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1.
A new xanthone derivative, aspidxanthone A ( 1 ), and three known compounds ((2S)-1-(β-D-galactopyranosyloxy)-3-(hexadecanoyloxy)propan-2-yl (9Z,12Z)-octadeca-9,12-dienoate ( 2 ), (25S)-spirostane-1β,3α,5β-triol ( 3 ), and asparenyldiol ( 4 )) were isolated from the whole of the endemic species Aspidistra letreae in Vietnam. Their structures were elucidated by means of extensive spectroscopic analyses and comparison with published data. In this study, we report the isolation and structure elucidation of a new compound aspidxanthone A, antioxidant activities of the extract and isolates 1 – 4 , and in silico molecular docking of aspidxanthone A. The ethyl acetate extract had good antioxidant activity with an IC50 value of 26.3 μg mL−1. Among the isolates, aspidxanthone A exhibited DPPH reduction activity with an IC50 value of 11.2 μM, which is in the same range as that of the positive control, ascorbic acid. The mechanism of action of aspidxanthone A on the tyrosinase and xanthine oxidase proteins have been clarified by in silico studies.  相似文献   

2.
The present study was designed to appraise the photoprotective, antioxidant, and antibacterial bioactivities of Ruellia tuberosa leaves extracts (RtPE, RtChl, RtEA, RtAc, RtMe, and RtHMe). The results showed that, RtHMe extracts of R. tuberosa was rich in total phenolic content, i. e., 1.60 mgGAE/g dry extract, while highest total flavonoid content was found in RtAc extract, i. e., 0.40 mgQE/g. RtMe showed effective antioxidant activity (%RSA: 58.16) at the concentration of 120 μL. RtMe, RtEA and RtHMe exhibited effective in vitro antibacterial activity against Gram-negative bacteria (E. coli). In silico docking studies revealed that paucifloside (−11.743 kcal/mol), indole-3-carboxaldehyde (−7.519 kcal/mol), nuomioside (−7.275 kcal/mol), isocassifolioside (−6.992 kcal/mol) showed best docking score against PDB ID 2EX8 [penicillin binding protein 4 (dacB) from Escherichia coli, complexed with penicillin-G], PDB ID 6CQA (E. coli dihydrofolate reductase protein complexed with inhibitor AMPQD), PDB ID 2Y2I [Penicillin-binding protein 1B in complex with an alkyl boronate (ZA3)] and PDB ID 2OLV (from S. aureus), respectively. Docked phytochemicals also showed good drug likeness properties.  相似文献   

3.
In this study, total phenolic and flavonoid analyses of flower, leaf, and stem aqueous extracts of C. orientalis were performed. Total phenolic contents of C. orientalis extracts ranged from 12.2±0.06 to 19.0±0.07 mg GAE/g extract. Total flavonoid values range between 2.0±0.11 and 6.6±0.19 mg CE/g extract. Urease, collagenase, tyrosinase, and α-glucosidase inhibition activities were determined in vitro and the relationship between them was examined. IC50 results for all enzymes were obtained between 0.18 and 3.53 μg/mL. The aqueous extract of the plant C. orientalis showed potent cytotoxic effects against the human colon cancer cell lines DLD-1. As the extract concentration increases, cell death increases. The main fatty acid composition by GC/MS analysis is erucic acid (36.5 %). The potential binding modes of the fatty acids in the plant extract to the enzymes and possible inhibition mechanisms were determined by molecular docking calculation.  相似文献   

4.
The chemical and pharmacological profiles of essential oils (EOs) hydrodistilled in yields of 0.03–0.77 % (w/w) from three exotic (Cinnamomum camphora, Petroselinum crispum, and Syzygium samarangense) and two endemic (Pittosporum senacia subsp. senacia and Syzygium coriaceum) medicinal plants were studied. GC-MS/GC-FID analysis of the EOs identified the most dominant components to be myristicin (40.3 %), myrcene (62.2 %), 1,8-cineole (54.0 %), β-pinene (21.3 %) and (E)-β-ocimene (24.4 %) in P. crispum, P. senacia and C. camphora, S. samarangense and S. coriaceum EOs, respectively. All EOs were found to possess anti-amylase (0.70–1.50 mM ACAE/g EO) and anti-tyrosinase (109.35–158.23 mg KAE/g) properties, whereas no glucosidase inhibition was displayed. Only Syzygium EOs acted as dual inhibitors of both acetyl- and butyryl-cholinesterases, while P. senacia and C. camphora EOs inhibited acetylcholinesterase selectively and P. crispum EO was inactive (AChE: 4.64–4.96 mg GALAE/g; BChE: 5.96 and 7.10 mg GALAE/g). Molecular docking revealed 1,8-cineole to present the best binding affinities with butyrylcholinesterase, amylase and tyrosinase, while both myristicin and β-pinene with acetylcholinesterase and finally β-pinene with glucosidase. In vitro antioxidant potency was also demonstrated in different assays (DPPH: 13.52–53.91 mg TE/g, ABTS: 5.49–75.62 mg TE/g; CUPRAC: 45.38–243.21 mg TE/g, FRAP: 42.49–110.64 mg TE/g; and phosphomolybdenum assay: 82.61–160.93 mM TE/g). Principal component analysis revealed the EOs to differ greatly in their bioactivities due to their chemodiversity. This study has unveiled some interesting preliminary pharmacological profiles of the EOs that could be explored for their potential applications as phytotherapeutics.  相似文献   

5.
Lactoperoxidase enzyme (LPO) is secreted from salivary, mammary, and other mucosal glands including the bronchi, lungs, and nose, which had functions as a natural and the first line of defense towards viruses and bacteria. In this study, methyl benzoates were examined in LPO enzyme activity. Methyl benzoates are used as precursors in the synthesis of aminobenzohydrazides used as LPO inhibitors. For this purpose, LPO was purified in a single step using sepharose-4B-l-tyrosine-sulfanilamide affinity gel chromatography with a yield of 9.91 % from cow milk. Also, some inhibition parameters including the half maximal inhibitory concentration (IC50) value and an inhibition constant (Ki) values of methyl benzoates were determined. These compounds inhibited LPO with Ki values ranging from 0.033±0.004 to 1540.011±460.020 μM. Compound 1 a (methyl 2-amino-3-bromobenzoate) showed the best inhibition (Ki=0.033±0.004 μM). The most potent inhibitor ( 1 a ) showed with a docking score of −3.36 kcal/mol and an MM-GBSA value of −25.05 kcal/mol, of these methyl benzoate derivatives ( 1 a – 16 a ) series are established H-bond within the binding cavity with residues Asp108 (distance of 1.79 Å), Ala114 (distance of 2.64 Å), and His351 (distance of 2.12 Å).  相似文献   

6.
Melanin is the major factor that determines skin color and protects from ultraviolet radiation. In present study we evaluated the anti‐melanogenesis effect of acetazolamide (ACZ) using four different approaches: enzyme kinetic, in vitro, in vivo and in silico. ACZ demonstrated significant inhibitory activity (IC50 7.895 ± 0.24 μm ) against tyrosinase as compared to the standard drug kojic acid (IC50 16.84 ± 0.64 μm ) and kinetic analyses showed that ACZ is a non‐competitive inhibitor without cytotoxic effect. In in vitro experiments, A375 human melanoma cells were treated with 20 or 40 μm of ACZ with or without 50 μm of l ‐DOPA. Western blot results showed that ACZ significantly (< 0.05) decreased the expression level of tyrosinase at 40 μm . Zebrafish embryos were treated with 10, 20 or 40 μm of ACZ and of positive control kojic acid. At 72 h of treatment with ACZ and kojic acid, ACZ significantly (< 0.001) decreased the embryos pigmentation to 40.8% of untreated embryos at the dose of 40 μm of ACZ while kojic acid decreased only 25.0% of pigmentation at the same dose of kojic acid. In silico docking were performed against tyrosinase using PyRx tool. Docking studies suggested that His244, Asn260 and His85 are the major interacting residues in the binding site of the protein. In conclusion, our results suggest that ACZ is a good candidate for the inhibition of melanin and it could be used as a lead for developing the drugs for hyperpigmentary disorders and skin whitening.  相似文献   

7.
镉胁迫下3种藓类植物抗氧化酶活性变化的比较研究   总被引:11,自引:2,他引:11  
采用水培实验研究了重金属Cd对3种藓类植物尖叶拟船叶藓(Dolichomitriopsis diversiformis)、湿地匍灯藓(Plagiomnium acutum)和匍枝青藓(Brachythecium procumbens)的抗氧化酶系统(SOD、POD和CAT)的影响.结果表明,在1-100 mg·L-1的镉胁迫浓度范围内,Cd对3种藓类植物的SOD活性都具有显著的促进作用,SOD对Cd胁迫的种间敏感性顺序为尖叶拟船叶藓>湿地匍灯藓>匍枝青藓;3种藓类植物的POD和CAT活性对Cd胁迫均表现为先升后降,POD对Cd胁迫的种间敏感性顺序为匍枝青藓>湿地匍灯藓>尖叶拟船叶藓;高浓度Cd对CAT具有明显的抑制效应,CAT对Cd胁迫的种间敏感性顺序为湿地匍灯藓>尖叶拟船叶藓>匍枝青藓.在Cd长期胁迫下,SOD对3种藓类植物体内活性氧的清除起到关键作用,可作为藓类植物抗镉能力强弱的敏感生理指标;3种鲜类植物中匍枝青藓的抗镉能力最强,湿地匍灯藓次之,尖叶拟船叶藓最弱,并且这种抗性与cd在植物体内的积累成反相关.  相似文献   

8.
Toddalia asiatica (L.) Lam. is extensively used in traditional medicinal systems by various cultures. Despite its frequent use in traditional medicine, there is still a paucity of scientific information on T. asiatica growing on the tropical island of Mauritius. Therefore, the present study was designed to appraise the pharmacological and phytochemical profile of extracts (methanol, ethyl acetate and water) and essential oil obtained from aerial parts of T. asiatica. Biological investigation involved the evaluation of in vitro antioxidant and enzyme inhibitory potentials. The chemical profile of the EO was determined using gas chromatography coupled to mass spectrometry (GC/MS) analysis, while for the extracts, the total phenolic (TPC) and flavonoid content were quantified as well as their individual phenolic compounds by LC/MS/MS. Quinic acid, fumaric acid, chlorogenic acid, quercitrin and isoquercitrin were the main compounds in the extracts. Highest total phenolic (82.5±0.94 mg gallic acid equivalent (GAE/g)) and flavonoid (43.8±0.31 mg rutin equivalent (RE/g)) content were observed for the methanol extract. The GC/MS analysis has shown the presence of 26 compounds with linalool (30.9 %), linalyl acetate (20.9 %) and β-phellandrene (7.9 %) being most abundant components in the EO. The extracts and EO showed notable antioxidant properties, with the methanol extract proved to be superior source of antioxidant compounds. Noteworthy anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BChE) effects were recorded for the tested samples, while only the methanol and ethyl acetate extracts were active against tyrosinase. With respect to antidiabetic effects, the extracts and EO were potent inhibitors of α-glucosidase, while modest activity was recorded against α-amylase. Docking results showed that linalyl acetate has the highest affinity to interact with the active site of BChE with docking score of −6.25 kcal/mol. The findings amassed herein act as a stimulus for further investigations of this plant as a potential source of bioactive compounds which can be exploited as phyto-therapeutics.  相似文献   

9.
铝胁迫对黑大豆膜脂过氧化及抗氧化酶活性的影响   总被引:1,自引:0,他引:1  
以耐酸型黑大豆(丹波黑大豆,简称RB)和酸敏感型黑大豆(简称SB)为材料,在水培条件下分析不同浓度的铝胁迫对这两种黑大豆叶和根膜脂过氧化和抗氧化酶活性的影响。结果显示:RB的铝耐受能力比SB强;在不同浓度铝胁迫下RB叶和根中的H2O2和MDA上升幅度低于SB,SB的叶和根中膜脂过氧化程度大于RB。在不同浓度铝胁迫下,RB叶和根中的SOD活性与SB差异不大,而CAT活性在RB和SB的叶和根中均被诱导显著升高,POD活性在RB叶和根中有下降趋势但仍然显著高于SB。因此,与酸敏感型的黑大豆相比,耐酸型黑大豆在铝胁迫下具有较强的保护酶活性,使其膜脂受氧化损伤的程度较低,从而表现出更强的耐铝胁迫能力。  相似文献   

10.
考察虎刺80%乙醇提取物和石油醚、二氯甲烷、乙酸乙酯、水溶性部位的抗氧化和抗菌活性以及与总黄酮含量的关系。乙酸乙酯部位在清除DPPH自由基和还原力模型中抗氧化活性最强,水溶性部位在总抗氧化力模型中抗氧化活性最强,而石油醚部位抗氧化活性最弱。二氯甲烷部位、乙酸乙酯部位和石油醚部位具有一定的抑菌活性。虎刺黄酮类成分可能是其抗氧化的物质基础。  相似文献   

11.
为了探讨脱落酸(ABA)对锁阳茎切口愈合及抗氧化酶活性的影响,测定了锁阳茎3个部位(上部、中部和下部)内源ABA含量和切口愈合能力(抗失水力)以及苯丙氨酸解氨酶(PAL)、过氧化物酶(SOD)、过氧化氢酶(CAT)及抗坏血酸过氧化物酶(APX)活性随切口愈合时间的变化。结果表明,内源ABA含量随切口愈合天数的增加整体呈上升趋势。外源ABA处理明显增强了锁阳茎3个部位的PAL活性及抗氧化酶活性,加速了锁阳茎切口愈合,减少失水也提高了其抗氧化能力。比较3个部位,各指标均呈现出上部高于中部,中部高于下部的趋势。  相似文献   

12.
We report the synthesis, spectroscopic characterization, molecular docking and biological evaluation of nine pyrazino-imidazolinone derivatives. These derivatives were evaluated for their anticancer activity against three cancer cell lines: 518A2 melanoma, HCT-116, and HCT-116 p53 knockout mutant colon carcinoma. The MTT assay was employed to assess their effectiveness. Among the nine compounds tested, four compounds (5 a, 5 d, 5 g, and 5 h) exhibited promising antiproliferative activity specifically against HCT-116 p53-negative cells (IC50 0.23, 0.20, 2.07 and 58.75 μM, respectively). Interestingly, treatment with the 3,4-dimethoxyphenyl derivative 5a resulted in a significant increase (199 %) in caspase activity in HCT-116 p53-negative cells compared to untreated cells while the bromo-pyrazine derivative 5d demonstrated (190 %) increase. These findings suggest that compounds 5a and 5 d induce p53-independent apoptotic cell death. Additionally, in silico molecular docking studies with EGFR and tyrosinase proteins indicated that compounds 5 d and 5 e have the potential to bind to important anticancer drug targets.  相似文献   

13.
Resinous beehive product propolis has many biological activities. It contains various aromatic substances that have great differences in their chemical composition depending on the natural flora. Thus, chemical characterization and biological properties of propolis samples is an important subject for the pharmaceutical industry. In this study, the propolis samples collected from three cities in Turkey were prepared as methanol (MEP), ethanol (EEP), chloroform (ChlEP), hexane (HxEP), and ethyl acetate (EAEP) extracts using an ultrasonic assisted technique. The antioxidant capacities of the samples were evaluated by free radical scavenging activity (DPPH), cation radical scavenging activity (ABTS), and reducing activity (CUPRAC) and (FRAP). The strongest biological activities were detected in ethanol and methanol extracts. Enzyme inhibition of the propolis samples were determined against the human glutathione S-transferase (GST) and angiotensin converting enzyme (ACE). IC50 values of MEP1, MEP2, and MEP3 samples against the ACE were found as 13.9 μg/mL, 14.8 μg/mL, and 12.8 μg/mL, while against the GST IC50 values of MEP1, MEP2, and MEP3 samples were as 5.92 μg/mL, 9.49 μg/mL, and 5.72 μg/mL. To know the possible causes of the biological test results advanced LC/MS/MS method was applied. trans-ferulic acid, kaempferol, and chrysin were found as the most abundant phenolic compounds in each sample. The propolis extracts obtained using the proper solvent have a good potential to be used in pharmaceuticals to treat the diseases related to oxidative damage, hypertension, and inflammation. Finally, the interactions between chrysin, trans-ferulic acid and kaempferol molecules with ACE and GST receptors were analyzed using molecular docking study. Selected molecules interact with active residues by binding to the active site of the receptors.  相似文献   

14.
International Journal of Peptide Research and Therapeutics - Angiotensin converting enzyme (ACE) and reactive oxygen species are crucial targets for nutritional management of hypertension. The aim...  相似文献   

15.
The present study was to find out the expression pattern and relative expression level of apoptotic (Bcl2, Bax, Casp3, and PCNA) and antioxidant enzyme [(GPx, Cu/Zn-SOD (SOD1) and Mn-SOD (SOD2)] genes in sheep oocytes and developing embryos produced in vitro by conventional RT-PCR and real time qPCR, respectively. Different developmental stages of embryos were produced in vitro from oocytes collected from local slaughter house ovaries. RT-PCR amplicons showed expression of Bcl2 and PCNA in all stages except at morula. In contrast Bax and Casp3 were expressed in all stages. GPx and SOD1 were expressed in all stages but SOD2 was not expressed in 8–16 cells, although expressed in the remaining stages. The qPCR analysis reflected that Bcl2 expression was significantly (P < 0.05) downregulated in morula and maximum upregulated expression was observed in in vitro matured oocytes. Higher upregulated expression (P < 0.05) of Bax was in morula and downregulated expression was at 2-4 cells. Casp3 was significantly upregulated at 8–16 cells and downregulated in in vitro matured oocyte. PCNA expression was highest at blastocyst and least expression was at morula. GPx was expressed significantly highest in matured oocytes and least expression was at zygote. SOD1 was expressed significantly highest at 8–16 cells and least expression was at zygote. Expression of SOD2 was least among all the antioxidant enzymes but significantly higher expression of SOD2 was in immature oocyte; however, least expression was at 8–16 cells. It can be concluded from the study that the sheep embryos produced in vitro are highly sensitive to culture condition, which alters the expression level of apoptotic and antioxidant enzyme genes.  相似文献   

16.
高山植物绵头雪莲花(Saussurea laniceps HandMazz.)组织培养苗经2℃低温锻炼后抗寒性明显增强,SOD、CAT、POD活性明显提高,可溶性蛋白质、脯氨酸含量升高,而可溶性糖含量没有明显变化.脱锻炼期间可溶性蛋白质含量仍高于低温锻炼期间的水平,脱锻炼后抗氧化酶活性略有上升或保持稳定状态.这些变化是绵头雪莲花组织培养苗适应低温逆境的生理生化基础.  相似文献   

17.
In this study, twenty new anthranilic acid hydrazones 6 – 9 ( a – e ) were synthesized and their structures were characterized by Fourier-transform Infrared (FT-IR), Nuclear Magnetic Resonance (1H-NMR – 13C-NMR), and High-resolution Mass Spectroscopy (HR-MS). The inhibitory effects of the compounds against COX-II were evaluated. IC50 values of the compounds were found in the range of >200–0.32 μM and compounds 6e , 8d , 8e , 9b , 9c , and 9e were determined to be the most effective inhibitors. Cytotoxic effects of the most potent compounds were investigated against human hepatoblastoma (Hep-G2) and human healthy embryonic kidney (Hek-293) cell lines. Doxorubicin (IC50: 8.68±0.16 μM for Hep-G2, 55.29±0.56 μM for Hek-293) was used as standard. 8e is the most active compound, with low IC50 against Hep-G2 (4.80±0.04 μM), high against Hek-293 (159.30±3.12), and high selectivity (33.15). Finally, molecular docking and dynamics studies were performed to understand ligand-protein interactions between the most potent compounds and COX II, Epidermal Growth Factor Receptor (EGFR), and Transforming Growth Factor beta II (TGF-βII). The docking scores were calculated in the range of −10.609–−6.705 kcal/mol for COX-II, −8.652–−7.743 kcal/mol for EGFR, and −10.708–−8.596 kcal/mol for TGF-βII.  相似文献   

18.
以6叶期蚕豆(Vicia faba L.)幼苗为材料,用不同浓度钴(0、20、40、80、120mg·kg-1)土培处理14d,研究不同浓度钴处理对蚕豆体内钴的富集和分布特征,以及叶片光合色素含量、叶绿素荧光参数、光合作用参数、生长指标和POD、SOD、CAT活性的影响。结果显示:(1)蚕豆的根、茎、叶均能吸收一定量的钴,但不同器官间积累量有显著差异,并表现为根叶茎,且在不同钴浓度处理下根吸收量也存在显著差异。(2)不同浓度钴处理下,蚕豆叶片叶绿素(a、b)含量、气孔导度(Gs)、最大光化学效率(Fv/Fm)、PSⅡ潜在活性(Fv/F0)等参数与对照组相比表现出0~40mg·kg-1浓度下促进,40~120mg·kg-1浓度下抑制,而净光合速率(Pn)、胞间CO2浓度(Ci)以及光系统Ⅱ最小荧光(F0)、最大荧光(Fm)表现为在0~80mg·kg-1浓度下促进,80~120mg·kg-1浓度下抑制,蒸腾速率(Tr)和类胡萝卜素含量则在各浓度下一直表现为促进,并且以上光合作用相关参数与对照组相比都在40mg·kg-1浓度下促进作用达到最大。(3)蚕豆幼苗的根长、株高、生物量以及抗氧化酶POD、SOD和CAT活性均随着钴浓度增加表现出先升高后降低的趋势。研究表明,蚕豆的根、茎、叶均能积累钴,且吸收量有随土壤钴浓度增加而增加的趋势,但以根部的富集能力最强、积累量最大;低浓度钴可以诱导蚕豆中抗氧化酶活性增强,促进其叶片光合色素含量、光合作用效率提高和植株生长发育,而高浓度钴则表现出相反趋势,抑制蚕豆的光合效率和生长发育。  相似文献   

19.
Cestrum diurnum L. (Solanaceae) is a fragrant ornamental tree cultivated in different parts around the world. In this study, the essential oil (EO) of the aerial parts was extracted by hydrodistillation (HD), steam distillation (SD) and microwave-assisted hydro-distillation (MAHD). GC/MS analysis of the three EOs revealed that phytol represents the major component in SD-EO and MAHD-EO (40.84 and 40.04 %, respectively); while in HD-EO it only represented 15.36 %. The SD-EO showed a strong antiviral activity against HCoV-229E with IC50 of 10.93 μg/mL, whereas, MAHD-EO and HD-EO showed a moderate activity with IC50 values of 119.9 and 148.2 μg/mL, respectively. The molecular docking of EO major components: phytol, octadecyl acetate and tricosane showed a strong binding to coronavirus 3-CL (pro). Moreover, the three EOs (50 μg/mL) decreased the levels of NO, IL-6 and TNF-α and suppressed IL-6 and TNF-α gene expression in LPS-induced inflammation model in RAW264.7 macrophage cell lines.  相似文献   

20.
用营养液水培,研究了根际低氧胁迫下24-表油菜素内酯(EBR)对2个抗低氧能力不同的黄瓜品种根系中抗氧化系统及无氧呼吸酶活性的影响。结果表明,在低氧胁迫下,EBR处理显著提高了低氧胁迫下2品种黄瓜幼苗根系SOD、POD及ADH活性,降低了O2-·、H2O2和MDA含量、LDH活性及‘中农八号’根系PDC活性,而对‘绿霸春四号’根系PDC及2个品种CAT活性无明显影响,表明外源EBR处理通过促进低氧胁迫下根系中抗氧化酶和ADH活性的提高,降低LDH活性及ROS含量,增强植株抗低氧胁迫的能力。  相似文献   

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