Centro Química e Bioquímica, Faculdade de Ciências da Universidade de Lisboa, Edifício C8, Campo Grande, 1749-016 Lisboa, Portugal.
J Ethnopharmacol. 2013 Nov 25;150(2):718-23. doi: 10.1016/j.jep.2013.09.029. Epub 2013 Oct 3.
Decoctions of the leaves of Annona cherimola Mill. are traditionally used in Azores to treat hypercholesterolemia. Although they are sold and consumed by people in order to improve their health, these are products that cannot be sold with claims for health benefits as they have never been studied scientifically.
The activities of decoctions from Annona cherimola leaves were analysed for the two therapeutic approaches currently used to reduce plasma cholesterol: inhibition of dietary cholesterol uptake and inhibition of HMG-CoA reductase activity. Furthermore, the composition of the decoction was elucidated by LC-MS and the permeability of the active components was analysed using Caco-2 cell monolayers as a model of the intestinal barrier (dietary cholesterol uptake).
The chemical composition of the Annona cherimola leaves' extract revealed that rutin was its main component. The in vitro gastrointestinal digestion did not modify the chemical composition of the extract. This extract was able to originate a slight reduction in cholesterol absorption through Caco-2 cells lines and to reduce the HMG-CoA reductase activity in 50% when using 137.3 μg of the extract/mL. Rutin, when used in the same concentration as that found in the extract, was able to reduce cholesterol absorption through Caco-2 cells monolayer in approximately 47%. This flavonoid had an IC50 of 17.85 μM relatively to the HMG-CoA reductase activity.
The traditional use of decoctions from the leaves of Annona cherimola may be justified, at least by the inhibition of HMG-CoA reductase activity.
安农西亚梨树叶的煎剂传统上被用于治疗高胆固醇血症。尽管这些煎剂被出售并被人们消费，以改善他们的健康，但这些产品不能声称具有健康益处，因为它们从未经过科学研究。
分析安农西亚梨树叶煎剂的活性，用于目前用于降低血浆胆固醇的两种治疗方法：抑制饮食胆固醇吸收和抑制 HMG-CoA 还原酶活性。此外，通过 LC-MS 阐明了煎剂的组成，并使用 Caco-2 细胞单层作为肠道屏障（饮食胆固醇吸收）的模型分析了活性成分的通透性。
安农西亚梨树叶提取物的化学成分表明芦丁是其主要成分。体外胃肠道消化并未改变提取物的化学成分。这种提取物能够通过 Caco-2 细胞系轻微减少胆固醇的吸收，并在使用 137.3μg/mL 提取物时将 HMG-CoA 还原酶活性降低 50%。芦丁在与提取物中相同的浓度下使用时，能够通过 Caco-2 细胞单层减少约 47%的胆固醇吸收。这种黄酮类化合物对 HMG-CoA 还原酶活性的 IC50 为 17.85 μM。
安农西亚梨树叶煎剂的传统用途可能是合理的，至少可以通过抑制 HMG-CoA 还原酶活性来解释。
