RESUMO
The incidence rate of diabetes in pregnancy is about 20%, and diabetes in pregnancy will have a long-term impact on the metabolic health of mothers and their offspring. Mothers may have elevated blood glucose, which may lead to blood pressure disease, kidney disease, decreased resistance and secondary infection during pregnancy. The offspring may suffer from abnormal embryonic development, intrauterine growth restriction, obesity, autism, and other adverse consequences. Resveratrol (RSV) is a natural polyphenol compound, which is found in more than 70 plant species and their products, such as Polygonum cuspidatum, seeds of grapes, peanuts, blueberries, bilberries, and cranberries. Previous studies have shown that RSV has a potential beneficial effect on complex pregnancy, including improving the indicators of diabetes and pregnancy diabetes syndrome. This article has reviewed the molecular targets and signaling pathways of RSV, including AMP-activated protein kinase, mitogen-activated protein kinases, silent information regulator sirtuin 1, miR-23a-3p, reactive oxygen species, potassium channels and CX3C chemokine ligand 1, and the effect of RSV on gestational diabetes mellitus (GDM) and its complications. RSV improves the indicators of GDM by improving glucose metabolism and insulin tolerance, regulating blood lipids and plasma adipokines, and modulating embryonic oxidative stress and apoptosis. Furthermore, RSV can ameliorate the GDM complications by reducing oxidative stress, reducing the effects on placentation, reducing the adverse effects on embryonic development, reducing offspring's healthy risk, and so on. Thus, this review is of great significance for providing more options and possibilities for further research on medication of gestational diabetes.
RESUMO
Paeonone A (1), a unique nonanortriterpenoid, and a new octanortriterpenoid, paeonone B (2), were isolated from the roots of Paeonia lactiflora, together with a known analogue, palbinone (3). Paeonone A (1) is the first example of naturally occurring nonanortriterpenoid with a diketo acid group. Extensive NMR and HRESIMS experiments were applied to identify the structures of 1 and 2, and their absolute configurations were solved by single-crystal X-ray diffraction and ECD data. Biological properties of 1-3 were explored against pancreatic lipase and cancer cell lines.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Inibidores Enzimáticos/farmacologia , Lipase/antagonistas & inibidores , Paeonia/química , Raízes de Plantas/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Lipase/metabolismo , Estrutura Molecular , Pâncreas/enzimologia , Relação Estrutura-AtividadeRESUMO
In a continuing search for potential inhibitors against human carboxylesterases 1A1 and 2A1 (hCES1A1 and hCES2A1), an EtOAc extract of the roots of Paeonia lactiflora showed strong hCES inhibition activity. Bioassay-guided fractionation led to the isolation of 26 terpenoids including 12 new ones (1-5, 7-12, and 26). Among these, sesquiterpenoids 1 and 6, monoterpenoids 10, 11, and 13-15, and triterpenoids 18-20, 22, and 24-26 contributed to the hCES2A1 inhibition, in the IC50 range of 1.9-14.5 µM, while the pentacyclic triterpenoids 18-26 were responsible for the potent inhibitory activity against hCES1A1, with IC50 values less than 5.0 µM. The structures of all the compounds were elucidated using MS and 1D and 2D NMR data, and the absolute configurations of the new compounds were resolved via specific rotation, experimental and calculated ECD spectra, and single-crystal X-ray diffraction analysis. The structure-activity relationship analysis highlighted that the free HO-3 group in the pentacyclic triterpenoids is crucial for their potent inhibitory activity against hCES1A1.
Assuntos
Inibidores Enzimáticos/farmacologia , Paeonia , Extratos Vegetais/farmacologia , Raízes de Plantas , Carboxilesterase/antagonistas & inibidores , Linhagem Celular Tumoral , Glucosídeos , Humanos , Estrutura Molecular , Monoterpenos , Sesquiterpenos , Relação Estrutura-AtividadeRESUMO
OBJECTIVE: To study the neuroprotective effect of inhalation of volatile oil of Cang Ai (VOCA) on cerebral ischemia-reperfusion injury model by MRI diffusion tensor imaging. METHODS: Twenty-four healthy adult male SD rats were randomly divided into sham operation group, model (middle cerebral artery occlusion (MCAO) ) group and VOCA group. Evaluated the degree of neurological impairment of rats in each group immediately after successful establishment of model or 7 d later according to Zea Longa scoring. Coronal diffusion tensor imaging (DTI) scan was performed at 3 h, 3 d, and 7 d after the model successfully established by using 7.0 T magnetic resonance imaging. Measured the apparent diffusion coefficient (ADC) and anisotropy score (FA) of the DTI in the striatal region and the motion flat zone of the maximum infarct level and then calculate the relative apparent diffusion coefficient (rADC) and relative anisotropy score (rFA). TTC staining was used to evaluate the cerebral infarction volume of rats in each group at 7 d post model establishment, and the correlation analysis of rFA, rADC and neural score was performed. RESULTS: No neurological defect was detected in mice in the sham operation group. The MCAO group and the VOCA group showed neurological defect to different degrees. The neurological function score of the VOCA group was obviously lower than that of MCAO group at 7 th day (P<0.05). The DTI scan results showed that the rADC value of striatum of rats in VOCA group was higher than that in MCAO group at 3 h and 3 d after modeling (P<0.05), while there was no significant difference between the three groups at 7 th day. The rADC value of the motor cortex in the VOCA group was higher than that in the MCAO group at 3 h after modeling (P<0.01), and there was no significant difference at 3 rdday and 7 thday. The rFA value of striatum in VOCA group was higher than that in MCAO group at 3 rd day and 7 th day after modeling (P<0.05). There were no significant differences in rFA value between the MCAO and the VOCA group at three time points. TTC staining results showed that there was no infarcted area in the sham operation group, and the infarct volume in the VOCA group was smaller than that of the MCAO group (P<0.05). Correlation analysis showed that the striatum rFA value was highly correlated with neurological scores (r=ï¼0.847, P<0.01). CONCLUSION: For the first time, we found that VOCA can effectively protect the neurological function of MCAO rats by reducing the toxic edema of cells in the ischemic area and accelerating the recovery of nerve fiber bundles after cerebral ischemia and reperfusion. rFA and rADC values can be used as effective indicators to evaluate the recovery of nerve function after cerebral ischemia and reperfusion.
Assuntos
Isquemia Encefálica , Fármacos Neuroprotetores , Óleos Voláteis , Traumatismo por Reperfusão , Animais , Isquemia Encefálica/diagnóstico por imagem , Isquemia Encefálica/tratamento farmacológico , Imagem de Tensor de Difusão , Infarto da Artéria Cerebral Média , Masculino , Fármacos Neuroprotetores/farmacologia , Óleos Voláteis/farmacologia , Ratos , Ratos Sprague-Dawley , Traumatismo por Reperfusão/diagnóstico por imagem , Traumatismo por Reperfusão/tratamento farmacológico , PesquisaRESUMO
Fractionation of an aqueous extract of the air-dried roots of a traditional Chinese medicinal plant, Paeonia lactiflora, yielded the new monoterpenoid glycosides 1-10. Their structures were assigned via spectroscopic techniques, and the absolute configurations of 1, 4-6, and 8 were verified via chemical methods, specific rotation, and electronic circular dichroism data. Compounds 1-4 are rare compared to the reported cage-like paeoniflorin derivatives; that is, they comprised two monoterpenoidal moieties. In the in vitro assay, compounds 5, 8, and 9 showed weak inhibitions against lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophages, with IC50 values of 64.8, 60.1, and 97.5 µM, respectively.
Assuntos
Glicosídeos/química , Glicosídeos/farmacologia , Monoterpenos/química , Monoterpenos/farmacologia , Paeonia/química , Raízes de Plantas/química , Animais , Linhagem Celular , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Glucosídeos/química , Glucosídeos/farmacologia , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Camundongos , Óxido Nítrico/metabolismo , Células RAW 264.7RESUMO
A new sesquiterpenoid ester glycoside (1) and a new monoterpenoid ester glycoside (2) have been isolated from an ethanol extract of the twigs of Litsea cubeba. Their structures were elucidated by extensive 1D- and 2D-NMR experiments, and the absolute configurations were determined by chemical methods, specific rotation, and a combination of experimental and theoretically calculated electronic circular dichroism spectra. Compound 1 exhibited selective cytotoxicity against A549 and HCT-8 cell lines with the IC50 values of 8.9 and 9.6 µM, respectively.
Assuntos
Glicosídeos/química , Litsea/química , Terpenos/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Humanos , Estrutura MolecularRESUMO
The air-dried twigs of Litsea cubeba, a traditional Chinese medicinal tree, afforded 10 new aromatic glycosides (1-10) and 26 known analogues. Their structures were assigned by extensive 1D and 2D NMR experiments, and the absolute configurations were resolved by chemical methods, electronic circular dichroism, specific rotation, and X-ray crystallographic analysis. Compound 4 is the first example of a naturally occurring homoneolignan glucoside. Compounds 4, 6-8, and the known neolignan glucosides (11, 12, and 14) at respective 10 µM concentrations were found to reduce acetaminophen-induced HepG2 cell injury with 30.5-46.0% inhibitions. Furthermore, compounds 12 and 15 demonstrated moderate inhibitory activities against HDAC1, with IC50 values of 3.6 and 4.6 µM, respectively.
Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Litsea/química , Caules de Planta/química , Acetaminofen/farmacologia , Algoritmos , Cristalografia por Raios X , Medicamentos de Ervas Chinesas/química , Glicosídeos/química , Células Hep G2 , Humanos , Concentração Inibidora 50 , Lignanas/química , Lignanas/isolamento & purificação , Lignanas/farmacologia , Lipopolissacarídeos/farmacologia , Conformação Molecular , Estrutura Molecular , Óxido Nítrico/biossíntese , Ressonância Magnética Nuclear Biomolecular , Raízes de Plantas/químicaRESUMO
OBJECTIVE: To explore the clinical features of horizontal semicircular canal benign paroxysmal positional vertigo. METHODS: The clinical manifestations of 239 patients with horizontal semicircular canal benign paroxysmal positional vertigo from August 2003 to December 2010 were retrospectively analyzed. RESULTS: 25.7% (239/931) of all the benign paroxysmal positional vertigo patients were the horizontal semicircular canal benign paroxysmal positional vertigo was involved. One hundred and ninety-seven patients showed geotropic nystagmus in head rolling test with a mean latency period of (0.88 ± 0.72) s and a mean duration period of (26.36 ± 19.71) s. Forty-two patients showed apogeotropic nystagmus in head rolling test with a mean latency period of (2.69 ± 1.83) s and a mean duration period of (53.48 ± 43.12) s. Among all the horizontal semicircular canal benign paroxysmal positional vertigo patients, 39 (16.3%) presented horizontal nystagmus with slight upbeating component. The nystagmus latency in apogeotropic nystagmus group was longer than that in geotropic nystagmus group (t = -6.33, P < 0.001), and nystagmus duration period was also longer (t = -3.99, P < 0.001). Applied Barbecue maneuver to the patients with geotropic nystagmus, 192 patients were cured after (1.6 ± 0.8) rotations; After applied head shaking maneuver to the patients with apogeotropic nystagmus, 40 patients changed to geotropic nystagmus and cured after (1.9 ± 0.8) rotations. CONCLUSIONS: Incidence rate of horizontal semicircular canal benign paroxysmal positional vertigo was higher than expectation. Barbecue maneuver was applied to patients with geotropic nystagmus. While to the patients with apogeotropic nystagmus, head shaking maneuver should be performed firstly and then followed by Barbecue maneuver.