ABSTRACT
The constituents from 95% ethanol extract of the roots of Stelleropsis tianschanica were purified by column chromatography techniques, leading to the isolation of 17 compounds. Their structures were elucidated by spectroscopic dataas 5'-methoxy lariciresinol(1), pinoresinol(2), daphnoretin(3), acutissimalignan B(4),(+)-secoisolariciresinol(5),(+)-epipinoresinol(6), 7-methyi-daphnoretin(7), thero-8S-7-methoxysyringylglycerol(8), 1-O-methyl-guaiacylglycerol(9), 2R-22'-ferulic acid ester-2,3-dihydroxypropyl ester(10), vesiculosin(11), 4β,5βH-guai-9,7(11)-dien-12,8-olide-1α,8α-diol(12),(-)-nortrachelogenin(13), 4α,5βH-guai-9,7(11)-dien-12,8-olide-1α,8α-diol(14), matairesinol(15), lariciresinol(16)and isolariciresinol(17). Among them, compounds 1-13 wereobtained for the first time fromthe genus Stelleropsis. Compounds 3, 7, 10-14 were tested for their activation of orphan nuclear receptor TR3 with the immunofluorescence technology in 50 μmol•L⁻¹. The results showed that compound 10 displayed moderate activity with the activity ratio of 76.38%, and the others were only about 50.0%.
ABSTRACT
ObjectiveTo compare of the thickness of left ventricular wall of Ang Ⅱ induced cardiac hypertrophy model in both TR3 konock-out C57BL/6 mice (TR3-/- mice) and wild type C57BL/6 mice (TR3+/+ mice) by high frequency ultrasound,combined with experimental research to discuss if TR3 take part in the process of cardiac hypertrophy.Methods26 TR3 -/- mice and 33 TR3 +/+ mice were randomized to 2 groups respectively:TR3+/+ + AngⅡ group (27 mice),TR3+/+ + PBS group(6 mice),TR3-/- + Ang Ⅱ group(20 mice),TR3-/- + PBS group(6 mice).Micro-pumps with AngⅡ or PBS were placed into the subcutaneous tissue of mice to construct hypertension model in 4 weeks.Interventricular septum enddiastolic thickness (IVSd) and left ventricular posterior wall end-diastolic thickness (LVPWd) were measured by echocardiography 2 days before operation and every week after operation until 4 weeks.Then,mice were killed and mice cardiomyocytes were isolated and detected in lab (HE dyeing test,Western blotting).Results①Echocardiography:before operation,IVSd and LVPWd was not statistically different between TR3+/+ group and TR3-/- group( P ＞0.05).1 - 2 weeks after operation,IVSd and LVPWd had peaked in both TR3-/- + Ang Ⅱ group and TR3 +/+ + Ang Ⅱ group,IVSd and LVPWd in TR3 +/+ + Ang Ⅱgroup were significantly thicker than control group (TR3 +/+ + PBS group) ( P ＜0.05),IVSd and LVPWd in TR3-/-+ AngⅡ group were slightly thicker than control group (TR3-/- + PBS group) ( P ＜0.05).Compared with TR3-/- + Ang Ⅱ group,IVSd and LVPWd in TR3+/+ + Ang Ⅱ group were markedly increased( P ＜0.05).After 4 weeks operation,IVSd and LVPWd of all 4 groups were not statistically different than that in the 2nd week.②HE dyeing test:The cell size of cardiomyocytes in TR3+/+ mice increased significantly after Ang Ⅱ treatment,while TR3-/- mice did not.③ Western blotting:Ang Ⅱ promoted TR3 expressions in TR3 +/+ mice( P ＜0.05).ConclusionsTR3 do take part in the process of Ang Ⅱ induced cardiac hypertrophy in mice and it is a key factor in this process.
ABSTRACT
OBJECTIVE: The present study examined the gonadotropin regulation of TR3 gene expression by luteinizing hormone (LH) in cultured human luteinized granulosa cells. METHODS: TR3 mRNA levels were detected by competitive reverse transcriptase-polymerase chain reaction (RT-PCR) method in cultured human luteinized granulosa cells collected from patients undergoing in vitro fertilization. RESULTS: TR3 transcript was transiently induced by LH, reaching maximum levels 1 hr after stimulation, in a dose-dependent manner. LH-stimulated TR3 expression was abolished by actinomycin D, but was superinduced by cycloheximide. Treatment of luteinized granulosa cells with Rp-cAMP, an inhibitor of protein kinase A, as well as, chelerythrin, an inhibitor of protein kinase C, suppressed LH-stimulated TR3 mRNA levels. In addition, forskolin and TPA mimicked the LH action on the induction of TR3 gene, implying the role of protein kinase A and C activation. CONCLUSION: Taken together, the present study demonstrates that TR3 gene was rapidly and transiently induced by LH in human luteinized granulosa cells. The results imply that TR3 may play a role in ovulation by initiating a cascade of ovulation-specific gene expression in response to LH.