtained from Cistus ladanifer L. by two different extraction methods: the Zamorean and the Andalusian processes. Although its main use is in the fragrance and perfumery sectors, ethnobotanical reports describe its use for medicinal purposes in managing hyperglycemia and mental illnesses. However, data concerning the bioactivities and pharmacological applications are scarce. In this work, it was found that the yield of labdanum resin extracted by the Andalusian process was 25-fold higher than the Zamorean one. Both resins were purified as absolutes, and the Andalusian absolute was purified into diterpenoid and flavonoid fractions. GC-EI-MS analysis confirmed the presence of phenylpropanoids, labdane-type diterpenoids, and methylated flavonoids, which are already described in the literature, but revealed other compounds, and showed that the different extracts presented distinct chemical profile. The potential antidiabetic activity, by inhibition of α-amylase and α-glucosidase, and the potential neuroprotective activity, by inhibition of acetylcholinesterase, were investigated. Diterpenoid fraction produced the higher α-amylase inhibitory effect (~30% and ~40% at 0.5 and 1 mg/mL, respectively). Zamorean absolute showed the highest α-glucosidase inhibitory effect (~14% and ~24%, at 0.5 and 1 mg/mL, respectively). Andalusian absolute showed the highest acetylcholinesterase inhibitory effect (~70% and ~75%, at 0.5 and 1 mg/mL, respectively). Using Caco-2 and HepG2 cell lines, Andalusian absolute and its purified fractions showed moderate cytotoxic/anti-proliferative activity at 24 h exposure (IC50 = 45-70 µg/mL, for Caco-2; IC50 = 60-80 µg/mL, for HepG2), whereas Zamorean absolute did not produce cytotoxicity (IC50 ≥ 200.00 µg/mL). Here we show, for the first time, that labdanum resin obtained by the Andalusian process, and its fractions, are composed of phytochemicals with anti-diabetic, neuroprotective and anti-proliferative potential, which are worth investigating for the pharmaceutical industry. However, toxic side-effects must also be addressed when using these products by ingestion, as done traditionally.
摘要：
Labdanum树脂或“胶”可以通过两种不同的提取方法从CistusladaniferL.获得：Zamorean和安达卢西亚工艺。虽然它的主要用途是在香料和香料行业，民族植物学报告描述了其在治疗高血糖和精神疾病中的药用用途。然而,有关生物活性和药理应用的数据很少。在这项工作中,发现通过安达卢西亚工艺提取的labdanum树脂的产率比Zamorean高25倍。两种树脂都被纯化为绝对树脂，并将安达卢西亚绝对纯化为二萜和类黄酮部分。GC-EI-MS分析证实了苯丙烷类的存在，拉布丹型二萜，和甲基化的类黄酮，文献中已经描述过，但揭示了其他化合物，并表明不同的提取物呈现不同的化学特征。潜在的抗糖尿病活性，通过抑制α-淀粉酶和α-葡萄糖苷酶，和潜在的神经保护活性，通过抑制乙酰胆碱酯酶，被调查了。二萜部分产生较高的α-淀粉酶抑制作用（0.5和1mg/mL时〜30％和〜40％，分别)。绝对Zamorean显示出最高的α-葡萄糖苷酶抑制作用（〜14％和〜24％，在0.5和1毫克/毫升，分别)。安达卢西亚绝对显示出最高的乙酰胆碱酯酶抑制作用(~70%和~75%，在0.5和1毫克/毫升，分别)。使用Caco-2和HepG2细胞系，安达卢西亚绝对及其纯化的部分在24小时暴露时显示出中等的细胞毒性/抗增殖活性（IC50=45-70µg/mL，对于Caco-2；IC50=60-80µg/mL，对于HepG2），而Zamorean绝对不会产生细胞毒性（IC50≥200.00µg/mL）。在这里我们展示，第一次,通过安达卢西亚工艺获得的拉布拉坦树脂，和它的分数，由抗糖尿病的植物化学物质组成，神经保护和抗增殖潜力，这对于制药行业来说是值得研究的。然而,通过摄入使用这些产品时，还必须解决毒副作用，传统上做的。
