Department of Respiratory Medicine, Affiliated Jiangsu Province Hospital of Traditional Chinese Medicine, Nanjing University of Traditional Chinese Medicine, Nanjing, China.
J Ethnopharmacol. 2009 Oct 29;126(1):143-8. doi: 10.1016/j.jep.2009.07.025. Epub 2009 Jul 28.
A Chinese herbal formula, Hu-qi-yin possessed an anti-pulmonary fibrosis effect. Pericarp of Citrus reticulata, one of the herbal drugs contained in this formula showed the most potent inhibitory activity on the proliferation of human embryonic lung fibroblasts (HELF). The present study was designed to clarify the active principles responsible for the activity and further explore the anti-pulmonary fibrosis effect in vivo.
The water, 75% ethanol and flavonoids-enriched extracts of Citrus reticulata were prepared and screened for their anti-proliferation activity using HELF culture system. The ethanol extract was further administered orally at doses of 100 and 200 mg/(kg day) to bleomycin (BLM)-induced pulmonary fibrosis rats. The analyses of the rat body weight, hydroxyproline levels in serum and lung, scores of alveolitis and fibrosis, as well as the expression of transforming growth factor-beta(1) (TGF-beta(1)) at the protein and the messenger ribonucleic acid (mRNA) levels in lung were performed.
The ethanol extract showed the strongest inhibitory activity on HELF proliferation. Further research using BLM-induced rat model revealed that the ethanol extract at the doses of 100 and 200 mg/(kg day) caused a marked increase of body weight at first 7 days, significantly lowered the hydroxyproline levels in lung, greatly improved the pathologic scores, as well as inhibited the overexpressions of TGF-beta(1) protein and mRNA.
The results suggest that the ethanol extract of Citrus reticulata has anti-pulmonary fibrosis effects and might have a great potential for the treatment of fibrosis of lung.
一种中药方剂“黄芪饮”具有抗肺纤维化作用。该方剂中的草药之一——陈皮，对人胚肺成纤维细胞（HELF）的增殖具有最强的抑制活性。本研究旨在阐明其活性的活性成分，并进一步探讨其体内抗肺纤维化作用。
制备陈皮的水提物、75%乙醇提取物和黄酮类化合物富集提取物，并在 HELF 培养体系中筛选其抗增殖活性。进一步将乙醇提取物以 100 和 200mg/（kg·天）的剂量口服给予博莱霉素（BLM）诱导的肺纤维化大鼠。分析大鼠体重、血清和肺组织羟脯氨酸水平、肺泡炎和纤维化评分以及转化生长因子-β1（TGF-β1）在肺组织中的蛋白和信使核糖核酸（mRNA）水平的表达。
乙醇提取物对 HELF 增殖的抑制活性最强。使用 BLM 诱导的大鼠模型进行的进一步研究表明，100 和 200mg/（kg·天）剂量的乙醇提取物在最初 7 天内使体重明显增加，显著降低肺羟脯氨酸水平，大大改善病理评分，并抑制 TGF-β1 蛋白和 mRNA 的过度表达。
结果表明，陈皮乙醇提取物具有抗肺纤维化作用，可能具有治疗肺纤维化的巨大潜力。
