RESUMEN
Three undescribed sesquiterpenes, designed as pichinenoid A-C (1-3), along with nine known ones (4-12) were isolated from the stems and leaves of Picrasma chinensis. The new isolates including their absolute configurations were elucidated based on extensive spectroscopic methods, single crystal X-ray diffraction, and electronic circular dichroism (ECD) experiments, as well as comparison with literature data. Structurally, compounds 1 and 2 are descending sesquiterpenes, while pichinenoid C (3) is a rare sesquiterpene bearing a 2-methylenebut-3-enoic acid moiety at the C-6 side chain. All the isolated compounds were tested for their neuroprotective effects against the H2O2-induced damage on human neuroblastoma SH-SY5Y cells, and most of them showed moderate neuroprotective activity. Especially, compounds 1, 3-5, and 7 showed a potent neuroprotective effect at 25 or 50 µM. Moreover, the neuroprotective effects of compounds 1 and 4 were tested on a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced Parkinson's disease (PD) mouse model. Results of western blot and immunofluorescence indicated that compound 4 significantly counteract the toxicity of MPTP, and reversed the expression of tyrosine hydroxylase (TH) in substantia nigra (SN) and striatum (ST) of the mouse brain. Interestingly, western blot data suggested compound 4 also enhanced B-cell lymphoma-2 (Bcl-2) and heme oxygenase 1 (HO-1) expressions in the brain tissues from MPTP damaged mouse.
Asunto(s)
Fármacos Neuroprotectores , Picrasma , Hojas de la Planta , Tallos de la Planta , Sesquiterpenos , Animales , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/aislamiento & purificación , Sesquiterpenos/farmacología , Sesquiterpenos/aislamiento & purificación , Ratones , Humanos , Línea Celular Tumoral , Estructura Molecular , Picrasma/química , Tallos de la Planta/química , Hojas de la Planta/química , Masculino , Hemo-Oxigenasa 1/metabolismo , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , China , Fitoquímicos/farmacología , Fitoquímicos/aislamiento & purificación , 1-Metil-4-fenil-1,2,3,6-Tetrahidropiridina , Ratones Endogámicos C57BLRESUMEN
OBJECTIVE: To observe the therapeutic effect of Qilin Pills combined with bromocriptine on idiopathic hyperprolactinemic (HPRL) oligoasthenospermia. METHODS: We conducted a randomized controlled study on 40 cases of idiopathic HPRL oligoasthenospermia, who were equally assigned to a trial group and a control group to be treated with Qilin Pills (6 g tid) combined with bromocriptine and bromocriptine alone, respectively, both for a course of 12 weeks. Then we observed the changes in the semen volume, sperm concentration, sperm motility and the levels of serum prolactin and testosterone, and compared the therapeutic results between the two groups before and after medication. RESULTS: Compared with the parameters before medication, both the trial and the control group showed significant improvement after treatment in sperm concentration ([11.60 +/- 3.90] x 10(6)/ml vs [28.10 +/- 13.50] x 10(6)/ml and [12.03 +/- 4.10] x 10(6)/ml vs [18.85 +/- 8.50] x 10(6)/ml), the percentage of grade a sperm ([8.75 +/- 6.65]% vs [24.35 +/- 13.25 ]% and [8.70 +/- 6.70] % vs [19.65 +/- 10.05]%), the percentage of grade a + b sperm ( [28.45 +/- 11.35]% vs [45.80 +/- 16.55]% and [27.65 +/- 10.65]% vs [35.66 +/-13.25]%), and sperm motility ([38.22 +/- 16.35]% vs [60.05 +/- 20.65]% and [37.25 +/- 15.75 ]% vs [52.65 +/- 18.25 ]%) (all P<0.01). No significant differences were found in semen volume (P>0.05). The serum prolactin levels were significantly decreased in the trial and control groups ([152.00 +/- 22.32] and [160.45 +/- 26.65] mIU/L), as compared with premedication ([482.25 +/- 65.32] and [477.32 +/- 60.25] mIU/L) (P<0.01), while the serum testosterone levels were remarkably higher ([16.35 +/- 5.52] and [11.15 +/- 4.65] nmol/L) than before treatment ([3.75 +/- 1.10] and [4.05 +/- 1.30] nmol/L) (P<0.01). There were no statistically significant differences in the serum prolactin and testosterone levels between the two groups after treatment (P>0.05). CONCLUSION: Qilin Pills combined with bromocriptine have a significantly better efficacy than bromocriptine alone in the treatment of idiopathic HPRL oligoasthenospermia.