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1.
Article in Chinese | WPRIM | ID: wpr-879018

ABSTRACT

Chemical constituents were isolated and purified from the water extract of Artemisia annua by column chromatography of HP-20 macroporous resin, silica gel, ODS, Sephadex LH-20, HW-40, and semi-preparative RP-HPLC. Their structures were elucidated by physicochemical properties and spectral analyses. As a result, Fifteen compounds were isolated and identified as vitexnegheteroin M(1), sibricose A5(2), securoside A(3), citrusin D(4), annphenone(5), E-melilotoside(6), esculetin(7), scopoletin-7-O-β-D-glucoside(8), eleutheroside B_1(9), chrysosplenol D(10), patuletin-3-O-β-D-glucopyranoside(11), quercetin-7-O-β-D-glucoside(12), rutin(13), apigenin 6,8-di-C-β-D-glucopyranoside(14), isoschaftoside(15), among them, compounds 1-4 were identified from Artemisia for the first time. Additionally, the isolates were evaluated for their inhibitory effects on the production of PGE_2 in LPS-simulated RAW264.7 macrophages. The results showed that compounds 1, 2, 8, and 10-15 could reduce PGE_2 levels, to a certain extent.


Subject(s)
Apigenin , Artemisia annua , Quercetin , Rutin
2.
Rev. bras. farmacogn ; 29(1): 69-76, Jan.-Feb. 2019. tab, graf
Article in English | LILACS | ID: biblio-990769

ABSTRACT

Abstract In this study, the adsorption/desorption characteristics of quercetin, luteolin and apigenin from Flos populi extract (Populus tomentosa Carrière, Salicaceae) on twelve macroporous resins (NKA-9, HPD-600, HPD-826, HPD-750, HPD-400, DM-130, AB-8, SP-825, X-5, D-101, HPD-100, HPD-200) were evaluated. Both high adsorption and desorption capacities of quercetin, luteolin and apigenin from Flos populi extract on SP-825 resin indicated that SP-825 resin was appropriate and its data were well fitted to the Langmuir and Freundlich isotherms. To get the optimal separation process, the influences of factors such as flow rates, loading sample volumes, concentrations of desorption solution were further investigated. Column packed with SP-825 resin was used to perform dynamic adsorption and desorption experiments. After one round of treatment, the contents of quercetin, luteolin and apigenin in the final products were 3.75-fold, 3.67-fold and 3.54-fold increased with recovery yields of 87.25, 85.19 and 82.22%, respectively. The results showed that the preparative enrichment of quercetin, luteolin and apigenin was available via adsorption and desorption on SP-825 resin. This method is a promising basis for the large-scale preparation of quercetin, luteolin and apigenin from Flos populi.


Subject(s)
Quercetin , Apigenin , Luteolin , Adsorption , Populus
3.
Natural Product Sciences ; : 326-333, 2019.
Article in English | WPRIM | ID: wpr-786427

ABSTRACT

The purpose of our study was to evaluate anti-AD potential of Cirsium maackii flowers. MeOH extract, CH2Cl2, EtOAc, and n-BuOH fraction of this flower notably inhibited BACE1 (IC₅₀ = 76.47 ± 1.66, 22.98 ± 1.45, 8.65 ± 0.63, and 72.47 ± 3.04 µg/mL, respectively). β-amyrenone (49.70 mg) (1), lupeol acetate (1.43 g) (2), lupeol (1.22 g) (3), lupenone (23.70 mg) (4), β-sitosterol (1.01 g) (6), and β-sitosterol glucoside (13.00 mg) (7) from CH₂Cl₂, apigenin (100.20 mg) (8), luteolin (19.00 mg) (9), apigenin 7-O-glucuronide methyl ester (21.30 mg) (14), and tracheloside (53.70 mg) (5) from EtOAc, apigenin 5-O-glucoside (11.00 mg) (10), luteolin 5-O-glucoside (11.00 mg) (11) and apigenin 7-O-glucuronide (91.00 mg) (12) from n-BuOH, and luteolin 7-O-glucuronide (22.00 mg) (13) from H₂O fraction were isolated. HPLC showed high levels of 8, 9 and 12 in MeOH extract (33.07 ± 0.07, 31. 44 ± 0.17 and 16.89 ± 0.33 mg/g, respectively), EtOAc (161.01 ± 1.78, 96.93 ± 0.34 and 73.38 ± 0.06 mg/g, respectively), and n-BuOH fraction (32.18 ± 0.33, 44.31 ± 0.32 and 105.94 ± 0.36 mg/g, respectively). Since, 3 and 9 are well-known BACE1 inhibitors, the anti-AD activity of C. maackii flower might be attributable to their presence.


Subject(s)
Alzheimer Disease , Apigenin , Chromatography, High Pressure Liquid , Cirsium , Flowers , Luteolin
4.
Biol. Res ; 52: 7, 2019. graf
Article in English | LILACS | ID: biblio-1011410

ABSTRACT

BACKGROUND: Currently, the prognosis of patients with non-small cell lung cancer (NSCLC) remains dismal; hence, it is critical to identify effective anti-NSCLC agents with limited side effects. This study aimed to evaluate the therapeutic potential of flavonoid compound vitexin in human NSCLC cells and the underlying mechanisms. RESULTS: The experimental results indicated that vitexin reduced the viability of A549 cells in a dose-dependent manner with nearly no toxicity against normal human bronchial epithelial 16HBE cells. Vitexin also dose-dependently increased A549 cell apoptosis, accompanied by the decreased Bcl-2/Bax ratio and the increased expression of cleaved caspase-3. Moreover, the in vivo anticancer activity of vitexin was further determined in nude mice bearing A549 cells. In addition, vitexin induced the release of cytochrome c from the mitochondria to the cytosol and the loss of mitochondrial membrane potential. Vitexin also significantly reduced the levels of p-PI3K, p-Akt and p-mTOR, and the pro-apoptotic effect of vitexin on A549 cells was partly blocked by SC79, an Akt activator. CONCLUSIONS: Accordingly, we believed that vitexin could be used as a potential therapeutic agent for the treatment of NSCLC in the future.


Subject(s)
Humans , Animals , Mice , Apoptosis/drug effects , Carcinoma, Non-Small-Cell Lung/pathology , Phosphatidylinositol 3-Kinases/drug effects , Apigenin/pharmacology , Proto-Oncogene Proteins c-akt/drug effects , TOR Serine-Threonine Kinases/drug effects , Lung Neoplasms/pathology , Antineoplastic Agents/pharmacology , Signal Transduction/drug effects , Carcinoma, Non-Small-Cell Lung/metabolism , Cell Line, Tumor , Cell Proliferation/drug effects , Membrane Potential, Mitochondrial/drug effects , A549 Cells , Lung Neoplasms/metabolism , Mice, Nude , Mitochondria/drug effects
5.
Annals of Dermatology ; : 694-700, 2018.
Article in English | WPRIM | ID: wpr-719022

ABSTRACT

BACKGROUND: Kaempferol (3,4′,5,7-tetrahydroxyflavone) is a flavonoid known to have a wide range of pharmacological activities. The 3-OH group in flavonoids has been reported to determine antioxidant activities. OBJECTIVE: We tested whether kaempferol can affect the expression of integrins and the stem cell fate of interfollicular epidermal stem cells. METHODS: Skin equivalent (SE) models were constructed, and the expression levels of stem cell markers and basement membrane-related antigens were tested. The immunohistochemical staining patterns of integrins, p63, and proliferating cell nuclear antigen (PCNA) were compared between kaempferol- and apigenin-treated SE models. Reverse transcription-polymerase chain reaction (RT-PCR) was used to evaluate the mRNA expression of integrins. RESULTS: Kaempferol increased the thickness of the epidermis when added to prepare SEs. In addition, the basal cells of kaempferol- treated SEs appeared more columnar. In the immunohistological study, the expression of integrins α6 and β1 and the numbers of p63- and PCNA-positive cells were markedly higher in the kaempferol-treated model. However, apigenin showed no effects on the formation of three-dimensional skin models. RT-PCR analysis also confirmed that kaempferol increased the expression of integrin α6 and integrin β1. CONCLUSION: Our findings indicated that kaempferol can increase the proliferative potential of basal epidermal cells by modulating the basement membrane. In other words, kaempferol can affect the fate of interfollicular epidermal stem cells by increasing the expression of both integrins α6 and β1. These effects, in particular, might be ascribed to the 3-OH group of kaempferol.


Subject(s)
Apigenin , Basement Membrane , Epidermis , Extracellular Matrix , Flavonoids , Integrins , Proliferating Cell Nuclear Antigen , RNA, Messenger , Skin , Stem Cells
6.
Article in English | WPRIM | ID: wpr-812109

ABSTRACT

Cancer is a major health concern and leading burden on economy worldwide. An increasing effort is devoted to isolation and development of plant-derived dietary components as effective chemo-preventive products. Phytochemical compounds from natural resources such as fruits and vegetables are responsible for decreasing the risk of certain cancers among the consuming populations. Apigenin, a flavonoid phytochemical found in many kinds of fruits and vegetables, has been shown to exert significant biological effects, such as anti-oxidant, anti-inflammatory and most particularly anti-neoplastic properties. This review is intended to summarize the most recent advances in the anti-proliferative and chemo-preventive effects of apigenin in different cancer models. Analysis of the data from the studied cancer models has revealed that apigenin exerts its anti-proliferative effects through multiple and complex pathways. This guided us to discover some controversial results about the exact role of certain molecular pathways such as autophagy in the anticancer effects of apigenin. Further, there were cumulative positive evidences supporting the involvement of certain pathways such as apoptosis, ROS and DNA damage and repair. Apigenin possesses a high potential to be used as a chemosensitizing agent through the up-regulation of DR5 pathway. According to these preclinical findings we recommend that further robust unbiased studies should consider the possible interactions between different molecular pathways.


Subject(s)
Animals , Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Apigenin , Chemistry , Pharmacology , Apoptosis , Autophagy , Humans , Neoplasms , Drug Therapy , Genetics , Metabolism , Phytochemicals , Chemistry , Pharmacology
7.
Article in English | WPRIM | ID: wpr-80167

ABSTRACT

Apigenin (4′,5,7-trihydroxyflavone) is a flavonoid commonly found in many fruits and vegetables such as parsley, chamomile, celery, and kumquats. In the last few decades, recognition of apigenin as a cancer chemopreventive agent has increased. Significant progress has been made in studying the chemopreventive aspects of apigenin both in vitro and in vivo. Several studies have demonstrated that the anticarcinogenic properties of apigenin occur through regulation of cellular response to oxidative stress and DNA damage, suppression of inflammation and angiogenesis, retardation of cell proliferation, and induction of autophagy and apoptosis. One of the most well-recognized mechanisms of apigenin is the capability to promote cell cycle arrest and induction of apoptosis through the p53-related pathway. A further role of apigenin in chemoprevention is the induction of autophagy in several human cancer cell lines. In this review, we discuss the details of apigenin, apoptosis, autophagy, and the role of apigenin in cancer chemoprevention via the induction of apoptosis and autophagy.


Subject(s)
Apigenin , Apium , Apoptosis , Autophagy , Cell Cycle Checkpoints , Cell Line , Cell Proliferation , Chamomile , Chemoprevention , DNA Damage , Fruit , Humans , In Vitro Techniques , Inflammation , Oxidative Stress , Petroselinum , Rutaceae , Vegetables
8.
Article in English | WPRIM | ID: wpr-177274

ABSTRACT

We examined whether apigenin affects the gene expression, secretion and activity of matrix metalloproteinase-3 (MMP-3) in primary cultured rabbit articular chondrocytes, as well as in vivo production of MMP-3 in the knee joint of rat to evaluate the potential chondroprotective effects of apigenin. Rabbit articular chondrocytes were cultured in a monolayer, and reverse transcription - polymerase chain reaction (RT-PCR) was used to measure interleukin-1β (IL-1β)-induced expression of MMP-3, MMP-1, MMP-13, a disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4), and ADAMTS-5. In rabbit articular chondrocytes, the effects of apigenin on IL-1β-induced secretion and proteolytic activity of MMP-3 were investigated using western blot analysis and casein zymography, respectively. The effect of apigenin on MMP-3 protein production was also examined in vivo. In rabbit articular chondrocytes, apigenin inhibited the gene expression of MMP-3, MMP-1, MMP-13, ADAMTS-4, and ADAMTS-5. Furthermore, apigenin inhibited the secretion and proteolytic activity of MMP-3 in vitro, and inhibited production of MMP-3 protein in vivo. These results suggest that apigenin can regulate the gene expression, secretion, and activity of MMP-3, by directly acting on articular chondrocytes.


Subject(s)
Animals , Apigenin , Blotting, Western , Caseins , Chondrocytes , Gene Expression , Knee Joint , Knee , Osteoarthritis , Polymerase Chain Reaction , Rats , Reverse Transcription , Thrombospondins
9.
Article in Chinese | WPRIM | ID: wpr-815122

ABSTRACT

To investigate the effect of apigenin on self-renewal for sphere-forming cells in human small cell lung cancer cell line NCI-H446 and the underlying mechanisms.
 Methods: Sphere-forming cells from NCI-H446 cell line were cultured in stem cell-conditioned culture medium with ultra-low attachment surface plates. The rate of sphere-forming cells in the second passage sphere-forming cells was used to evaluate the inhibitory effects of apigenin on the self-renewal for sphere-forming cells. The protein level of urokinase-type plasminogen activator receptor (uPAR) in spheroids was analyzed by Western blot.
 Results: Apigenin signifcantly inhibited the self-renewal of the second passage sphere-forming cells [0, 5.0, 10.0, 20.0 μmol/L apigenin: (18.2±1.9)%, (13.6±1.7)%, (10.6±1.6)%, (6.9±1.3)%, respectively] and down-regulated uPAR expression in a concentration-dependent manner (P<0.05).
 Conclusion: Apigenin inhibits the self-renewal capacity of sphere-forming cells in NCI-H446 cells, which may be associated with down-regulation of uPAR expression.


Subject(s)
Apigenin , Pharmacology , Cell Line, Tumor , Down-Regulation , Genetics , Humans , Lung Neoplasms , Neoplastic Stem Cells , Pathology , Physiology , Receptors, Cell Surface , Receptors, Urokinase Plasminogen Activator , Genetics , Metabolism , Signal Transduction , Small Cell Lung Carcinoma , Drug Therapy , Pathology , Spheroids, Cellular , Physiology , Stem Cells
10.
Article in Chinese | WPRIM | ID: wpr-815121

ABSTRACT

To investigate the effect of jianpi-jiedu (JPJD) prescription-contained serum on colorectal cancer SW48 cell proliferation and the underlying mechanisms.
 Methods: Crude extract from JPJD was made by water extract method and the main components of crude extract from JPJD were analyzed by ultra-performance liquid phase high resolution time of flight mass spectrometry (UPLC-Q-TOF/MS). The low, medium, and high-concentration of JPJD-contained serum were prepared by the serum pharmacological method. The effect of serum containing JPJD on SW48 cell proliferation was determined by MTT assay. The cell cycle was detected by flow cytometric method. The protein levels of mammalian target of rapamycin (mTOR), phospho-mTOR, P-P53, and -P21, and the mRNA level of mTOR were examined by Western blot and RT-PCR, respectively.
 Results: Seven compounds including calycosin-7-glucoside, astragaloside, ginsenoside-Re, ginsenoside-Rb1, glycyrrhizinic acid, apigenin, atractylenolide-II were identified. MTT assays demonstrated that the SW48 cell proliferation was inhibited by medium and high concentration of JPJD-contained serum and the percentages of cells at G1 phase in SW48 cell cultured in the medium and high concentration of JPJD serum group were significantly higher than those in the control group (P<0.05). Meanwhile, the levels of mTOR mRNA and phospho-mTOR protein in the medium and high concentration of JPJD serum groups were substantially lower than those in the control group (P<0.05). Conversely, the expressions of phospho-P53 and P21 protein were significantly increased in the medium and high concentration of JPJD serum group compared with those in the control group.
 Conclusion: JPJD prescription-contained serum can inhibit SW48 cell proliferation, which may be related to mTOR-P53-P21 signaling pathways.


Subject(s)
Animals , Apigenin , Blotting, Western , Cell Cycle , Cell Division , Cell Proliferation , Genetics , Colorectal Neoplasms , Cyclin-Dependent Kinase Inhibitor p21 , Drugs, Chinese Herbal , Pharmacology , Flow Cytometry , Ginsenosides , Glycyrrhizic Acid , Humans , Lactones , Phosphorylation , Genetics , RNA, Messenger , Saponins , Sesquiterpenes , Signal Transduction , TOR Serine-Threonine Kinases , Triterpenes , Tumor Suppressor Protein p53
11.
Article in Chinese | WPRIM | ID: wpr-351224

ABSTRACT

Totally 80 rats were randomly divided into the control group, the model group, low, middle and high dose (25, 50, 100 mg x kg(-1)) scutellarin( SC) groups and the colchicine ( Col) group. Apart from the blank group, all of the remaining groups were intraperitoneally injected with 0.5 mL pig serum twice every week for consecutively 13 weeks and orally administered with the corresponding drugs since the 9th week. The blank group and the model group were orally given equal volume of normal saline once every for consecutively four weeks. After the experiment, efforts were made to detect the contents of alanine aminotransferase (ALT), aspertate aminotransferase (AST), albumin (ALB), total protein (TP), total bilirubin (TBIL), hyaluronic acid (HA), laminin (LN) and collagen type IV (CIV), collect liver tissues of fixed positions, observe the pathological changes through hematoxylin-eosin (HE) staining, conduct the pathological grading for liver fibrosis, determine the expressions of hepatic collagen type I and III (C I, C III) and calculate their color rendering index. Compared with the model group, low, middle and high dose (25, 50, 100 mg x kg(-1)) SC groups could decrease the contents of ALT, AST, TBIL, HA, LN, CIV, increase the contents of ALB, TP in serum and reduce the contents of C I, C III in liver tissues. In conclusion, scutellarin has a certain therapeutic effect on immune liver fibrosis in rats induced by pig serum.


Subject(s)
Alanine Transaminase , Genetics , Metabolism , Animals , Apigenin , Bilirubin , Genetics , Metabolism , Collagen Type IV , Genetics , Metabolism , Drugs, Chinese Herbal , Glucuronates , Humans , Liver , Metabolism , Liver Cirrhosis , Drug Therapy , Genetics , Metabolism , Male , Rats , Rats, Sprague-Dawley
12.
Article in Chinese | WPRIM | ID: wpr-330229

ABSTRACT

Lomatogonium rotatum (L.) Fries, Gentianopsis barbata (Froel) Ma, and Gentianella acuta (Michx.) Hulten, the three kinds of Digeda-species Mongolian medicinal materials belonging to the family Gentianaceae, bad been widely used for the treatment of liver diseases. To analyze comparatively the content of swertiamarin and swertisin among these three kinds of Digeda-species Mongolian medicinal materials. HPLC method was applied for qualitative and quantitative analysis of swertiamarin and swertisin. The Phenomenex C18 (4.6 mm x 250 mm, 5 μm) was used, chromatographic methanol and water as mobile phase, the flow rate was 1.5 mL x min(-1) with UV detected at 237 nm, column oven temperature was 25 degrees C. Results showed that the contents of swertiamarin and swertisin were closely related the different species and producing areas. The content range of swertiamarin in L. rotatum from different habitats was 1.73% - 2.72%, 0.43% - 0.96% for the swertisin content; the content of swertiamarin in G. barbata from Alxa Left Banner was 0.38%, and the content of swertiamarin and swertisin in G. barbata from the others habitats and G. Acuta from different habitats were all detected qualitatively. The contents of swertiamarin and swertisin among these medicinal plants showed a significant difference due to the different species and producing areas. As a consequence, these medicinal plants should not be put together for clinical applications.


Subject(s)
Apigenin , Chromatography, High Pressure Liquid , Gentianaceae , Chemistry , Classification , Gentianella , Chemistry , Classification , Iridoid Glucosides , Medicine, Mongolian Traditional , Mongolia , Plant Extracts , Pyrones
13.
Chinese Journal of Hepatology ; (12): 124-129, 2015.
Article in Chinese | WPRIM | ID: wpr-337027

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of apigenin on the protein expression levels of peroxisome proliferator-activated receptors (PPARs) in liver tissues of rats with nonalcoholic steatohepatitis (NASH).</p><p><b>METHODS</b>The NASH rat model was established by feeding of a high-fat diet. Unmodeled rats served as the normal controls. The modeled rats were divided into a model control group, Essentiale treatment grouP(300 mg/kg/day),and three apigenin treatment groups for low-dose (15 mg/kg/day), moderate-dose (30 mg/kg/day) and high-dose (60 mg/kg/day). After 13 weeks of treatment,changes in insulin sensitivity from pre-treatment baseline were assessed by measuring the alanine aminotransferase (ALT), aspartate aminotransferase (AST),total cholesterol (TC),triglycerides (TG),low-density and high-density lipoprotein cholesterol (LDL-C and HDL-C),fasting blood glucose (FBG) and fasting insulin (FINS).The liver index and HOMA-IR were also calculated.Protein and gene expression of PPARα and PPARgamma in liver tissue were assessed by immunohistochemistry and RT-PCR.Statistical analysis was performed by the LSD test and Games-Howell test.</p><p><b>RESULTS</b>The apigenin-treated groups showed a significantly greater change in insulin sensitivity than the untreated model group,with the most significant change occurring in the high-dose grouP(P less than 0.05).Compared with the untreated model group,the apigenin-treated groups showed lower levels of ALT (95.4+/-7.3),AST (183.7+/-14.3),TC (1.61+/-0.25),TG (1.23+/-0.21),LDL-C (1.86+/-0.14),FBG (5.29+/-1.45) and FINS (0.76+/-0.86),but a higher level of HDL-C (1.04+/-0.17); again,the high-dose group showed the greatest change (all P less than 0.05).Compared to the untreated model group,the apigenin-treated groups showed significantly lower liver index (3.75+/-0.25 vs.2.90+/-0.17) and HOMA-IR (1.34+/-0.06 vs.0.18+/-0.04),with the high-dose group showing the greatest change (both P less than 0.05). Compared to the untreated model group,the apigenin-treated groups showed higher levels of protein and mRNA of PPARα (18.27+/-4.05 and 0.63+/-0.02,respectively) and PPARgamma(8.48+/-5.05 and 0.39+/-0.02),with the high-dose group showing the greatest change (all P < 0.05).</p><p><b>CONCLUSION</b>Apigenin can improve glucose tolerance,lipid metabolism and insulin resistance while decreasing blood levels of TC,TG,LDL-C,FBG,FINS and HOMA-IR,and increasing HDL-C in NASH,as shown in a high-fat diet induced rat model, and may have therapeutic potential.</p>


Subject(s)
Alanine Transaminase , Metabolism , Animals , Apigenin , Pharmacology , Aspartate Aminotransferases , Metabolism , Blood Glucose , Metabolism , Cholesterol , Metabolism , Disease Models, Animal , Insulin , Metabolism , Insulin Resistance , Lipid Metabolism , Liver , Non-alcoholic Fatty Liver Disease , Metabolism , PPAR alpha , Metabolism , PPAR gamma , Metabolism , Peroxisome Proliferator-Activated Receptors , Metabolism , Rats , Rats, Sprague-Dawley , Triglycerides , Metabolism
14.
Article in Chinese | WPRIM | ID: wpr-305290

ABSTRACT

Vitexin, a naturally occurring flavone glycoside in plants, has many pharmacological effects, which is widely distributed in nature. This paper reviewed the research progress of the distribution of vitexin in the plant resources and its pharmacological effects, and summarized its application prospects, aiming to provide a useful reference for the development of vitexin-enriched plant resources.


Subject(s)
Animals , Antineoplastic Agents , Pharmacology , Antioxidants , Pharmacology , Apigenin , Pharmacology , Humans , Hypoglycemic Agents , Pharmacology , Myocardial Infarction , Drug Therapy , Plant Dispersal
15.
Article in English | WPRIM | ID: wpr-812148

ABSTRACT

Scutellarin (SCU), a flavonoid from a traditional Chinese medicinal plant. Our previous study has demonstrated that SCU relaxes mouse aortic arteries mainly in an endothelium-depend-ent manner. In the present study, we investigated the vasoprotective effects of SCU against HR-induced endothelial dysfunction (ED) in isolated rat CA and the possible mechanisms involving cyclic guanosine monophosphate (cGMP) dependent protein kinase (PKG). The isolated endothelium-intact and endothelium-denuded rat CA rings were treated with HR injury. Evaluation of endothelium-dependent and -independent vasodilation relaxation of the CA rings were performed using wire myography and the protein expressions were assayed by Western blotting. SCU (10-1 000 μmol·L(-1)) could relax the endothelium-intact CA rings but not endothelium-denuded ones. In the intact CA rings, the PKG inhibitor, Rp-8-Br-cGMPS (PKGI-rp, 4 μmol·L(-1)), significantly blocked SCU (10-1 000 μmol·L(-1))-induced relaxation. The NO synthase (NOS) inhibitor, NO-nitro-L-arginine methylester (L-NAME, 100 μmol·L(-1)), did not significantly change the effects of SCU (10-1 000 μmol·L(-1)). HR treatment significantly impaired ACh-induced relaxation, which was reversed by pre-incubation with SCU (500 μmol·L(-1)), while HR treatment did not altered NTG-induced vasodilation. PKGI-rp (4 μmol·L(-1)) blocked the protective effects of SCU in HR-treated CA rings. Additionally, HR treatment reduced phosphorylated vasodilator-stimulated phosphoprotein (p-VASP, phosphorylated product of PKG), which was reversed by SCU pre-incubation, suggesting that SCU activated PKG phosphorylation against HR injury. SCU induces CA vasodilation in an endothelium-dependent manner to and repairs HR-induced impairment via activation of PKG signaling pathway.


Subject(s)
Animals , Apigenin , Pharmacology , Cell Adhesion Molecules , Cell Hypoxia , Coronary Vessels , Cyclic GMP , Metabolism , Pharmacology , Cyclic GMP-Dependent Protein Kinases , Glucuronates , Pharmacology , Microfilament Proteins , NG-Nitroarginine Methyl Ester , Metabolism , Pharmacology , Phosphoproteins , Rats , Rats, Sprague-Dawley , Reperfusion Injury , Signal Transduction , Thionucleotides , Metabolism , Pharmacology , Vasodilation , Physiology
16.
Article in Chinese | WPRIM | ID: wpr-327833

ABSTRACT

In this study the chemical constituents of the higher polar sustances from Desmodium caudatum were investigated.The compounds were isolated by using column chromatographies over silicagel, polyamide, ODS, Sephadex LH-20, and preparative HPLC. The structures of these compounds were identified on the basis of NMR and MS spectra. Thirteen compounds were obtained and their structures were identified as vanillin(1), loliolide(2), indole-3-carboxaldehyde(3), salicylic acid(4), swertisin(5), saccharumoside C(6), isosinensin (7), kaempferol 3-O-β-D-glucopyranoside-7-O-α-L-rhamnopyranoside (8), isovitexin (9), vitexin (10), nothofagin(11), resveratroloside (12), and 2"-α-rhamnopyranosyl-7-O-methylvitexin (13). Except for compound 5, the remaining compounds were isolated from D. caudatum for the first time. Compounds 2, 3, 6-8, 11-13 were separated from the genus Desmodium for the first time.


Subject(s)
Apigenin , Chemistry , Drugs, Chinese Herbal , Chemistry , Fabaceae , Chemistry , Molecular Structure , Saponins , Chemistry , Spectrometry, Mass, Electrospray Ionization
17.
Chonnam Medical Journal ; : 45-51, 2014.
Article in English | WPRIM | ID: wpr-788290

ABSTRACT

Excessive accumulation of beta-amyloid peptide (Abeta) is one of the major mechanisms responsible for neuronal death in Alzheimer's disease. Flavonoids, primarily antioxidants, are a group of polyphenolic compounds synthesized in plant cells. The present study aimed to identify flavonoid compounds that could inhibit Abeta-induced neuronal death by examining the effects of various flavonoids on the neurotoxicity of Abeta fragment 25-35 (Abeta25-35) in mouse cortical cultures. Abeta25-35 induced concentration- and exposure-time-dependent neuronal death. Neuronal death induced by 20 microM Abeta25-35 was significantly inhibited by treatment with either Trolox or ascorbic acid. Among 10 flavonoid compounds tested [apigenin, baicalein, catechin, epicatechin, epigallocatechin gallate (EGCG), kaempferol, luteolin, myricetin, quercetin, and rutin], all except apigenin showed strong 1,1-diphenyl-2-pycrylhydrazyl (DPPH) scavenging activity under cell-free conditions. The flavonoid compounds except apigenin at a concentration of 30 microM also significantly inhibited neuronal death induced by 20 microM Abeta25-35 at the end of 24 hours of exposure. Epicatechin, EGCG, luteolin, and myricetin showed more potent and persistent neuroprotective action than did the other compounds. These results demonstrated that oxidative stress was involved in Abeta-induced neuronal death, and antioxidative flavonoid compounds, especially epicatechin, EGCG, luteolin, and myricetin, could inhibit neuronal death. These findings suggest that these four compounds may be developed as neuroprotective agents against Alzheimer's disease.


Subject(s)
Alzheimer Disease , Animals , Antioxidants , Apigenin , Ascorbic Acid , Catechin , Flavonoids , Luteolin , Mice , Neurons , Neuroprotective Agents , Oxidative Stress , Plant Cells , Quercetin
18.
Rio de Janeiro; s.n; 2014. xvii,69 p. ilus, tab, graf, mapas.
Thesis in Portuguese | LILACS | ID: lil-781870

ABSTRACT

A leishmaniose ainda é uma das doenças mais negligenciadas do mundo. Ela está presente nos cinco continentes e é endêmica em 98 países, com 350 milhões de pessoas vivendo em zonas de risco e mais de 12 milhões de pessoas infectadas. Compreende um complexo de doenças causadas por mais de 20 espécies do gênero Leishmania. No Brasil, a Leishmania amazonensis é uma espécie dermotrópica importante. Apesar do progresso na compreensão da bioquímica e biologia deste parasito, este conhecimento ainda não tem refletido na descoberta de novos e eficazes agentes quimioterápicos contra a doença. O tratamento atual é insatisfatório, com altas taxas de toxidez e ineficácia, e não há vacina humana licenciada. A pesquisa de novos medicamentos, a partir de fontes naturais, é amplamente utilizada como uma abordagem bem sucedida na detecção de compostos para o tratamento de doenças parasitárias. Compostos puros obtidos de plantas, como certos flavonoides, exibem atividade antiprotozoária. A apigenina é uma flavona bioativa, abundantemente presente em frutas,ervas e legumes, que mostrou atividade leishmanicida. A apigenina inibiu o crescimento celular de ambas as formas evolutivas de L. amazonensis de maneira dose-dependente. Este efeito inibitório, em promastigotas, foi igual a 74 por cento após 24 h de tratamento com 96 miM de apigenina e, em amastigotas intracelulares, foi igual a 71 por cento após 72 h de tratamento com 12miM do composto. O IC50/24 h em promastigotas foi 23,68 M e o IC50/72 h em amastigotas foi 4,33 miM. Observou-se que a apigenina foi capaz de induzir o aumento nos níveis de EROnos promastigotas e nos macrófagos infectados com L. amazonensis...


Leishmaniasis is still one of the most neglected diseases in the world. It is present on fivecontinents and is endemic in 98 countries, with 350 million people living in areas at risk andmore than 12 million people infected. Comprises a complex of diseases caused by over 20species of the genus Leishmania. In Brazil, Leishmania amazonensis is an importantdermotropic specie. Despite progress in understanding the biochemistry and biology of thisparasite, this knowledge has not been reflected in the discovery of new and effectivechemotherapeutic agents against the disease. The current treatment is unsatisfactory, withhigh toxicity and ineffectiveness, and there is no licensed human vaccine. The research ofnew drugs from natural sources is widely used as a successful approach in detectingcompounds for the treatment of parasitic diseases. Pure compounds obtained from plants,such as certain flavonoids, exhibit antiprotozoal activity. Apigenin is a bioactive flavone,abundantly present in fruits, herbs and vegetables, which showed leishmanicidal activity.Apigenin inhibited cell growth of both forms of L. amazonensis in dose-dependent manner.This inhibitory effect on promastigotes was equal to 74 percent after 24 h of treatment with 96miMapigenin and on intracellular amastigotes was equal to 71 percent after 72 h of treatment with 12 miM of the compound. The IC50/24 h) in promastigotes was 23.68 miM and the IC50/72 h inamastigotes was 4.33 miM. It was observed that apigenin was able to induce increased levels ofROS in treated promastigotes and L. amazonensis-infected macrophages...


Subject(s)
Animals , Apigenin/chemistry , Flavonoids , Leishmania , Leishmaniasis/epidemiology , Amphotericin B , Cell Death
19.
Article in English | WPRIM | ID: wpr-228919

ABSTRACT

Apigenin, a natural flavonoid found in a variety of vegetables and fruits, has been shown to possess many biological functions. The present study was undertaken to investigate the influence of apigenin on vascular smooth muscle contractility and to determine the mechanism involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Apigenin significantly relaxed fluoride-, thromboxane A2 mimetic- or phorbol ester-induced vascular contraction, which suggests that apigenin could be an anti-hypertensive that reduces agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, apigenin significantly inhibited fluoride-induced increases in pMYPT1 levels and phorbol ester-induced increases in pERK1/2 levels, which suggests the mechanism involving the inhibition of Rho-kinase and MEK activity and the subsequent phosphorylation of MYPT1 and ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of apigenin on agonist-induced vascular contraction regardless of endothelial function.


Subject(s)
Animals , Apigenin , Calcium , Fluorides , Fruit , Humans , Isometric Contraction , Male , Muscle, Smooth, Vascular , Nitric Oxide , Phosphorylation , Rats , Relaxation , rho-Associated Kinases , Thromboxane A2 , Vegetables
20.
Article in Chinese | WPRIM | ID: wpr-321324

ABSTRACT

<p><b>OBJECTIVE</b>To investigate whether the ERK/FoxO3a signal axis could induce the inhibitory effect of vitexin 1 (VB-1) in HepG2 cell proliferation.</p><p><b>METHOD</b>The MTT method was adopted to observe the effect of different concentrations of VB-1 on human hepatoma carcinoma cell line HepG2 and immortalized human embryo liver cell line L-02. The cell growth was assessed by the clone formation assay. The protein phosphorylation levels of ERK1/2 and FoxO3a were measured by the western blot.</p><p><b>RESULT</b>VB-1 inhibited the viability of HepG2 cell line in a concentration-dependent manner, with a weak effect on L-02 cell line. VB-1 could effectively inhibit the anchorage-dependent growth of HepG2 cells, and reduce the expression levels of pERK1/2 and pFoxO3a in a concentration-dependent manner. MEK1/2 inhibitor PD98059 could enhance VB-1' s effect in inhibiting HepG2 cell proliferation and ERK1/2, FoxO3a phosphorylation.</p><p><b>CONCLUSION</b>VB-1 inhibits the proliferative activity of hepatoma carcinoma cell line HepG2 by blocking the ERK/FoxO3a signal axis.</p>


Subject(s)
Apigenin , Pharmacology , Carcinoma, Hepatocellular , Drug Therapy , Genetics , Metabolism , Cell Proliferation , Drugs, Chinese Herbal , Pharmacology , Extracellular Signal-Regulated MAP Kinases , Genetics , Metabolism , Forkhead Box Protein O3 , Forkhead Transcription Factors , Genetics , Metabolism , Growth Inhibitors , Pharmacology , Hep G2 Cells , Humans , Liver Neoplasms , Drug Therapy , Genetics , Metabolism , Signal Transduction
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