槟榔化学成分研究

目的:研究槟榔种子的化学成分。方法:采用硅胶柱、反相RP-18柱、Sephadex LH-20柱等色谱方法进行分离纯化,根据理化性质与波谱数据鉴定化合物结构。结果:分离鉴定了13个化合物,分别为:异鼠李素(1)、槲皮素(2)、甘草素(3)、5,7,4'-trihydroxy-3',5'-dimethoxyflavanone(4)、(+)-儿茶素(5)、反式白黎芦醇(6)、阿魏酸(7)、香草酸(8)、过氧麦角甾醇(9)、豆甾-4-烯-3-酮(10)、β-谷甾醇(11)、环阿尔廷醇(12)、de-O-methyllasiodiplodin(13)。结论:其中,化合物2～4、6、7、9、10、12、13为首次从该植物中分离得到。     

槟榔黄叶病与根际线虫的探讨

本文介绍了槟榔黄叶病的研究概况和笔者从植物线虫学方面所作的探讨,并着重报道了广东、海南两省槟榔园线虫的调查结果。     

槟榔果实脂溶性化学成分的GC-MS分析

目的：研究槟榔果实脂溶性化学成分。方法：采用气相色谱一质谱联用法（GC—MS）分析槟榔果实的脂溶性成分。结果：从槟榔果实脂溶性部分鉴定了13个化学成分,占其总量的96．14％,其中主要化学成分为脂肪酸。结论：本次研究为槟榔的进一步开发和利用提供了一定的理论基础。     

Potential Antidepressant Activity of Areca catechu Nut via Elevation of Serotonin and Noradrenaline in the Hippocampus of Rats

The current study was aimed at investigating the potential antidepressant activity of Areca catechu nut ethanol extract and its various fractions using behavioral (acute and sub‐chronic forced swim tests) and biochemical (monoamines and their metabolite levels using high performance liquid chromatography) tests. The areca nut ethanol extract and its aqueous fraction exhibited antidepressant activity in both acute and sub‐chronic forced swim tests (IC₅₀ ~ 50 and 20 mg/kg, respectively), which was further confirmed by unaltered locomotor (horizontal and vertical) activities of rats in the activity cage. Phytochemical analysis revealed that saponins of areca nut may be the active component in its antidepressant action. The rats treated sub‐chronically with areca nut extract displayed toxic effects, whereas its active aqueous fraction was non‐toxic, indicating the presence of different constituents for antidepressant and toxic effects. In the hippocampus of rats, the areca nut extract (50 mg/kg) and aqueous fraction (20 mg/kg) caused a significant elevation of serotonin (around 35%) and noradrenaline (around 30%) compared with the control (261 ± 25 and 512 ± 29 ng/g, respectively). In conclusion, the areca nut possesses potential antidepressant effect via the elevation of serotonin and noradrenaline. Copyright © 2012 John Wiley & Sons, Ltd.     

响应面分析用于槟榔储藏条件考察的研究

探寻A.flavus菌株在槟榔原药材中生长及产黄曲霉毒素（AFB1,AFB2,AFG1和AFG2）的规律,分析槟榔药材的最佳储藏条件。采用响应面分析法（Response Surface Analysis,RSA）结合Central composite设计,通过测定染菌后的槟榔中水分含量及总黄曲霉毒素的变化,考察温度（Temp,20～40 ℃）和湿度（Hum,80%～95%）两个环境因子对药材上A.flavus菌株产毒的影响,分析该菌株的最适产毒条件。结果发现,储藏后的槟榔水分含量发生了显著的增加;当湿度范围为90%～95%,温度高于25 ℃时,A.flavus菌株在槟榔中生长较快并产生大量黄曲霉毒素。研究表明,当储存条件为湿度小于90%,温度低于25 ℃,槟榔药材在储藏过程中不易霉变产毒,为槟榔储藏规范的制定及降低真菌毒素污染的概率提供了较好的依据。     

厚朴汤剂对变形链球菌影响的实验研究

目的探讨厚朴汤剂对变形链球菌的影响,为厚朴作为防龋药物的临床应用提供实验依据。方法选取120只SD大鼠,采用随机数字表法分为A、B、C、D组,每组各30只。SD大鼠在出生21~23 d给予含广谱抗生素的致龋饲料,其他时间的饲料中不添加抗生素。24~27 d连续4 d给予大鼠口腔内接种变形链球菌。出生后28 d A、B、C、D组分别使用厚朴汤剂(0.3 mL)、氟化钠溶液(0.3 mL)、0.2%酸性氟磷酸钠(0.3 mL)、蒸馏水(0.3 mL)处理,1次/d,连续处理60 d。比较各组变形链球菌菌落计数,并采用keyes龋齿记分法观察各组处理方式对SD大鼠磨牙龋龋齿损害情况。结果A组变形链球菌菌落计数低于B组、C组、D组,B、C组变形链球菌菌落计数低于D组,差异有统计学意义(P<0.05);B、C变形链球菌菌落计数比较,差异无统计学意义(P>0.05);A组E级、Ds级、Dm级、Dx级评分低于B组、C组、D组,B、C组E级、Ds级、Dm级、Dx级评分低于D组,差异有统计学意义(P<0.05);B、C组E级、Ds级、Dm级、Dx级评分比较,差异无统计学意义(P>0.05)。结论厚朴汤剂能减轻大鼠龋病形成,减轻龋损破坏程度,对大鼠人工龋病发生有一定的防治作用。     

Activity of Ku Shen compounds against Staphylococcus aureus and Streptococcus mutans

Ten compounds were isolated from the Chinese crude drug, Ku Shen (Sophora flavescens Aiton). Seven compounds showed antimicrobial activity against Staphylococcus aureus and Streptococcus mutans. The activity principles were identified as kurarinone, sophoraflavanone G, iso-kurarinone, kuraridine, kushenol C, D and nor-anhydroicaritin.     

Antimicrobial activity of terpenoids from Copaifera langsdorffii Desf. against cariogenic bacteria

In the present work, the anticariogenic activities of nine labdane type‐diterpenes and four sesquiterpenes were investigated. Among these metabolites, (‐)‐copalic acid (CA) was the most active compound displaying MIC values very promising (ranging from 2.0 to 6.0 µg/mL) against the main microorganisms responsible for dental caries: Streptococcus salivarius, S. sobrinus, S. mutans, S. mitis, S. sanguinis and Lactobacillus casei. Time kill assays performed with CA against the primary causative agent (S. mutans) revealed that, in the first 12 h, this compound only inhibits the growth of the inoculum (bacteriostatic effect). However, its bactericidal effect is clearly noted thereafter (between 12 and 24 h). Also, CA did not show a synergistic effect when combined with the anticariogenic gold standard (chlorhexidine, CHD) in the checkerboard assays against S. mutans. In conclusion, the results points out CA as an important metabolite in the search for new effective anticariogenic agents. Copyright © 2010 John Wiley & Sons, Ltd.     

In vitro effects of a fraction separated from Polygonum cuspidatum root on the viability, in suspension and biofilms, and biofilm formation of mutans streptococci

Polygonum cuspidatum (Polygonaceae) has traditionally been used in folk medicine to control oral diseases. Nevertheless, there are no reports related to its possible effect on the diseases, particularly on biofilm-related diseases such as dental caries. In this study, we evaluated in vitro effects of a fraction separated from Polygonum cuspidatum root on the viability, in both suspension and biofilms, and the biofilm formation of mutans streptococci. The separated fraction (F1) showed bacteriostatic and bactericidal activity against mutans streptococci in suspension, with minimum inhibitory concentration (MIC) range of 31.3-250 microg/ml and minimum bactericidal concentration (MBC) range of 0.5-1 mg/ml. At a concentration of 1.5 mg/ml, F1 killed approximately 2 log(10)CFU/ml of Streptococcus mutans and Streptococcus sobrinus after 2h of exposure. In biofilms, F1 also inhibited the viability of Streptococcus mutans and Streptococcus sobrinus, dependent on the biofilm age, the concentration of F1, and the treatment time. Four hours of exposure to 1.5 mg/ml F1 reduced the viable counts of Streptococcus mutans and Streptococcus sobrinus by greater than 2 log(10)CFU/disc. Furthermore, at sub-MIC levels, F1 inhibited biofilm formation by Streptococcus mutans and Streptococcus sobrinus in a dose-dependent fashion. Based on the preliminary phytochemical analysis, the activity of F1 may be related to the presence of anthraquinones, cardiac glycosides, terpenoids, and phenolics. These results indicate that F1 is probably useful in the control of oral biofilms and subsequent dental caries development.     

Anti-ulcerogenic activity and isolation of the active principles from Sambucus ebulus L. leaves

Ethnopharmacological relevance

Sambucus ebulus L. has a very prominent place in Turkish folk medicine. Leaves of the plant are practiced externally to relieve rheumatic pain, to treat abscess, for wound healing and internally against hemorrhoids and stomachache. In a previous work, aqueous extract of the leaves was shown to possess potent antiulcerogenic activity on water immersion and immobilization-induced stress ulcer model in rats. This study aims to investigate the antiulcerogenic activity profile of the plant on various in vivo peptic ulcer models and gastric biochemical parameters and through bioassay-guided processing to isolate the active constituent (s) and to elucidate its structure.

Materials and methods

Among the subextracts obtained by successive solvent extractions from the MeOH extract of the leaves, the butanol subextract exerted significant antiulcerogenic activity against water-immersion and immobilization-induced stress ulcer model in rats as the bioassay model. This subextract was then subjected to successive chemical separation techniques (precipitation, column chromatography based on ion-exchange, silica gel and sephadex) and the activity of each fraction/subfraction was tested using the same bioassay model. After determination of active principles, further studies were performed on the active subextract by using various in vivo test models (ethanol-, serotonin-, pyloric ligation-induced ulcerogenesis) in rats as well as biochemical methods for the evaluation of antiulcerogenic potential.

Results

Bioassay-guided fractionation procedures yielded two flavonol glycosides as the active antiulcerogenic principles. The structures of these compounds were elucidated as isorhamnetin-3-O-monoglycoside and quercetin-3-O-monoglycoside by using ¹H, ¹³C-NMR, and FAB-MS techniques.

Conclusion

This study has proven the folkloric use of Sambucus ebulus leaves for the treatment of gastric ailments in Turkish folk medicine. The antiulcerogenic activity of the two flavonol glycosides isolated in the present study was not previously reported elsewhere.     

Antinociceptive,anticonvulsant and antibacterial effects of the essential oil from the flower heads of Egletes viscosa L

The essential oil from flower heads of Egletes viscosaL. was investigated for possible antinociceptive, anticonvulsant effects in mice and for antibacterial efficacy against resistant Staphylococcus aureus in vitro. It was found to possess a significant dose-dependent analgesic activity as assessed by acetic acid writhing and formalin tests and also an anticonvulsant activity against convulsions induced by pentylenetetrazol in mice. The plant oil displayed good antibacterial activity against resistant strains of S. aureus with the minimal inhibitory concentrations (MIC) ranging from 0.625 to 2.5 μL/mL. © 1998 John Wiley & Sons, Ltd.     

Isolation and identification of antibacterial and cytotoxic compounds from the leaves of Muntingia calabura L.

Ethnopharmacological relevance

Muntingia calabura (Elaeocarpaceae) is one of the most common roadside trees in Malaysia. Its leaves, barks, flowers and roots have been used as a folk remedy for the treatment of fever, incipient cold, liver disease, as well as an antiseptic agent in Southeast Asia. The aim of this study is to isolate and identify the antibacterial and cytotoxic compounds from the leaves of Muntingia calabura L.

Materials and methods

Antibacterial and cytotoxic activities were determined by micro-broth dilution and MTT assays, respectively. Seven fractions (F1–F7), three flavones and a chalcone were isolated from the active EtOAc extract using bioassay-guided screening. The structures of four compounds were elucidated by spectroscopic methods and compared with published data. The compounds were further tested for their antibacterial and cytotoxic activities.

Results

Three flavones and a chalcone [5,7-dihydroxy-3,8-dimethoxyflavone (1), 2′,4′-dihydroxychalcone (2), 5-hydroxy-3,7-dimethoxyflavone (3) and 3,5,7-trihydroxy-8-methoxyflavone (4)] were isolated from the active fraction F5 of EtOAc extract. Compounds 1 and 3 were isolated for the first time from Muntingia calabura L. Antibacterial activity indicates that compound 2 exhibited the most significant activity with MIC value of 50 μg/mL and 100 μg/mL against MSSA and MRSA, respectively. Cytotoxic activity indicates that compounds 2 and 3 exhibited very strong activity against HL60 with IC₅₀ values of 3.43 μg/mL and 3.34 μg/mL, respectively.

Conclusion

The antibacterial activity of the leaves of Muntingia calabura L. is ascribable to the active compound 2 while the cytotoxic activity is ascribable to the active compounds 2 and 3.     

洋金花中生物碱类成分的分离与鉴定

为了分离、鉴定洋金花中的生物碱类化学成分,采用硅胶柱、ODS开放柱和制备液相等色谱方法分离,从提取物中分离得到6个生物碱类化合物,并通过IR、NMR和MS等技术确定了其化学结构分别为曼陀罗碱（meteloidine）、莨菪碱（hyoscyamine）、去水阿托品（apoatropine）、山莨菪碱（anisodamine）、东莨菪碱（hyoscine）和norharman。     

Growth inhibitory activity of biflavonoids and diterpenoids from the leaves of the Libyan Juniperus phoenicea against human cancer cells

Three biflavonoids [cupressuflavone ( 1 ), amentoflavone ( 2 ), and sumaflavone ( 3 )], four diterpenoids [13‐epi‐cupressic acid ( 4 ), imbricatholic acid ( 5 ), 3‐hydroxy‐sandaracopimaric acid ( 6 ), and dehydroabietic acid ( 7 )], and one lignan [β‐peltatin methyl ether ( 8 )] were isolated from the cytotoxic fractions of the extracts of the leaves of the Libyan Juniperus phoenicea L. The structures of these compounds were elucidated by spectroscopic means. Cytotoxicity of compounds 1 – 6 were assessed against the human lung cancer cell line A549 using the MTT assay. Compounds 1 and 3 showed cytotoxicity against the A549 cells (IC₅₀ = 65 and 77 μM, respectively), whereas compound 2 did not show any activity. Diterpenes 4 – 6 exhibited weak cytotoxicity against the A549 cells with the IC₅₀ values of 159, 263, and 223 μM, respectively. The cytotoxicity of each compound was compared with the anticancer drug, etoposide (IC₅₀ = 61 μM). Cupressuflavone ( 1 ) was evaluated also for cytotoxicity against both the human PC3 cancer cell line and the normal prostate cell line (PNT2), and this compound revealed a high degree of cytotoxic selectivity towards the prostate cancer cells (PC3), with IC₅₀ value of 19.9 μM, without any evidence of cytotoxicity towards the normal prostate cell line (PNT2).     

塔原1号红花黄色素提取及成分分离鉴定

目的提取塔原1号红花黄色素并分离鉴定其成分。方法采用溶剂提取、澄清剂除杂和柱层析法分离纯化红花黄色素,利用质谱和核磁共振谱确定分子结构。结果从塔原1号提取出的黄色素中分离得到羟基红花黄色素A。结论羟基红花黄色素A含量为95.09%,产率为0.33%。     

Antimicrobial activity against bacteria with dermatological relevance and skin tolerance of the essential oil from Coriandrum sativum L. fruits

The aim of this work was to determine the antibacterial activity of essential coriander oil (ECO) on bacteria with dermatological relevance and to assess the skin tolerance of antimicrobial effective ECO concentrations. Essential coriander oil was tested on clinical isolates of different bacteria species, all of which may cause superficial skin infections. Antimicrobial susceptibility testing was performed using a standardized macrodilution test. Essential coriander oil showed good antibacterial activity towards the majority of the bacterial strains tested, including Streptococcus pyogenes (Lancefield group A) and methicillin resistant Staphylococcus aureus (MRSA), with mean minimal inhibitory concentrations of 0.04% v/v and 0.25% v/v, respectively. The skin tolerance of a cream and a lotion containing 0.5% and 1.0% ECO was assessed in 40 healthy volunteers using the occlusive patch test. No skin irritation could be observed by sensitive photometric assessment in any of the volunteers. Because of its activity against Streptococcus pyogenes, Staphylococcus aureus and MRSA combined with excellent skin tolerance, ECO might be useful as an antiseptic for the prevention and treatment of skin infections with Gram-positive bacteria.     

斑纹芦荟中芦荟苦素的分离鉴定

从斑纹芦荟叶中分得结晶,经理化数据和光谱解析等方法鉴定为芦荟苦素。