Abstract
This study evaluated the anti-ascites effect of total diterpenoids extracted from Euphorbiae ebracteolatae Radix (TDEE) on malignant ascitic mice and elucidated its underlying mechanism. TDEE was extracted by dichloromethane and subjected to column chromatography. The purity of six diterpenoids isolated from TDEE was determined to be 77.18% by HPLC. TDEE (3 and 0.6 g raw herbs/kg, p.o.) reduced ascites and increased urine output. Meanwhile, analysis of tumor cell viability, cycle and apoptosis indicated that TDEE had no antitumor activity. In addition, the expression levels of aquaporins (AQPs) and the membrane translocation levels of protein kinase C (PKC) α and PKCβ in kidney and cells were measured. TDEE reduced the levels of AQP1–4, and inhibited PKCβ expression in membrane fraction. Four main diterpenoids, except compound 2, reduced AQP1 level in human kidney-2 cells. Compounds 4 and 5 inhibited AQP2–4 expression in murine inner medullary collecting duct cells. The diterpenoid-induced inhibition of AQP1–4 expression was blocked by phorbol-12-myristate-13-acetate (PMA; agonist of PKC). The diterpenoids from TDEE are the main anti-ascites components. The anti-ascites effect of diterpenoids may be associated with alterations in AQPs in the kidneys to promote diuresis. The inhibition of AQP1–4 expression by TDEE is related to the inhibition of PKCβ activation.
Highlights
Euphorbia ebracteolata Hayata (EEH) is a member of the genus Euphorbia in the familyEuphorbiaceae and is widely used in the treatment of abdominal distension and edema, parasitic infection, tuberculosis, and other diseases in traditional Chinese medicine (TCM) [1]
Treatment of ascitic mice with total extract of EER (TEER) and total diterpenoids from EER (TDEE) (3 and 0.6 g raw herbs/kg, p.o.) and furosemide significantly reduced the increase in ascitic fluid weight compared to the model group (Figure 1A)
In the TEER and TDEE groups at dose of 3 g raw herbs/kg, a significant increase in fecal water content was observed compared with the model group (Figure 1D)
Summary
Euphorbiaceae and is widely used in the treatment of abdominal distension and edema, parasitic infection, tuberculosis, and other diseases in traditional Chinese medicine (TCM) [1]. The root of EEH (EER) contains various terpenoids, which are considered to be effective components. Recent studies on terpenoids have been conducted to determine their antiinflammatory, antiviral, anti-tuberculosis, and other effects in vitro [2,3,4,5]. Basic research investigations on the traditional effects of EER in the treatment of abdominal distension and edema are limited. According to theory of TCM, EER can rapidly eliminate abdominal distension and edema by promoting urination and diarrhea [6]. Our previous studies have shown that total diterpenoids from EER (TDEE) can cause diarrhea by regulating the expression of aquaporin (AQP)-1 and AQP3 [7]. To date, the effective substances of anti-ascites in EER remain unclear
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