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1.
《Pharmaceutical biology》2013,51(7):1052-1057
Abstract

Context: Leishmaniasis is a complex disease with a broad spectrum of clinical presentations.

Objective: We evaluated the anti-leishmanial effects of Nigella sativa L. (Ranunculaceae) against Leishmania tropica and Leishmania infantum with an in vitro model.

Materials and methods: Antileishmanial effects of essential oil and methanolic extract of N. sativa (0–200?µg/mL) and thymoquinone (0–25?µg/mL) on promastigotes of both species and their cytotoxicity activities against murine macrophages were evaluated using the MTT assay at 24, 48, and 72?h. Moreover, their leishmanicidal effects against amastigotes were investigated in a macrophage model, for 48 and 72?h.

Results: The findings showed that essential oil (L. tropica IC50 9.3?μg/mL and L. infantum IC50 11.7?μg/mL) and methanolic extract (L. tropica IC50 14.8?μg/mL and L. infantum IC50 15.7?μg/mL) of N. sativa, particularly thymoquinone (L. tropica IC50 1.16?μg/mL and L. infantum IC50 1.47?μg/mL), had potent antileishmanial activity on promastigotes of both species after 72?h. In addition, essential oil (L. tropica IC50 21.4?μg/mL and L. infantum IC50 26.3?μg/mL), methanolic extract (L. tropica IC50 30.8?μg/mL and L. infantum IC50 34.6?μg/mL), and thymoquinone (L. tropica IC50 2.1?μg/mL and L. infantum IC50 2.6?μg/mL) mediated a significant decrease in the growth rate of amastigote forms of both species. Thymoquinone (CC50 38.8?μg/mL) exhibited higher cytotoxic effects against murine macrophages than the other extracts.

Conclusion: N. sativa, especially its active principle, thymoquinone, showed a potent leishmanicidal activity against L. tropica and L.infantum with an in vitro model.  相似文献   

2.
《Pharmaceutical biology》2013,51(11):1677-1683
Abstract

Context: To date, there are no reports to validate the Indian traditional and folklore claims of Artemisia maderaspatana L. (syn. Grangea maderaspatana L.) (Asteraceae) for the treatment of Alzheimer’s disease.

Objective: The present study characterizes the volatile components (non-polar compounds) of A. maderaspatana and evaluates its acetylcholinesterase inhibition potential.

Materials and methods: The essential oils (yield 0.06% v/w) were obtained from fresh aerial part of A. maderaspatana. The characterization of volatile components (non-polar compounds) was performed by GC–MS data and with those of reference compounds compiled in the spectral library of in-house database. The in vitro acetylcholinesterase (AChE) inhibition of the volatile organic constituents (VOC’s) of A. maderaspatana aerial part was evaluated in varying concentration ranges (0.70–44.75?µg/mL) with Ellman’s method.

Results: The major components were α-humulene (46.3%), β-caryophyllene (9.3%), α-copaene (8.2%), β-myrcene (4.3%), Z(E)-α-farnesene (3.7%), and calarene (3.5%). Chemical variability among other Artemisia spp. from different climatic regions of India and countries namely Iran and France was observed. The experimental results showed that diverse volatile organic constituents of A. maderaspatana have significant acetylcholinesterase inhibitory activity (an IC50 value of 31.33?±?1.03?µg/mL). This is the first report on the inhibition of acetylcholinesterase properties of essential oil of A. maderaspatana obtained from fresh aerial part.

Conclusions: The present results indicate that essential oil of A. maderaspatana isolated from the northern region of India could inhibit AChE moderately. Therefore, the possibility of novel AChE inhibitors might exist in VOCs of this plant.  相似文献   

3.
分析中国沉香的挥发油成分,并测试其抗耐甲氧西林金葡菌活性。采用水蒸气蒸馏法提取中国沉香挥发油进行GC/MS分析,峰面积归一化法计算各成分相对含量,采用NIST05和WILEY275L数据库匹配,以及将质谱图与文献数据进行对照的方法进行鉴定。采用滤纸片琼脂扩散法测试挥发油抗菌活性。挥发油对耐甲氧西林金葡菌显示强活性。共检测到66个色谱峰,其中30个化合物得到鉴定,占挥发油总量的59.80%。26个化合物被鉴定为倍半萜类化合物,占挥发油总量的54.26%。β-沉香呋喃(8.96%),枯苏醇(7.82%),(-)-jinkoh-eremol(5.04%),沉香螺旋醇(4.53%),白木香呋喃酸(4.09%)为主要的倍半萜。4个降倍半萜和其他一些倍半萜,如10-表-γ-桉叶油醇,α-沉香呋喃,epi-ligulyl oxide等为首次从中国沉香中检出。本文首次报道了中国沉香挥发油对耐甲氧西林金葡菌具有抗菌活性。  相似文献   

4.
《Pharmaceutical biology》2013,51(7):888-892
Abstract

Context: Artemisia absinthium L. (Asteraceae) is an aromatic, herbaceous, perennial plant commonly known as wormwood. Artemisia absinthium is traditionally used as an anthelmintic, antiseptic, antispasmodic and for bacillary dysentery, cancers and neurodegenerative diseases.

Objective: The essential oil composition of the leaves of A. absinthium growing in the Western Ghats region of North West Karnataka, India, is investigated for the first time in this region and the oil was screened for antimicrobial properties.

Materials and methods: The chemical composition of the hydro-distilled essential oil obtained from the leaves of A. absinthium was analyzed by GC-FID and GC/MS. The oil was tested against five Gram positive and, eight Gram negative bacteria and three fungi by the tube-dilution method at a concentration range of 5000–9?µg/mL.

Results: Results demonstrated that the leave oil was found to be rich in oxygenated monoterpenes (39.7% and 41.1%). The major compounds were borneol (18.7% and16.7%), methyl hinokiate (11.9% and 12.9%), isobornyl acetate (4.0% and 4.7%), β-gurjunene (3.8% and 4.4%) and caryophyllene oxide (3.7% and 4.3%), among 64 identified compounds, comprising 91.7% and 90.1% of the total oil. The organism Micrococcus luteus was found more susceptible to the oil with an MIC value of 25?±?4?µg/mL, followed by Micrococcus flavus, Bacillus subtilis, Penicillium chrysogenum and Aspergillus fumigatus with MIC values of 58?±?8, 65?±?8, 84?±?15 and 91?±?13?µg/mL, respectively.

Discussion and conclusion: The oil showing antimicrobial activity against bacteria and fungi validate the traditional use of the plant as an antiseptic.  相似文献   

5.
Context: Pelargonium endlicherianum Fenzl. (Geraniaceae) roots and flowers are traditionally used in Turkey as a decoction treatment against intestinal parasites. Neither the chemical composition nor the potential bioactivity of the plant roots has been studied before.

Objectives: The phenolic content and effects of P. endlicherianum root extracts on antioxidant enzyme levels on A549 cells were studied for the first time.

Materials and methods: The chemical composition was analyzed via spectrophotometric and chromatographic (HPLC MS/MS and HPLC) techniques. The antioxidant activity was determined at different concentrations ranging from 0.001 to 2?mg/mL using DPPH? and ABTS?+ radical scavenging activity, β-carotene-linoleic acid co-oxidation assay, protection of 2-deoxyribose and bovine brain-derived phospholipids against a hydroxyl radical-mediated degradation assay. Glutathione peroxidase and superoxide dismutase activities were also studied as well as the effects of the extracts on nitric oxide levels on IL-1β stimulated A549 cells.

Results: The key parameters for the most active ethyl acetate extract included the following: DPPH? IC50: 0.23?mg/mL, TEAC/ABTS: 2.17?mmol/L Trolox, reduction: 0.41?mmol/g AsscE, and protection of lipid peroxidation IC50: 0.05?mg/mL. Furthermore, the ethyl acetate extract increased the SOD level significantly compared to control group (4.48?U/mL) at concentrations of 100 and 200?μg/mL SOD, 5.50 and 5.67?U/mL, respectively. Apocynin was identified as the major component, and the ethyl acetate fraction was found to be rich in phenolic compounds.

Discussion and conclusion: Pelargonium endlicherianum root extracts displayed antioxidant activity and increased the antioxidant enzyme levels in IL-1β stimulated A549 cells, while decreasing the NO levels.  相似文献   

6.
《Pharmaceutical biology》2013,51(6):643-650
The antioxidant, antiplatelet, and cytoxoxic effects of seven South African plant extracts, namely, Combretum vendae A.E. van Wyk (Combretaceae), Commiphora harveyi (Engl.) Engl. (Burseraceae), Khaya anthotheca (Welm.) C.DC (Meliaceae), Kirkia wilmsii Engl. (Kirkiaceae), Loxostylis alata A. Spreng. ex Rchb. (Anacardiaceae), Ochna natalitia (Meisn.) Walp. (Ochnaceae), and Protorhus longifolia (Bernh. Ex C. Krauss) Engl. (Anacardiaceae), were evaluated using established in vitro assays. All the extracts showed comparably low toxicity except for the extract of C. harveyi that showed high hemagluttination assay titer value, which indicates toxicity. The extracts of P. longifolia, K. wilmsii, O. natalitia, L. alata, C. harveyi, and C. vendae exhibited antioxidant properties in the qualitative assay using DPPH. In the quantification of antioxidation using ABTS, only the extracts of P. longifolia, L. alata, and C. vendae showed antioxidant activity with respective TEAC values of 1.39, 1.94, and 2.08. Similarly, in the quantitative DPPH assay, L. alata (EC50, 3.58?±?0.23?µg/mL) and K. wilmsii (EC50, 3.57?±?0.41?µg/mL) did not differ significantly (p?≤?0.05) from the control. K. anthotheca showed a higher EC50 (176.40?±?26.56?µg/mL) value, and differed significantly (p?≤?0.05) from all the other extracts and control. In addition, the extracts of C. vendae and C. harveyi showed significant (p?≤?0.05) antiplatelet activity and did not differ from the control (aspirin) with EC50 of 0.06?±?0.01?µg/mL and 0.19?±?0.00?µg/mL, respectively. Lower EC50 values in the antioxidant and antiplatelet studies are indicative of superior activity of the plant extract against oxidation and platelet aggregation.  相似文献   

7.
In our ongoing search for bioactive constituents, a new sesquiterpene polyol ester, named triptersinine U (1), together with five known triterpenes (2–6) and seven sesquiterpene pyridine alkaloids (7–13), were isolated from the roots of Tripterygium wilfordii Hook. f. Their chemical structures were elucidated using extensive spectroscopic analyses, including 1D and 2D NMR, and HRESIMS, as well as comparison with previously reported data. Cytotoxic activities of all compounds 1–13 were evaluated against six human tumor cell lines (HepG2, Hep3B, Bcap37, U251, MCF-7 and A549) using the MTT in vitro assay. The results showed that triterpenes exhibited moderate cytotoxic activities toward the tested cell lines.  相似文献   

8.
肯尼亚没药挥发油化学成分研究   总被引:5,自引:1,他引:4  
利用气相色谱-质谱和气相色谱-红外光谱联机分析技术对中药没药挥发油进行了分离研究,证明其主要成分是单萜和倍半萜。共鉴定出16个化合物。  相似文献   

9.
目的:鉴定沙美特罗在小鼠尿中的主要代谢产物.方法:ig给药后,收集小鼠尿液,经固相提取,葡萄糖醛酸酶水解,进行LC/MS/MS分析和硅烷化后进行GC/MS分析同时分离鉴定沙美特罗代谢产物.结果和结论:在给药后尿样中发现沙美特罗原型和4种代谢产物M1~M4,其结构推测为19-羟基沙美特罗(M1)、2-羰基沙美特罗(M2)、19-羰基沙美特罗(M3)和19-羟基-8-甲氧基沙美特罗(M4).  相似文献   

10.
Abstract

In the current study, we evaluated the activity of extracts and (-)mammea A/BB from the leaves of Calophyllum brasiliense. Camb. (Clusiaceae), against Leishmania braziliensis.. The dichloromethane extract and the coumarin (-)mammea A/BB showed significant activity against the promastigote forms of L. braziliensis., with a 50% lethal dose (LD50) at concentrations of 60 and 23.2 μ g/mL, respectively. However, the aqueous extract from the leaves and amentoflavone showed no activity against promastigote forms. For the intracellular amastigote form, the dichloromethane extract and the coumarin (-)mammea A/BB reduced by 50% the infection index of parasites in macrophages at concentrations of 22 and 29 μ g/mL, respectively. In addition, the dichloromethane extract did not show cytotoxic effects against mouse peritoneal macrophages at concentration up to 1000 μ g/mL. On the other hand, the coumarin (-)mammea A/BB showed more cytotoxicity than the dichloromethane extract. The compounds were characterized by one and two-dimensional 1H and 13C NMR analyses, and LC/UV/MS was used to identify (-)mammea A/BB and amentoflavone in the dichloromethane extract. These results provide new perspectives on the development of novel drugs with leishmanicidal activities obtained from natural products.  相似文献   

11.
代谢组学分析技术平台和数据处理的新进展   总被引:1,自引:0,他引:1  
分析技术和生物计量学促进了代谢组学的飞速发展。代谢组学快速、灵敏、可定量、非侵入性以及系统性的特点,使其在新药研发、药物毒性筛选、疾病诊断等领域显示出广阔的前景。本文综述了代谢组学研究中的某些关键问题:样品处理方法,分析技术和数据处理的方法和原则,代谢组动态变化、生物标记物的鉴定和代谢途径的检索近年来的进展。评价了各种分析手段的优缺点,并展望代谢组学发展前景。  相似文献   

12.
《Pharmaceutical biology》2013,51(10):1293-1297
Abstract

Context. Cymbopogon winterianus Jowitt ex Bor (Poaceae), known as citronella grass, is an aromatic herbaceous plant and the essential oil extracted from this grass is used in cosmetics, perfumes, hygiene and cleanliness products worldwide.

Objective: This study investigated the composition and molluscicidal and larvicidal activities of the essential oil of C. winterianus cultivated in North Brazil.

Materials and methods: The oil was obtained by hydrodistillation, analyzed by gas chromatography (GC) and GC-mass spectrometry and then its molluscicidal and larvicidal activities against snails (Biomphalaria glabrata) and hatched larvae of Artemia salina, respectively, were evaluated at concentrations from 10 to 1000?mg/L.

Results: The main constituents of oil were citronellal (26.5%), geraniol (16.2%), elemol (14.5%) and citronellol (7.3%). The molluscicidal test revealed significant lethal concentration (LC) values (LC90?=?97.0?mg/L, LC50?=?54.0?mg/L and LC20?=?22.0?mg/L), indicating the presence of molluscicidal compounds in the oil. In addition, the oil showed moderate larvicidal activity (LC50?=?181.0?mg/L) against the larvae of A. salina, which could justify its use in the aquatic environment without affecting other living organisms.

Discussion and conclusion: The results suggest that the oil of C. winterianus could be an effective alternative to control schistosomiasis, with an average margin of safety to other living organisms that coexist with snails.  相似文献   

13.
山东金银花鲜花挥发油化学成分的研究   总被引:3,自引:2,他引:1  
采用气相色谱—质谱法(GC/MS)对山东金银花主流品种大毛花鲜花挥发油的化学成分进行了分析,共分析鉴定出不在此列(王古)(王巴)烯芳樟醇等47种化合物,占全部挥发油总含量的92.70%。并测定了各成分在挥发油中的百分含量。  相似文献   

14.
Context: Eucalyptus cinerea F. Muell. ex Benth. (Myrtaceae) is a medium-sized tree cultivated in Egypt.

Objective: First, to determine the chemical composition of the volatile oil of the juvenile leaves and stems of E. cinerea to identify its chemotype. Second, to study the in vivo antioxidant activity and in vitro antimicrobial activity of the studied volatile oils against selected Gram-positive, Gram-negative bacteria, yeast, and mycelia fungi.

Materials and methods: The volatile oil was prepared by hydrodistillation and then identified by GC/MS analysis. Broth microdilution and agar dilution methods were applied for determining the MIC. The antioxidant activity was studied by determination of glutathione level in blood of alloxan-induced diabetic rats.

Results: The yield of the volatile oil hydrodistilled from the juvenile leaves and stems of E. cinerea was 4.5 and 0.5%, respectively. 1,8-Cineole was the major identified oxygenated monoterpenoid (84.55% and 60.15% in the juvenile leaves and stems, respectively). The antibacterial activity of the oil of the juvenile leaves was more potent against all the tested organisms than that of the stems. The (MIC) of volatile oil of the juvenile leaves against Escherichia coli, Pseudomonas aeruginosa, Streptococcus faecalis, Candida albicans, and Aspergillus flavus were 5.2, 5.6, 4, 4.8, and 12.8?μg/ml, respectively. Also, the juvenile leaves’ oil was more active as an antioxidant than that of the stems. They restored glutathione level by 33.7?±?1.1 and 29.6?±?0.7?mg/dl, respectively, compared with vitamin E (35.9?±?1.2?mg/dl) which was used as a reference.

Discussion and conclusion: Results suggest that the volatile oil is 1,8-cineole chemotype. Moreover, the oil of the juvenile leaves of E. cinerea might find usefulness as a therapeutic agent following further development.  相似文献   

15.
《Pharmaceutical biology》2013,51(7):756-763
Context: Crocus sativus Linn. (Iridaceae), commonly known as saffron, becomes more and more popular due to its versatile biological and medicinal properties. At present, studies mainly focus on the traditional medicinal part, the saffron stigma, with less attention to the other parts of saffron, such as the perianth, the stamen, and the corm, which are high yield compared to the stigma and also possess various pharmacological effects.

Objective: To determine the chemical compositions, antifungal, cytotoxic, and antioxidant activities of the ether fractions from the stamen, perianth, and stigma of saffron.

Materials and methods: The chemical constituents of the ether fractions from different parts of saffron were investigated by gas chromatography/mass spectrometry. Several pathogenic fungi isolates and tumor cell lines were employed to evaluate the antifungal and cytotoxic activities of these three ether fractions. 1,1-Diphenyl-2-picrylhydrazyl assay was used to determine the free radical-scavenging activity.

Results: The ether fractions composition of the three C. sativus parts are different from each other, but lauric acid, hexadecanoic acid, 4-hydroxydihydro-2(3H)-furanone, and stigmasterol were the common constituents shared by all the three fractions. The stamen ether fraction displayed the strongest antifungal and cytotoxic activities, whereas both of the saffron stamen and perianth ether fractions exhibited significant antioxidant activities.

Discussion and conclusion: These findings demonstrate that the saffron stamen and perianth possess significant antifungal, cytotoxic, and antioxidant activities as well as the stigma, though not to the same extent, prompting us to expand the medicinal resource and make best use of this valuable plant.  相似文献   

16.
The chemical composition of the essential oil and methanol extract of Calycotome villosa (Poiret) Link leaves collected in Sardinia (Italy) has been studied by analytical and spectroscopic methods. Falcarinol and some alcohols, terpenes, furan derivatives, and paraffins have been isolated from the essential oil. Thirteen alkaloids and falcarinol have been identified in the chloroform fraction of the basic methanol extract. Six flavonoids and four anthraquinones have been isolated in the chloroform fraction after acidification of the basic methanol extract. The cytotoxic and antimicrobial activities have also been evaluated. The essential oil, the methanol extract in toto, and the fraction of the basic extract showed strong cytotoxicity, whereas the fraction of the acid extract showed lower cytotoxicity. Furthermore, this fraction showed good antibacterial activity against Staphylococcus aureus, Bacillus lentus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Providencia rettgeri, and Morganella morganii. It can therefore be stated that this plant's cytotoxicity is prevalently due to falcarinol.  相似文献   

17.
蓖麻壳水提液的镇痛作用及其成分分析   总被引:1,自引:0,他引:1  
目的:研究蓖麻壳水提液的镇痛作用和主要成分的 HPLC 及质谱联用技术分析。方法:以啮齿动物的疼痛模型热板试验和乙酸扭体试验对蓖麻壳的水提液的镇痛进行了评价并利用高效液相色谱/质谱联用技术对浸提液的主要成分进行了分析。结果:小鼠 IP 蓖麻壳水提液组比对照组的扭体次数显著性减少和热板耐受时间显著性增加并有镇痛抑制率和耐受力随剂量增加而显著性提高(P<0.001)。利用 HPLC 和 HPLC/MS 联用技术分析蓖麻壳水提液其主要成分为蓖麻碱。结论:蓖麻壳水提液的活性成分可以明显抑制化学性刺激和热刺激所致的小鼠痛反应,有可能是多模式镇痛,减弱中枢神经系统接收到的疼痛信号和抑制外周疼痛信号。  相似文献   

18.
《Pharmaceutical biology》2013,51(9):920-926
Context: Tanacetum parthenium Schultz Bip. (Asteraceae) is an aromatic perennial plant, widely distributed in the northern hemisphere. This species traditionally has been used in insecticides, cosmetics, balsams, dyes, medicines and preservatives.

Material and methods: The essential oil of T. parthenium was obtained by hydrodistillation in three developmental stages and analyzed by gas chromatography-mass spectrometry. The antibacterial activity of the oils was investigated against four Gram-positive and four Gram-negative bacteria. The oil was tested for cytotoxicity against THP-1 cells using the Trypan blue assay.

Results: Twenty-nine components were identified in the essential oil; the highest amount was extracted at the flowering stage. The main component, in the flowering stage, was camphor (18.94%) and other major components were bornyl acetate (18.35%), camphene (13.74%), bornyl isovalerate (3.15%), borneol (10.93%), juniper camphor (6.23%) and β-eudesmol (2.65%). Minimum inhibitory concentration of essential oil was evaluated from 4 µL mL?1 against Staphylococcus subtilis to 38 µL mL?1 against Entrobacter aerogenes. Toxicity assay showed that the oil has no significant toxicity at 5–15% v/v concentrations on THP-1 cells.

Discussion and conclusion: This study demonstrates the occurrence of camphor/bornyl acetate chemotype of T. parthenium in western regions of Iran. The finding showed also the studied oils have relatively good antibacterial activity without significant toxicity, thus have great potentiality to be used as natural health product.  相似文献   

19.
Daphne gnidium L. (Thymelaeaceae) is an evergreen shrub from the Mediterranean area traditionally used for its medicinal and non-medicinal properties. Several studies showed its adverse impact on different targets including malignant cells, microbes, radicals, insects. The negative interactions between D. gnidium and other plant species have been rather neglected so far, as well as its chemical volatile composition. Therefore, this work aimed to assess the phytotoxic activity of D. gnidium on filter paper and soil in pre-emergence conditions by testing both the aqueous extract (10–100%) and the powder (0.25–1 g) obtained from the leaves as bioagrochemicals. The results showed that D. gnidium was able to significantly decrease seed germination and growth parameters of the receiver plants with different effectiveness (p-values < 0.05). Overall, Sinapis alba L. (Brassicaceae) was the most susceptible species followed by Lolium multiflorum Lam. (Poaceae) and Trifolium incarnatum L. (Fabaceae) while aqueous extract was more active than the powder. Solid-Phase Microextraction (SPME) sampling technique and Gas Chromatograph/Mass spectrometer (GC/MS) analyses were used to characterize the volatile fraction highlighting considerable differences in the composition of the analyzed samples. Hexahydrofarnesyl acetone (29.7%) followed by 3,7,11,15-tetramethyl-2-hexadecen-1-ol (28.3%) and β-damascenone (32.0%) followed by eudesma-1,4(15), 11-triene (27.1%) were detected as main volatile compounds of the powder and the aqueous extract, respectively.  相似文献   

20.
丁香罗勒油气相色谱与气质联用分析   总被引:5,自引:0,他引:5  
目的 :建立丁香罗勒油中丁香酚的含量测定方法和鉴定挥发性化学成分。方法 :气相色谱法 ,4mm× 2m不锈钢柱 ,10 %SE 30为固定液 ,ChromosorbWAW 6 0 80目担体 ,FID检测器 ,柱温 110℃ ,水杨酸甲酯为内标物 ;气质联用 ,以HP 5毛细管柱 ,柱温起始 12 0℃保持 5min后以 5℃ .min-1升温至 15 0℃保持 7min ,检测质荷比范围 10~ 42 5。结果 :丁香酚在 2~ 10mg .mL-1范围内具良好线性关系 ,平均加样回收率为 10 0 .0 8% ,RSD为 0 .95 % ;气质联用鉴定了 39个化合物。结论 :方法简便 ,快速 ,准确 ,可排除其它成分的干扰。  相似文献   

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