RESUMO
In this research, the total phenolic and flavonoid amounts, phenolic compositions, inâ vitro antioxidant, antibacterial and antidiabetic properties of the methanol extracts obtained from Scabiosa L. (Caprifoliaceae) species distributed in the flora of Türkiye were investigated using chemometric methods. For this purpose, principal component (PCA) and agglomerative hierarchical clustering analysis were performed as chemometric methods. Chlorogenic acid, quinic acid and cyranoside were determined in the extracts. According to chemometric analysis, S. columbaria subsp. ochroleuca var. ochroleuca and S. triniifolia species were found to be valuable in terms of methanol extract yields, total phenolic and flavonoid contents, antioxidant and antidiabetic activities while S. columbaria subsp. ochroleuca var. webbiana species were found to be valuable in terms of phenolic composition. The methanol extracts of Scabiosa species showed high antioxidant activity, with high phenolic and flavonoid contents. Among the tested 13 bacteria, Scabiosa extracts showed only low activity against Klebsiella pneumoniae, Streptococcus pneumoniae and Pseudomonas aeruginosa. The extracts showed high α-amylase and α-glucosidase inhibitory activity. The results show that Scabiosa methanol extracts may be a source of alternative antioxidants that may be beneficial in slowing or preventing the progression of various oxidative stress-related diseases.
Assuntos
Caprifoliaceae , Dipsacaceae , Antioxidantes/farmacologia , Antioxidantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Quimiometria , Metanol , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Flavonoides/farmacologia , Compostos Fitoquímicos/farmacologiaRESUMO
In the field of research on medicinal plants from the Armenian flora, the phytochemical study of two Scabiosa L. species, S. caucasica M. Bieb. and S. ochroleuca L. (Caprifoliaceae), has led to the isolation of five previously undescribed oleanolic acid glycosides from an aqueous-ethanolic extract of the roots: 3-O-α-L-rhamnopyranosyl-(1â3)-ß-D-glucopyranosyl-(1â4)-ß-D-glucopyranosyl-(1â4)-ß-D-xylopyranosyl-(1â3)-α-L-rhamnopyranosyl-(1â2)-α-L-arabinopyranosyloleanolic acid 28-O-ß-D-glucopyranosyl-(1â6)-ß-D-glucopyranosyl ester, 3-O-ß-D-xylopyranosyl-(1â2)-[α-L-rhamnopyranosyl-(1â4)]-ß-D-glucopyranosyl-(1â4)-ß-D-glucopyranosyl-(1â4)-ß-D-xylopyranosyl-(1â3)-α-L-rhamnopyranosyl-(1â2)-α-L-arabinopyranosyloleanolic acid 28-O-ß-D-glucopyranosyl-(1â6)-ß-D-glucopyranosyl ester, 3-O-ß-D-xylopyranosyl-(1â2)-[α-L-rhamnopyranosyl-(1â4)]-ß-D-glucopyranosyl-(1â4)-ß-D-glucopyranosyl-(1â4)-ß-D-xylopyranosyl-(1â3)-α-L-rhamnopyranosyl-(1â2)-α-L-arabinopyranosyloleanolic acid, 3-O-ß-D-xylopyranosyl-(1â2)-[α-L-rhamnopyranosyl-(1â4)]-ß-D-xylopyranosyl-(1â4)-ß-D-glucopyranosyl-(1â4)-ß-D-xylopyranosyl-(1â3)-α-L-rhamnopyranosyl-(1â2)-α-L-arabinopyranosyloleanolic acid 28-O-ß-D-glucopyranosyl-(1â6)-ß-D-glucopyranosyl ester, 3-O-α-L-rhamnopyranosyl-(1â4)-ß-D-glucopyranosyl-(1â4)-ß-D-glucopyranosyl-(1â4)-ß-D-xylopyranosyl-(1â3)-α-L-rhamnopyranosyl-(1â2)-α-L-arabinopyranosyloleanolic acid 28-O-ß-D-glucopyranosyl-(1â6)-ß-D-glucopyranosyl ester. Their full structural elucidation required extensive 1D and 2D NMR experiments, as well as mass spectrometry analysis. For the biological activity of the bidesmosidic saponins and the monodesmosidic saponin, their cytotoxicity on a mouse colon cancer cell line (MC-38) was evaluated.
Assuntos
Caprifoliaceae , Dipsacaceae , Ácido Oleanólico , Saponinas , Triterpenos , Animais , Camundongos , Glicosídeos/farmacologia , Glicosídeos/química , Ácido Oleanólico/farmacologia , Ácido Oleanólico/química , Saponinas/química , Caprifoliaceae/química , Triterpenos/farmacologia , Triterpenos/químicaRESUMO
Intraspecific variations in pollen morphological traits are poorly studied. Interspecific variations are often associated with pollination systems and pollinator types. Altitudinal environmental changes, which can influence local pollinator assemblages, provide opportunities to explore differentiation in pollen traits of a single species over short distances. The aim of this study is to examine intraspecific variations in pollen traits of an insect-pollinated shrub, Weigela hortensis (Caprifoliaceae), along an altitudinal gradient. Pollen spine phenotypes (length, number and density), pollen diameter, lipid mass (pollenkitt) around pollen grains, pollen production per flower and pollinator assemblages were compared at four sites at different altitudes. Spine length and the spine length/diameter ratio of pollen grains were greater at higher altitudes but not correlated with flower or plant size. Spine number and density increased as flower size increased, and pollen lipid mass decreased as plant size increased. Bees were the predominant pollinators at low-altitude sites whereas flies, specifically Oligoneura spp. (Acroceridae), increased in relative abundance with increasing altitude. The results of this study suggest that the increase in spine length with altitude was the result of selection favouring longer spines at higher-altitude sites and/or shorter spines at lower-altitude sites. The altitudinal variation in selection pressure on spine length could reflect changes in local pollinator assemblages with altitude.
Assuntos
Caprifoliaceae , Insetos , Abelhas , Animais , Pólen , Altitude , Polinização , Flores/anatomia & histologia , PlantasRESUMO
The ethanolic extracts of the dried flower buds of two Caprifoliaceae plants, Lonicera japonica and Abelia × grandiflora, showed considerable inhibitory activities against adenosine triphosphate (ATP)-citrate lyase (ACL), a new promising drug target for the treatment of metabolic disorders. Bioassay-guided purification in conjunction with HPLC-PDA profiling led to the isolation and characterization of thirty-five (1-35) and fourteen (1'-14') structurally diverse compounds from the above two plant extracts, respectively. Compounds 1-9 and 1'-6' are previously undescribed glycosides. Their structures were elucidated on the basis of spectroscopic data, electronic circular dichroism (ECD), and single crystal X-ray diffraction analyses. In particular, lonicejaposide A (1) has an unprecedented skeleton generated through the coupling of C-7 in secologanin with C-2'' in phenylacetaldehyde via an aldol condensation. Abeliflorosides A (1') and B (2') are hitherto unknown glycosides of triterpene and bisiridoid conjugates constructed through the formation of a 1,3-dioxane moiety. All the isolates were evaluated for their inhibitory activities against ACL. Compounds 9, 25-28, 31, 1', 2', and 14' displayed significant inhibitory effects, with IC50 values ranging from 0.1 to 14.2 µM. The interactions of selected compounds possessing different structure features (e.g., 9, 25, 31, and 2') with ACL were thereafter performed by employing molecular docking studies. In addition, compound 2', the most complex triterpene-bisiridoid conjugate glycoside reported herein, also inhibited acetyl-CoA carboxylase 1 (ACC1), with an IC50 value of 7.9 µM. The dried material of the flower buds of L. japonica (honeysuckle) is a well-known traditional oriental medicine (i.e., Flos Lonicerae Japonicae, FLJ) and has long been used in large quantities. The above findings not only provide new insights for the development of multipurpose utilization of FLJ in healthcare community, but also provide profitable clues indicating that the flower buds of A. × grandiflora might be a potential alternative to FLJ in the traditional Chinese medicine market.
Assuntos
Caprifoliaceae , Lonicera , Triterpenos , Trifosfato de Adenosina , Flores/química , Glicosídeos/química , Lonicera/química , Simulação de Acoplamento Molecular , Complexos Multienzimáticos , Oxo-Ácido-LiasesRESUMO
Pterocephalus hookeri, as a kind of popular traditional Tibetan medicine, is reputed to treat inflammatory related diseases. In the present work, a cyclooxygenase-2 functionalized affinity solid-phase extraction HPLC system was developed and combined with preparative-HPLC for rapidly screening and separating cyclooxygenase-2 ligand from P. hookeri extracts. Firstly, ligands of cyclooxygenase-2 were screened from extracts by affinity solid-phase extraction HPLC system. Then directed by the screening results, the recognized potential active compounds were targeted separated. As a result, the major cyclooxygenase-2 inhibitor of P. hookeri was obtained with a purity of >95%, which was identified as sylvestroside I. To test the accuracy of this method, the anti-inflammatory activity of sylvestroside I was inspected in lipopolysaccharide-induced RAW 264.7 cells. The results show that sylvestroside I significantly suppressed the release of prostaglandin E2 with dose-dependent, which was in good agreement with the screening result of the affinity solid-phase method. This method of integration of screening and targeted separation proved to be very efficient for the recognition and isolation of cyclooxygenase-2 inhibitors from natural products.
Assuntos
Anti-Inflamatórios/química , Caprifoliaceae/química , Cromatografia de Afinidade/métodos , Inibidores de Ciclo-Oxigenase 2/química , Extratos Vegetais/química , Extração em Fase Sólida/métodos , Animais , Anti-Inflamatórios/metabolismo , Anti-Inflamatórios/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão/métodos , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/farmacologia , Medicina Tradicional Tibetana/métodos , Camundongos , Simulação de Acoplamento Molecular , Ligação Proteica , Células RAW 264.7 , Transdução de Sinais/efeitos dos fármacosRESUMO
Pterocephalus hookeri, a classical Tibetan herb, is mainly used to treat rheumatoid arthritis (RA) and contains various constituents potentially with cyclooxygenase-2 (COX-2) selective inhibition. A novel strategy for screening and target separating COX-2 inhibitors from the extracts of P. hookeri based on affinity solid-phase extraction (ASPE) column combined with preparative high-performance liquid chromatography (pre-HPLC) was successfully developed. The potential COX-2 inhibitors of P. hookeri were screened and recognized by the ASPE-HPLC system, which strategy is to analyze the compounds isolated by the ASPE column. Then, the active compounds were targeted separated by pre-HPLC according to real-time chromatograms. The control drugs celecoxib and glipizide were analyzed to verify the specificity and accuracy of the developed method. As a result, two pure compounds with COX-2 binding affinities were successfully separated from P. hookeri. They were characterized as swertisin and scopoletin using 1H- and 13C NMR spectroscopy, and the in vitro COX-2 inhibitory activities were verified. Compounds with COX-2 inhibitory activities could be screened and targeted separated from crude extracts by this strategy, which indicated that the proposed method was feasible, robust and effective for rapid separation of COX-2 inhibitors from natural products.
Assuntos
Caprifoliaceae/química , Cromatografia Líquida de Alta Pressão/métodos , Inibidores de Ciclo-Oxigenase 2 , Extração em Fase Sólida/métodos , Inibidores de Ciclo-Oxigenase 2/análise , Inibidores de Ciclo-Oxigenase 2/química , Inibidores de Ciclo-Oxigenase 2/isolamento & purificação , Extratos Vegetais/químicaRESUMO
BACKGROUND: Pterocephalus hookeri (C. B. Clarke) Höeck, a Tibetan medicine widely used for treatment of rheumatoid arthritis, was recorded in Chinese Pharmacopoeia (2020 version) with slight toxicity. The liver injury was observed in mice with administration of n-butanol extract (BUE) in our previously study. However, the toxic components and the mechanism were still unrevealed. PURPOSE: The present study was aimed to isolate and structural elucidate of the toxic compound pterocephin A (PA), as well as evaluate its liver toxicity and investigate its mechanism. METHODS: PA was isolated from the BUE of P. hookeri. Its structure was determined by analysis of HRMS, NMR and ECD data. L-02 cellular viability, LDH, ALT, AST, ROS, intracellular Ca2+ and the fluidity of cell membrane were assessed by multifunctional microplate reader. The PI staining, cell membrane permeability assessment, and mitochondrial fluorescence staining analysis were determined through the fluorescence microscope. Liver samples for mice were assessed by pathological and immunohistochemistry analysis. Expression levels of indicated proteins were measured by western blotting assays. RESULTS: PA was determined as a previously undescribed oleanolane-type triterpenoid saponin. In vitro study revealed PA significantly induced hepatotoxicity by inhibition of L-02 cell growth, abnormally elevation of ALT and AST. Mechanically, PA induced the damage of cell membrane, fragmentation of mitochondria, and subsequently increase of intracellular Ca2+ and ROS levels, which trigged by necroptosis with the activation of RIP1 and NF-κB signaling pathways. In vivo study confirmed PA could induce liver injury in mice with observation of the body weight loss, increasing of serum ALT and AST, and the histopathological changes in liver tissues. CONCLUSION: Our present study indicated that PA was an undescribed toxic constituent in P. hookeri to induce liver injury in mice by activation of necroptosis and inflammation. And the findings are of great significance for the clinical use safely of this herb.
Assuntos
Caprifoliaceae/química , Doença Hepática Crônica Induzida por Substâncias e Drogas/patologia , Necroptose , Saponinas/efeitos adversos , Triterpenos/efeitos adversos , Animais , Linhagem Celular , Feminino , Humanos , Inflamação , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Medicina Tradicional Tibetana , Camundongos , Estrutura Molecular , NF-kappa B/metabolismo , Compostos Fitoquímicos/efeitos adversos , Extratos Vegetais/efeitos adversosRESUMO
Two undescribed sesamin-type sesquilignans ptehoosines A (1) and B (2), together with 4 known lignans (3-6), were isolated from Pterocephalus hookeri (C.B. Clarke) Höeck which was widely used as traditional Tibetan medicine for treatment of rheumatoid arthritis. Their structures were determined by HR-ESI-MS, NMR analysis and CD experiment. The in vitro antiangiogenic effect of all isolated compounds against human umbilical vein endothelial cells (HUVECs) were evaluated by CCK-8 assay. Among them, compound 1 exhibited significant proliferative inhibition on HUVECs with IC50 value of 32.82 ± 0.99 µM. Further in vitro study indicated 1 could arrest cell cycle at G0/G1 phase and reduce the migration of HUVECs. In vivo experiment exhibited 1 could inhibit tail vessels plexus in zebrafish. The above finding suggested that 1 was a promising lead compound against RA by inhibiting of angiogenesis.
Assuntos
Inibidores da Angiogênese/farmacologia , Caprifoliaceae/química , Dioxóis/farmacologia , Lignanas/farmacologia , Inibidores da Angiogênese/isolamento & purificação , Animais , Pontos de Checagem do Ciclo Celular , Dioxóis/isolamento & purificação , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Humanos , Lignanas/isolamento & purificação , Medicina Tradicional Tibetana , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Tibet , Peixe-ZebraRESUMO
Floral traits are recognized to have evolved under selection for abiotic and biotic factors. Complex zygomorphic flowers usually face horizontally. It has been proved that a horizontal orientation facilitates pollinator recognition and pollination efficiency, but its significance in adaptation to abiotic factors remains unknown. The floral orientation of Abelia × grandiflora naturally varies around horizontal (with an angle of -30 to +33° between the floral main axis and the horizontal). We examined whether three different floral orientations affected flower thermal conditions, response to rain and pollination. Results showed that floral orientation had no effect on diurnal variations in flower temperature. The anthers of all three flower orientations were wetted by rainfall, but the inclined upward-facing flowers contained significantly more rainwater. The horizontal flowers received significantly higher visitation by hawkmoths and had a higher stigmatic pollen load. In contrast, the upward flower orientation reduced pollination precision, while downward-facing flowers had decreased pollinator attraction. This study indicates that horizontal flowers may have evolved as a trade-off between rain protection and pollination. Zygomorphic flowers that deviate from a horizontal orientation may have lower fitness because of flower flooding by rainwater and decreased pollen transfer.
Assuntos
Caprifoliaceae/anatomia & histologia , Flores/anatomia & histologia , Polinização , Chuva , Pólen , TemperaturaRESUMO
Palynology gives the evidence for identification and elimination of taxonomically complex genera. Pollen morphology of nine species (three subg., three sect.) of the genus Cephalaria Schrad. was studied using light microscopy and scanning electron microscopy. Pollen grains of all investigated species are triporate, suboblate to subprolate (P/E = 0.75-1.28), and large-sized (P = 58.52 µm-114.38, E = 63.84-119.70 µm). The outline of pollen grains in equatorial view is circular or elliptic, in polar view circular, circular-triangular, or triangular. Pores are distinct, lolongate, elliptic, or circular, with an annulus, operculum, and distinct or indistinct, wide halo surrounding the aperture. Exine sculpture is echinate-microechinate or echinate-microechinate-nanoechinate. Additional diagnostic characters at the species level in Cephalaria Schrad. that can be used for the purposes of taxonomy are size of pollen grains and pores, the shape of pores, the width of the annulus, structure of the exine, dimension of echini and microechini, location of microechini, and presence/absence of nanoechini. Palynomorphological data are compared with the taxonomical classification system of investigated taxa. It is shown that pollen grains morphology of the genus Cephalaria Schrad. is similar to the pollen morphology of the genus Dipsacus L., which confirms their inclusion in the Dipsaceae tribe.
Assuntos
Caprifoliaceae , Dipsacaceae , Microscopia Eletrônica de Varredura , PólenRESUMO
This work obtained and identified pterocephanoside A (1), one new iridoid glucoside derivative with rare structure of three iridoid glycosides linked to cyclopenta[c]pyran-3(1H)-one, and 10 known iridoids (2-11) from Pterocephalus hookeri through silica gel column chromatography and semi-preparative HPLC. The structure of the new compound was confirmed by 1D and 2D NMR and HRMS data analysis. Compounds 1 and 2 were isolated from this plant for the first time. The iridoids mostly possessed seco-iridoid subtype and iridoid subtype skeletons from P. hookeri. Compounds 1, 3, 4, and 6-11 showed weak anti-inflammatory activity.
Assuntos
Caprifoliaceae , Medicina Tradicional Tibetana , Glicosídeos Iridoides , Iridoides , Estrutura MolecularRESUMO
In order to study the interaction between Pterocephalus hookeri and bitter taste receptors,three-dimensional structural models of bitter taste receptors TAS2 R16,TAS2 R14 and TAS2 R13 were established by homology modeling in this paper. Maestro software was used for docking the chemical constituents of P. hookeri with bitter taste receptors. The results showed that 25 chemical components of P. hookeri can regulate three bitter taste receptors. And these components were mainly iridoid glycosides and phenolic acids.This research focused on the comprehensive application of homology modeling and molecular docking technology to explore the interaction between bitter chemical constituents of P. hookeri and bitter taste receptors. This study provided assistance in revealing pharmacodynamic basis of bitter Tibetan medicine at molecular level. It also provided new ideas and methods for the study of Tibetan medicine.
Assuntos
Caprifoliaceae/química , Medicina Tradicional Tibetana , Simulação de Acoplamento Molecular , Receptores Acoplados a Proteínas G/metabolismo , Correlação de Dados , Humanos , PaladarRESUMO
The intestinal absorption characteristics of ten iridoid glycosides and phenolic acids in the Pterocephali Herba were evaluated via rat intestinal valgus model. The intestinal sac fluids at different time after administration of high,medium and low concentrations of Pterocephali Herba extract were collected and ten chemical components in fluid samples were detected by UPLC-PDA. Accumulative absorbed doses( Q) and absorption rate constants( Ka) of ten chemical constituents were calculated,while proportions between Pterocephali Herba extract and intestinal absorption liquid were compared. The results showed that the intestinal absorption of 10 chemical components was linear absorption( R2>0. 9) at different concentrations,which accorded with the zero-order absorption rate. The absorption rate constant was related to the concentration of the drug and the intestinal site,which indicated that intestinal adsorption mechanism of the components were passive diffusion and active transport. Proportions of chemical constituents in intestinal sac fluid were different from those in Pterocephali Herba extract. Therefore,those ten chemical components in Pterocephali Herba extract can be absorbed in whole intestine. Everted intestinal sac model can be used to evaluate intestinal absorption characteristics of ingredients in Pterocephali Herba extract effectively.
Assuntos
Caprifoliaceae/química , Medicamentos de Ervas Chinesas/farmacocinética , Absorção Intestinal , Extratos Vegetais/farmacocinética , Animais , Intestinos , Ratos , Ratos Sprague-DawleyRESUMO
Seven oleanane-type glycosides were extracted and isolated by various chromatographic methods from the roots of Weigela x "Bristol Ruby" (1-7), six previously undescribed (1-6) and a known one (7). Their structures were assigned by spectroscopic analysis mainly 2D NMR and mass spectrometry (ESIMS). Selected triterpenoid glycosides (1-3, 6, 7) displayed a good cytotoxic activity against a mouse colon cancer cell line CT26.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Caprifoliaceae/química , Glicosídeos/farmacologia , Ácido Oleanólico/análogos & derivados , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Glicosídeos/isolamento & purificação , Camundongos , Estrutura Molecular , Ácido Oleanólico/isolamento & purificação , Ácido Oleanólico/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Raízes de Plantas/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologiaRESUMO
Pterocephalus hookeri (C. B. Clarke) Höeck, recorded in the Chinese Pharmacopoeia (2015 version) as a Tibetan medicine for the treatment of various diseases, especially rheumatoid arthritis, was believed to possess a slight toxicity. However, hardly any research has been carried out about it. The present study aimed to evaluate the toxicity in vivo and in vitro. Toxicity was observed by the evaluation of mice weight loss and histopathological changes in the liver. Then, the comparison research between ethyl acetate extract (EAE) and n-butanol extract (BUE) suggested that liver toxicity was mainly induced by BUE. The mechanical study suggested that BUE-induced liver toxicity was closely associated with necrosis detected by MTT and propidium iodide (PI) staining, via releasing lactate dehydrogenase (LDH), reducing the fluidity, and increasing the permeability of the cell membrane. Western blot analysis confirmed that the necrosis occurred molecularly by the up-regulation of receptor-interacting protein kinase 1 (RIP1) and receptor-interacting protein kinase 3 (RIP3), as well as the activation of the nuclear factor-kappa-gene binding (NF-κB) signaling pathway in vivo and in vitro. This finding indicated that the liver toxicity induced by BUE from P. hookeri was mainly caused by necrosis, which provides an important theoretical support for further evaluation of the safety of this folk medicine.
Assuntos
Caprifoliaceae , Doença Hepática Induzida por Substâncias e Drogas , Fígado/efeitos dos fármacos , Necrose/induzido quimicamente , Extratos Vegetais/toxicidade , Animais , Carragenina , Linhagem Celular , Membrana Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Edema/induzido quimicamente , Feminino , Proteínas Ativadoras de GTPase/metabolismo , Humanos , Fígado/metabolismo , Fígado/patologia , Masculino , Camundongos , NF-kappa B/metabolismo , Necrose/metabolismo , Necrose/patologia , Proteína Serina-Treonina Quinases de Interação com Receptores/metabolismoRESUMO
Honeyberry (Lonicera caerulea) has been used for medicinal purposes for thousands of years. Its predominant anthocyanin, cyanidin-3-O-glucoside (C3G), possesses antioxidant and many other potent biological activities. We aimed to investigate the effects of honeyberry extract (HBE) supplementation on HepG2 cellular steatosis induced by free fatty acids (FFA) and in diet-induced obese mice. HepG2 cells were incubated with 1 mM FFA to induce lipid accumulation with or without HBE. Obesity in mice was induced by a 45% high fat diet (HFD) for 6 weeks and subsequent supplementation of 0.5% HBE (LH) and 1% HBE (MH) for 6 weeks. HBE suppressed fatty acid synthesis and ameliorated lipid accumulation in HepG2 cells induced by FFA. Moreover, HBE also decreased lipid accumulation in the liver in the supplemented HBE group (LH, 0.5% or MH, 1%) compared with the control group. The expressions of adipogenic genes involved in hepatic lipid metabolism of sterol regulatory element-binding protein-1 (SREBP-1c), CCAAT/enhancer-binding protein alpha (C/EBPα), peroxisome proliferator-activated receptor gamma (PPARγ), and fatty acid synthase (FAS) were decreased both in the HepG2 cells and in the livers of HBE-supplemented mice. In addition, HBE increased mRNA and protein levels of carnitine palmitoyltransferase (CPT-1) and peroxisome proliferator-activated receptor α (PPARα), which are involved in fatty acid oxidation. Furthermore, HBE treatment increased the phosphorylation of AMP-activated protein kinase (AMPK) and Acetyl CoA Carboxylase (ACC). Honeyberry effectively reduced triglyceride accumulation through down-regulation of hepatic lipid metabolic gene expression and up-regulation of the activation of AMPK and ACC signaling in both the HepG2 cells as well as in livers of diet-induced obese mice. These results suggest that HBE may actively ameliorate non-alcoholic fatty liver disease.
Assuntos
Caprifoliaceae/química , Dieta Hiperlipídica/efeitos adversos , Hepatopatia Gordurosa não Alcoólica/induzido quimicamente , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Sobrevivência Celular , Células Hep G2 , Hepatócitos/efeitos dos fármacos , Humanos , Camundongos , Fitoterapia , Extratos Vegetais/químicaRESUMO
The intestinal absorption characteristics of ten iridoid glycosides and phenolic acids in the Pterocephali Herba were evaluated via rat intestinal valgus model. The intestinal sac fluids at different time after administration of high,medium and low concentrations of Pterocephali Herba extract were collected and ten chemical components in fluid samples were detected by UPLC-PDA. Accumulative absorbed doses( Q) and absorption rate constants( Ka) of ten chemical constituents were calculated,while proportions between Pterocephali Herba extract and intestinal absorption liquid were compared. The results showed that the intestinal absorption of 10 chemical components was linear absorption( R2>0. 9) at different concentrations,which accorded with the zero-order absorption rate. The absorption rate constant was related to the concentration of the drug and the intestinal site,which indicated that intestinal adsorption mechanism of the components were passive diffusion and active transport. Proportions of chemical constituents in intestinal sac fluid were different from those in Pterocephali Herba extract. Therefore,those ten chemical components in Pterocephali Herba extract can be absorbed in whole intestine. Everted intestinal sac model can be used to evaluate intestinal absorption characteristics of ingredients in Pterocephali Herba extract effectively.
Assuntos
Animais , Ratos , Caprifoliaceae , Química , Medicamentos de Ervas Chinesas , Farmacocinética , Absorção Intestinal , Intestinos , Extratos Vegetais , Farmacocinética , Ratos Sprague-DawleyRESUMO
In order to study the interaction between Pterocephalus hookeri and bitter taste receptors,three-dimensional structural models of bitter taste receptors TAS2 R16,TAS2 R14 and TAS2 R13 were established by homology modeling in this paper. Maestro software was used for docking the chemical constituents of P. hookeri with bitter taste receptors. The results showed that 25 chemical components of P. hookeri can regulate three bitter taste receptors. And these components were mainly iridoid glycosides and phenolic acids.This research focused on the comprehensive application of homology modeling and molecular docking technology to explore the interaction between bitter chemical constituents of P. hookeri and bitter taste receptors. This study provided assistance in revealing pharmacodynamic basis of bitter Tibetan medicine at molecular level. It also provided new ideas and methods for the study of Tibetan medicine.
Assuntos
Humanos , Caprifoliaceae , Química , Correlação de Dados , Medicina Tradicional Tibetana , Simulação de Acoplamento Molecular , Receptores Acoplados a Proteínas G , Metabolismo , PaladarRESUMO
Species represent the most basic unit of taxonomy. As such, species delimitation represents a crucial issue for biodiversity conservation. Taxonomic practices were revolutionized in the last three decades due to the increasing availability of molecular phylogenetic data. The genus Triplostegia (Caprifoliaceae) traditionally consists of two species, T. glandulifera and T. grandiflora, distinguishable mainly based on quantitative morphological features. In this study, we sequenced nine chloroplast loci (i.e., accD, psbK-psbI, rbcL-accD, rpoB-trnC, rps16-trnQ, trnE-trnT, trnF-ndhJ, trnH-psbA, trnS-trnG) and one nuclear locus (ITS) of 16 individuals of Triplostegia representing the entire distribution range of both species recognized. Furthermore, we also obtained whole chloroplast sequences for 11 of the 16 individuals for which silica gel-dried leaves were available. Our phylogenetic analyses integrating chloroplast genome sequences and multiple loci data revealed that Triplostegia includes four main clades that largely match geography. Neither T. grandiflora nor T. glandulifera was recovered as monophyletic and no diagnosable differences in leaf, flower, and pollen traits were detected between the two species, indicating the need for a revised species circumscription within Triplostegia. Our study highlights the importance of combining data from different sources while defining species limits.
Assuntos
Caprifoliaceae/genética , Loci Gênicos , Genoma de Cloroplastos , Sequência de Bases , Cloroplastos/genética , Genes de Plantas , Geografia , Filogenia , Folhas de Planta/anatomia & histologia , Pólen/ultraestrutura , Especificidade da EspécieRESUMO
Flos Lonicerae was an important Chinese medicine. In this research, a microwave assisted extraction method was applied for the extraction of chlorogenic acid from Flos Lonicerae. The operating conditions were optimized using a Box-Behnken design test. Under the optimal conditions, the extraction yield of chlorogenic acid reached 32.52⯱â¯1.31â¯mg/g. Next, a direct analysis in real time mass spectrometry (DART-MS) method was utilized to quantify of chlorogenic acid in Flos Lonicerae extracts. The primary parameters were optimized to obtain maximum signal intensity. In the detection process of the actual samples, the results obtained by DART-MS are consistent with those obtained by HPLC method with short detection time and acceptable repeatability and precision (<15%). In addition, the DART-MS/MS method has several advantages, such as speed, low cost and simplicity. Therefore, the DART-MS method is an efficient method that can be applied in the quantification of chlorogenic acid in Flos Lonicerae.