高温环境对川芎挥发油化学成分的影响研究

目的:考察高温环境对川芎挥发油化学成分的影响,明确川芎"散气走味"物质基础。方法:川芎在40℃环境下放置0、5、10 d,用水蒸气蒸馏法提取挥发油,采用GC-MS对其化学组分进行分析比较。结果:5 d后川芎挥发油中化合物数目增加,10 d后化合物数目减少,化学成分变化明显,主要是桧烯、萜品烯、萜品油烯、萜品醇等烯萜类化合物减少。结论:高温会引起川芎挥发油成分变化,川芎在贮藏过程中"散气走味"变质现象的物质基础可能是烯萜类和苯酞类成分。     

川芎挥发性成分的水蒸气蒸馏提取与顶空进样GC-MS分析

目的:分析比较不同提取方法制备的川芎中挥发性成分。方法:分别采用顶空进样法和水蒸气蒸馏法制备川芎挥发油,并对其进行气相色谱-质谱(GC-MS)分析。结果:两种方法制备的川芎挥发油的化学成分类型和相对含量有所差异,顶空进样法制备的挥发油含29个化学成分,其中烯萜类成分占挥发油总量76%,苯酞类成分占挥发油总量的16%。水蒸气蒸馏法制备的挥发油共鉴定出32个化合物,烯萜类占挥发油总量的4.50%,苯酞类占挥发油总量的88%。结论:两种提取方法,分别提供了不同沸点川芎挥发油的化学信息,运用这两种方法可建立更全面的川芎挥发性成分GC-MS信息。     

国家中药材GAP基地产川芎挥发油化学成分的GC-MS分析

目的:研究国家中药材GAP基地"川芎GAP都江堰示范基地"种植川芎挥发油的化学成分,为其质量控制和标准制定提供科学依据。方法:采用水蒸气蒸馏法提取挥发油,GC毛细管柱色谱法进行分析,归一化法测定其相对含量,气相色谱-质谱联用技术辅助人工检索鉴定其化学成分。结果:检出142个色谱峰,鉴定了62个化合物,占挥发油总量的87.36%。总结了川芎挥发油中苯酞类化合物及其衍生物的质谱裂解规律,主要存在侧链断裂脱烯/烃和开环脱水再脱羰基两个电子轰击裂解途径。并以此为依据,推测了4,5-二氢-3,1′-二羟基-3-戊基苯酞的结构。结论:"川芎GAP都江堰示范基地"种植川芎挥发油的主要化学成分为苯酞类化合物及其衍生物;4,5-二氢-3,1′-二羟基-3-戊基苯酞为新的化合物。     

β-环糊精包合茶芎挥发油的工艺条件优化研究

茶芎为伞形科植物茶芎(Ligusticum SinenseO liv.CV.Chaxiong)的根茎,是江西特产中药。茶芎挥发油是茶芎的根茎经水蒸气蒸馏提取所得到的挥发油。药理实验表明,茶芎挥发油对心血管、子宫平滑肌等均有明显的生理活性,还有很好的抗惊厥作用,且毒性较低。茶芎挥发油中含苯酞类成分约90%,由于苯酞类成分易氧化聚合,使折光率、比重和色泽均发生明显改变,因而严重影响茶芎挥发油的稳定性[1],不利于其开发和利用。本文采用饱和溶液法制备茶芎挥发油β-环糊精包合物,以提高茶芎挥发油的稳定性。按照β-环糊精包合茶芎挥发油的最佳配料比[2],以包…     

茶芎挥发油-β-环糊精包合物的制备

本文报道了用饱和水溶液法制备茶芎挥发油-β-环糊精包合物,并经红外光谱分析,证实β-环糊精能将茶芎中挥发油成分包合,将有利于提高茶芎挥发油的稳定性。     

茶芎挥发油—β—环糊精包合物制备

本文报道了用饱和水溶液法制备茶芎挥发油β－环糊精包合物，并经红外光谱分析，证实β－环糊精能将茶芎中挥发油成分包合，将有利于提高茶芎挥发油的稳定性。     

炮制对川芎有效成分的影响

对川芎及其炮制品进行了挥发油、阿魏酸的含量测定，比较了川芎炮制前后挥发油组成的变化。为探讨川芎炮制意义，提供了一定的实验依据。     

新鲜和干燥川芎根、茎、叶、花挥发油的GC⁃MS分析

目的对新鲜和干燥川芎根、茎、叶、花挥发油进行GC?MS分析。方法采用挥发油提取器提取新鲜和干燥川芎不同部位的挥发油,结合GC?MS分析鉴定其化学成分及相对含量。结果共分离鉴定出47种成分,主要由苯酞类和萜烯类组成;新鲜和干燥川芎挥发油总体相差不大,干燥后川芎挥发油中藁本内酯相对含量稍有增加;干燥川芎根、茎、叶、花挥发油中相同成分共16种,相对含量最高的均为藁本内酯和新川芎内酯;干燥根挥发油中苯酞类成分相对含量明显高于茎、叶、花,萜烯类成分相对含量明显低于茎、叶、花。结论干燥过程或可有益于川芎药效的发挥;川芎不同部位挥发油有一定的共性,但与根相比,同一类成分相对含量在茎、叶、花挥发油中较大差异。     

计算机在初均速法预测茶芎挥发油稳定性中的应用

中药茶芎是江西特产中药之一.茶芎香气非常浓郁,挥发油含量较高.茶芎挥发油含苯酞类成分90%左右[1].但苯酞类成分容易氧化聚合,使折光率数值改变,引起茶芎挥发油不稳定[2].本实验采用初均速法[3]预测其稳定性.采用power Builder语言编制出计算程序,将实验数据输入计算机进行运算,结果显示出Arrhenius图,建立了直线回归方程,y=-8673.6818x 17.07,预测出茶芎挥发油的活化能和稳定性.     

用初均速法测定茶芎挥发油的稳定性

以水蒸汽蒸馏法提取茶芎挥发油,应用初均速法预测茶芎挥发油的稳定性。选择了九个温度进行了恒温加速试验,于阿贝折射仪上测定了茶芎挥发油的折光率数值。用作图法和数理统计法处理结果,建立了直线回归方程Ｙ＝－８６７３．６８１８ｘ＋１７．０７０３标出了直线相关系数ｒ＝－０．９９０,预测了茶芎挥发油的稳定性,ｔ０．９＝２．０３ａ;ｔ０．８＝４．２９ａ;ｔ０．７＝６．８６ａ。     

基于网络药理学探讨辛热中药挥发油外用的药效物质基础及潜在分子机制

目的基于网络药理学分析辛热中药挥发油外用的药效物质基础及潜在分子机制。方法采用气相色谱-质谱联用技术分析高良姜Alpiniae Officinarum Rhizoma、干姜Zingiberis Rhizoma、肉桂Cinnamomi Cortex、吴茱萸Euodiae Fructus、胡椒Piperis Fructus 5种辛热中药挥发油的质量分数,并与防风Saposhnikoviae Radix等10味辛温中药挥发油进行比较,得到差异倍半萜类化合物;采用中药系统药理学数据库与分析平台(TCMSP)和SwissTargetPrediction数据库对差异倍半萜类化合物进行靶点预测,采用TIGER数据库筛选在皮肤中表达的蛋白,用Cytoscape 3.7.0软件建立"药材-成分-靶点"网络,并用STRING数据库建立潜在关键靶点的蛋白质-蛋白质互作(protein-protein interaction,PPI)网络。结果辛热中药挥发油中倍半萜类成分质量分数高于辛温中药挥发油,倍半萜类成分在辛热中药挥发油外用给药时更倾向于滞留在皮内,是决定透皮促渗能力的关键成分,可能为辛热中药挥发油的关键物质基础。"药材-成分-靶点"网络及PPI结果表明辛热中药挥发油外用主要涉及产热相关的核受体共激活蛋白2(nuclear receptor coactivator 2,NCOA2)靶点及脂代谢相关的过氧化物酶体增殖剂激活受体α(peroxisome proliferator-activated receptorα,PPARA)、类视黄酸X受体α(retinoic acid X receptorα,RXRA)、NCOA2靶点及抗炎相关的前列腺素内过氧化物合酶1(prostaglandinG/Hsynthase1,PTGS1)、PTGS2、白细胞介素-6(interleukin-6,IL-6)靶点,提示产热、减脂、抗炎为辛热中药挥发油倍半萜类成分的主要药理作用。结论β-石竹烯、α-muurolene、吉马烯、β-榄香烯、δ-榄香烯、β-芹子烯、α-胡椒烯等倍半萜类成分为辛热中药挥发油的特征组分,可能通过作用于PPARA-RXRA-NCOA2信号轴及PTGS2、PTGS1、IL-6等炎性因子,从而产生产热、减脂、抗炎等作用。     

A possible role of partially pyrolysed essential oils in Australian Aboriginal traditional ceremonial and medicinal smoking applications of Eremophila longifolia (R. Br.) F. Muell (Scrophulariaceae)

Ethnopharmacological significance

Eremophila longifolia is one of the most respected of the traditional medicines used by Australian Aboriginal people. Customary use involves smoldering the leaves over hot embers of a fire to produce an acrid smoke, believed to have therapeutic effects broadly consistent with antimicrobial, antifungal and anti-inflammatory capacity.

Aim of the study

The current study aims to examine the contribution of partially pyrolysed and non-pyrolysed essential oils in traditional usage of Eremophila longifolia.

Materials and methods

Non-pyrolysed and partially pyrolysed essential oils were produced by hydrodistillation and part-wet/part-dry distillation, respectively. All samples were tested for antimicrobial activity by broth dilution. Some of these samples were further treated to an incrementally stepped temperature profile in a novel procedure employing a commercial thermocycler in an attempt to mimic the effect of temperature gradients produced during smoking ceremonies. Components from the pyrodistilled oils were compared with the non-pyrodistilled oils, using GC–MS, GC-FID and HPLC-PAD. The 2,2-diphenyl-1-picrylhydrazyl method, was used to compare free radical scavenging ability.

Results

Partially pyrolysed oils had approximately three or more times greater antimicrobial activity, enhanced in cultures warmed incrementally to 60 °C and held for 30 s and further enhanced if held for 2 min. Partially pyrolysed oils showed a radical scavenging capacity 30–700 times greater than the corresponding non-pyrolysed oils. HPLC-PAD revealed the presence of additional constituents not present in the fresh essential oil.

Conclusion

These results, by showing enhanced antimicrobial and antioxidant activities, provide the first known Western scientific justification for the smoking ceremonies involving leaves of Eremophila longifolia. During customary use, both partially pyrolysed as well as non-pyrolysed essential oils may contribute significantly to the overall intended medicinal effect.     

Antigenotoxic and antioxidant activities of palmarosa and citronella essential oils

Ethnopharmacological relevance

Essential oils of palmarosa and citronella have been extensively used in ancient Indian and South-east Asian traditional medicines.

Aim of the study

These essential oils have been reported to exhibit antimicrobial, anti parasitic effects against bacteria, yeasts, filamentous fungi, and viruses. In the present study the oils were tested for their potential antigenotoxic and antioxidant properties in human lymphocyte cells.

Materials and methods

The antigenotoxic effect on human lymphocyte cells (measurement of cell viability, DNA damage) was studied using trypan blue dye exclusion test, plasmid pBR322 DNA strand scission, and comet assay. Anti-oxidant activity was evaluated by DPPH⁺ free radical scavenging and lipid peroxidation assay.

Results

The essential oils showed a good antigenotoxic activity against methyl methanesulphonate (MMS) and hydrogen peroxide. In addition, a significant dose dependent antioxidant activity was observed.

Conclusion

Our data provide evidence that support the usage of palmarosa and citronella essential oils in traditional herbal preparations. They can constitute a natural source of a new and safe antioxidant.     

Effect of Brazilian copaiba oils on Leishmania amazonensis

Ethnopharmacological relevance

Copaiba oil has been used in folk medicine since the 19th century. The use of copaiba oils to treat leishmaniasis is cited in several ethnopharmacological studies. Nevertheless, the potential antileishmania of copaiba oils had not been studied.

Aim of the study

Eight different kinds of Brazilian copaiba oils were screened for antileishmanial activity.

Materials and methods

The antiproliferative effect of copaiba oil on promastigote and amastigote axenic were determined. To determine the survival index peritoneal macrophage were infected with promastigotes of Leishmania amazonensis and treated with copaiba oil. The cytotoxic effect of copaiba oil was assessed on macrophage strain J774G8 by assay of sulforhodamine B.

Results

Copaiba oils showed variable levels of activity against promastigote forms with IC₅₀ values in the range between 5 and 22 μg/mL. The most active oil was that from Copaifera reticulata (collected in Pará State, Brazil) with IC₅₀ values of 5, 15, and 20 μg/mL for promastigote, axenic amastigote and intracellular amastigote forms, respectively. Amphotericin B showed IC₅₀ of 0.058 and 0.231 μg/mL against promastigote and amastigote forms, respectively. Cytotoxicity assay showed that this copaiba oil obtained from Copaifera reticulata showed low cytotoxicity against J774G8 macrophages.

Conclusion

Copaiba oils showed significant activity against the parasite Leishmania amazonensis.     

Appraisal on the wound healing and anti-inflammatory activities of the essential oils obtained from the cones and needles of Pinus species by in vivo and in vitro experimental models

Ethnopharmacological relevance

According to ethnobotanical data, Pinus species have been used against rheumatic pain and for wound healing in Turkish folk medicine.Essential oils from the cones and needles of five different Pinus species (Pinus brutia Ten., Pinus halepensis Mill., Pinus nigra Arn., Pinus pinea L. and Pinus sylvestris L.) were evaluated for their in vivo wound healing and anti-inflammatory activities.

Materials and methods

In vivo wound healing activity of the ointments prepared from essential oils was evaluated by linear incision and circular excision experimental wound models subsequently histopathological analysis and hydroxyproline content. Furthermore, the essential oils were screened for anti-hyaluronidase activity. Additionally anti-inflammatory activity was assessed by using the method of Whittle, which is based on the inhibition of acetic acid-induced increase in capillary permeability.

Results

The essential oils obtained from the cones of Pinus pinea and Pinus halepensis demonstrated the highest effects on the wound healing activity models. On the other hand, the rest of the essential oils did not show any significant wound healing and anti-inflammatory activities.

Conclusion

The experimental study revealed that essential oils obtained from the cones of Pinus pinea and Pinus halepensis display remarkable wound healing activity.     

Antidepressant-like effect of Salvia sclarea is explained by modulation of dopamine activities in rats

Aim of the study

The purpose of the present study was to screen aromatic essential oils that have antidepressant effects to identify the regulatory mechanisms of selected essential oils.

Materials and methods

The antidepressant effects of essential oils of Anthemis nobilis (chamomile), Salvia sclarea (clary sage; clary), Rosmarinus officinalis (rosemary), and Lavandula angustifolia (lavender) were assessed using a forced swim test (FST) in rats. Rats were treated with essential oils by intraperitoneal injection or inhalation. Serum levels of corticosterone were assessed by enzyme-linked immunosorbent assay (ELISA).

Results

Among the essential oils tested, 5% (v/v) clary oil had the strongest anti-stressor effect in the FST. We further investigated the mechanism of clary oil antidepression by pretreatment with agonists or antagonists to serotonin (5-HT), dopamine (DA), adrenaline, and GABA receptors. The anti-stressor effect of clary oil was significantly blocked by pretreatment with buspirone (a 5-HT_1A agonist), SCH-23390 (a D₁ receptor antagonist) and haloperidol (a D₂, D₃, and D₄ receptor antagonist).

Conclusions

Our findings indicate that clary oil could be developed as a therapeutic agent for patients with depression and that the antidepressant-like effect of clary oil is closely associated with modulation of the DAnergic pathway.     

Cytotoxicity and antibacterial activity of Lindera strychnifolia essential oils and extracts

Aim of the study

Lindera strychnifolia (LS) is widely used in traditional Chinese medicine. In the present study, we investigated cytotoxicity and antibacterial activity of essential oils and various fractions of ethanol extract of LS to explore the active components of LS and their pharmacological effects.

Materials and methods

The in vitro cytotoxicities of essential oils and various solvent fractions of LS on three human cancer cell lines (A549, HeLa and Hep G2) and a non-cancerous cell line (HUVEC) were examined using a modified MTT assay. And by using agar disc diffusion and broth microdilution methods, the antibacterial activity of these samples was evaluated against 10 bacteria including 5 clinically isolated strains. The compositions of the essential oils from the leaves and roots of LS were also analyzed by GC and GC–MS.

Results

The leaf oil showed the strongest cytotoxicity on the cancer cell lines tested with the IC₅₀ values ranged from 22 to 24 μg/ml after 24 h of treatment. The most sensitive microbial strain to all the samples was Staphylococcus aureus ATCC 25923.

Conclusions

Our results showed that the essential oils of LS exhibited greater cytotoxicity and antibacterial activity than the solvent fractions of ethanol extract of LS.     

Antioxidant,antimicrobial and toxicological properties of Schinus molle L. essential oils

Ethnopharmacological relevance

Schinus molle L. has been used in folk medicine as antibacterial, antiviral, topical antiseptic, antifungal, antioxidant, anti-inflammatory, anti-tumoural as well as antispasmodic and analgesic; however, there are few studies of pharmacological and toxicological properties of Schinus molle essential oils. The aim of this study was to evaluate the antioxidant and antimicrobial activities of Schinus molle leaf and fruit essential oils, correlated with their chemical composition and evaluate their acute toxicity.

Materials and methods

The chemical composition of Schinus molle leaf and fruit essential oils were evaluated by GC-FID and GC–MS. Antioxidant properties were determined using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) free radical and β-carotene/linoleic acid methods. Antimicrobial properties were evaluated by the agar disc diffusion method and minimal inhibitory concentration assay. Toxicity in Artemia salina and acute toxicity with behavioural screening in mice were evaluated.

Results

The dominant compounds found in leaf and fruit essential oils (EOs) were monoterpene hydrocarbons, namely α-phellandrene, β-phellandrene, β-myrcene, limonene and α-pinene. EOs showed low scavenging antioxidant activity by the DPPH free radical method and a higher activity by the β-carotene/linoleic acid method. Antimicrobial activity of EOs was observed for Gram+, Gram− pathogenic bacteria and food spoilage fungi. EOs showed totoxicity for Artemia salina and lower toxicity in Swiss mice.

Conclusions

The result showed that EOs of leaves and fruits of Schinus molle demonstrated antioxidant and antimicrobial properties, suggesting their potential use in food or pharmaceutical industries.     

Biofilm inhibition by Cymbopogon citratus and Syzygium aromaticum essential oils in the strains of Candida albicans

Ethnopharmacological relevance

Oils of Cymbopogon citratus and Syzygium aromaticum have been used in traditional medicine to treat fungal infections of skin, mouth, urinary and vaginal tract in Asian countries particularly India and other developing countries.

Aim of the study

To evaluate essential oils of Cymbopogon citratus and Syzygium aromaticum for their anti-biofilm activity against strong biofilm forming strains of Candida albicans.

Materials and methods

XTT reduction assay, Time kill assays, light microscopy and scanning electron microscopy (SEM) were employed to determine the effect of test oils on the Candida albicans biofilms.

Results

Most of the Candida albicans strains tested displayed formation of moderate to strong biofilms. Preformed Candida biofilms showed ≥1024 times increased resistance to antifungal drugs, 2 times to Syzygium aromaticum, but no increased tolerance for Cymbopogon citratus. Test oils were more active against preformed biofilms compared to amphotericin B and fluconazole. At 0.5× MIC, Cymbopogon citratus followed by Syzygium aromaticum were most inhibitory against biofilm formation. Light and electron microscopic studies revealed the deformity of three dimensional structures of biofilms formed in the presence of sub-MICs of Cymbopogon citratus. The cell membranes appeared to be the target site of compounds in sessile cells as displayed by SEM observations.

Conclusion

Our data had demonstrated promising in vitro anti-biofilm activity by Cymbopogon citratus and Syzygium aromaticum and confirm the ethnopharmacological use of these oils in muco-cutaneous Candida infections. Furthermore, it suggests exploitation of these oils as new anti-biofilm products to deal with the problem of drug-resistance and recurrent infection associated with biofilm mode of growth of Candida spp.     

Essential oils of Salvia bracteata and Salvia rubifolia from Lebanon: Chemical composition,antimicrobial activity and inhibitory effect on human melanoma cells

Aim of the study

Salvia bracteata Banks et Sol. and Salvia rubifolia Boiss. are known in folk medicine of Lebanon for the treatment of microbial infections, cancer, urinary and pulmonary problems. In the present study the chemical composition and antimicrobial activity of essential oils from aerial parts of Salvia bracteata and Salvia rubifolia collected in Lebanon were evaluated. The oils were also tested for their potential antiproliferative effects against M14 human melanoma cells.

Material and methods

The oils were studied by GC and GC–MS and their antibacterial activity (MIC and MBC) was tested against ten bacteria species using the broth dilution method. The inhibitory effect on human melanoma cells (measurement of cell vitality, cell membrane integrity and genomic DNA fragmentation) was studied using MTT assay, calculation of LDH release and COMET assay.

Results

The oils showed a good antibacterial activity (MIC = 50 μg/ml) against Gram+ bacteria. They besides exhibited an inhibitory effect on the human cancer cells examined inducing also apoptotic cell death, but the oil of Salvia rubifolia was significantly (p < 0.001) more active as compared to the oil of Salvia bracteata.

Conclusion

The results on the pharmacological activities of these Salvia species provide an in vitro scientific support for the use of these plants in traditional herbal preparations.