Guangdong Provincial Academy of Chinese Medical Sciences, Guangdong Provincial Traditional Chinese Medicine Hospital, Guangzhou University of Traditional Chinese Medicine, Neihuanxi Road, University Town, Guangzhou, 510006 Guangdong Province, China.
J Ethnopharmacol. 2010 Mar 24;128(2):433-7. doi: 10.1016/j.jep.2010.01.032. Epub 2010 Jan 18.
Zhuling, sclerotia of Polyporus umbellatus FRIES, a Traditional Chinese Medicine, has long been used as a diuretic. The aim of the present study was to evaluate the diuretic effect on the urinary electrolyte concentration (Na(+), K(+), and Cl(-)) and regulation of the relative mRNA expression of aquaporin-1 (AQP1), aquaporin-2 (AQP2), aquaporin-3 (AQP3) and vasopressin V(2) receptor (V(2)R) post-oral administration of sclerotia of Polyporus umbellata aqueous extract in normal rats.
Aqueous extract of sclerotia of Polyporus umbellatus (50 mg/kg, 250 mg/kg, 500 mg/kg) or the reference drug, furosemide (10mg/kg) were administrated orally to male SD rats and their urine output was quantified and collected 24h and 8 days after the treatment. The kidney medulla AQP1, AQP2, AQP3 and V(2)R mRNA relative expressions were measured with RT-PCR.
After single dose of the exact of sclerotia of Polyporus umbellata, urine output was found to be significantly increased, which began at 4h, and at 24h after the treatment, the sclerotia of Polyporus umbellatus extract and furosemide treatment produced the similar total volume of urine excreted. The extract increases urinary levels of Na(+), K(+), and Cl(-), to about the same extent, while furosemide increased urinary levels of Na(+) and Cl(-). After the 8-day doses, all two substances induced significant diuresis, natriuresis and chloriuresis. These two substances do not regulate the AQP1 and AQP3 mRNA level in normal rat kidney medulla. The AQP2 mRNA level of sclerotia of Polyporus umbellata extract was down-regulated significantly, the V(2)R mRNA level of sclerotia of Polyporus umbellata extract 50mg/kg dose group and 250 mg/kg dose group were down-regulated significantly too. Interestingly, the low-dose group had higher effect on regulation of AQP2 and V(2)R mRNA level.
Aqueous extract of sclerotia of Polyporus umbellatus has conspicuous diuretic effect confirming its ethnopharmacological use. From the pattern of excretion of water, sodium, potassium, chlorine, AQP2 and V2R mRNA level, it may be logically concluded that it has effect from down-regulating AQP2, and down-regulate AQP2 by down-regulating V(2)R.
灵芝,多孔菌科真菌茯苓的菌核,是一种传统中药,一直被用作利尿剂。本研究的目的是评估口服茯苓水提物对正常大鼠尿电解质浓度(Na(+)、K(+)和 Cl(-))和水通道蛋白 1(AQP1)、水通道蛋白 2(AQP2)、水通道蛋白 3(AQP3)和血管加压素 V2 受体(V2R)相对 mRNA 表达的利尿作用。
口服茯苓水提物(50mg/kg、250mg/kg、500mg/kg)或参比药物呋塞米(10mg/kg),雄性 SD 大鼠给药 24 小时和 8 天后,定量收集尿液并收集尿液。采用 RT-PCR 法测定肾髓质 AQP1、AQP2、AQP3 和 V2R mRNA 的相对表达。
单次给药后,发现茯苓水提物可显著增加尿量,4 小时开始,24 小时后,茯苓水提物和呋塞米处理产生相似的总尿量。该提取物增加尿中 Na(+)、K(+)和 Cl(-)的水平,程度相似,而呋塞米增加尿中 Na(+)和 Cl(-)的水平。8 天剂量后,两种物质均诱导显著利尿、排钠和排氯。这两种物质均不调节正常大鼠肾髓质 AQP1 和 AQP3 mRNA 水平。茯苓水提物显著下调 AQP2 mRNA 水平,茯苓水提物 50mg/kg 剂量组和 250mg/kg 剂量组 V2R mRNA 水平也显著下调。有趣的是,低剂量组对 AQP2 和 V2R mRNA 水平的调节作用更高。
茯苓水提物具有明显的利尿作用,证实了其在民族药理学中的应用。从水、钠、钾、氯、AQP2 和 V2R mRNA 水平的排泄模式可以合理地推断,它通过下调 AQP2 起作用,并通过下调 V2R 来下调 AQP2。