藏药砂生槐种子提取物抑菌和细胞毒活性的初步研究

砂生槐是我国西藏高原一种特有植物,是一种极为宝贵的药用植物资源.我们首次从砂生槐种子中获得氯仿、95%乙醇、75%乙醇和水提取物,用琼脂扩散实验测定其抑菌活性和用MTT法测定其对肿瘤细胞的细胞毒效应,表明氯仿提取物和95%乙醇提取物具有广谱的抑菌活性,抑菌活性较强的是氯仿提取物.各种提取物显示出浓度依赖性的细胞毒效应,氯仿、95%乙醇、75%乙醇和水提取物对胃癌SGC-7901细胞系的LC50分别是4.5、1.4、1.9和41.7 mg/mL,抑制胃癌SGC-7901细胞增殖作用较强的成分是砂生槐种子95%乙醇提取物.这一发现为开发砂生槐这一宝贵植物资源的药用价值提供了重要的依据.     

Diastereoselective Sonochemical Synthesis of Spirocyclopropaneoxindoles and Evaluation of Their Antioxidant and Cytotoxic Activities

An efficient diastereoselective synthesis of spirocyclopropaneoxindoles is reported using three‐component reactions of various phenacylidenetriphenylphosphorane, isatins and phenacyl bromide under ultrasonic irradiation. The structures of synthesized spirocyclopropaneoxindoles were characterized by their spectral data. The antioxidant activities of the synthesized compounds were evaluated by 1,1‐diphenyl‐2‐picrylhydrazyl radical scavenging assay. Among the products, those with NH group in their structure exhibited higher antioxidant activities than other derivatives. Also, in vitro cytotoxicity of compounds 4b , 4e , 4j , 4k were examined against heLa cancer cell lines using MTT assay. The results revealed that compound 4j with chlorine substituent on phenyl group displayed higher cytotoxicity activity (IC₅₀=4.50±0.30 μg/mL) after 48 h.     

Antimicrobial and Cytotoxic Activities of Lepidium latifolium L. Hydrodistillate,Extract and Its Major Sulfur Volatile Allyl Isothiocyanate

The cultivated Lepidium latifolium L. was investigated to decipher its glucosinolate profile, antimicrobial, and cytotoxic activities. HPLC/ESI‐MS analyses of the intact glucosinolates and GC/MS analysis of their hydrolysis products showed the presence of sinigrin ( 1 ), glucocochlearin ( 2 ), glucotropaeolin ( 3 ), and 4‐methoxyglucobrassicin ( 4 ). Hydrodistillate, extract, and allyl isothiocyanate, the main volatile resulting from sinigrin degradation, showed antimicrobial activity against all eleven tested pathogenic and food spoilage bacteria and fungi, with highest effect observed against Candida albicans with MIC₅₀ 8 and 16 μg/mL. Hydrodistillate and extract showed the best cytotoxic activity on bladder cancer UM‐UC‐3 cell line during an incubation time of 24 h (IC₅₀ 192.9 and 133.8 μg/mL, respectively), while the best effect on glioblastoma LN229 cell line was observed after 48 h (IC₅₀ 110.8 and 30.9 μg/mL, respectively). Pure allyl isothiocyanate displayed a similar trend in cytotoxic effect on both cell lines (IC₅₀ 23.3 and 36.5 μg/mL after 24 h and 48 h, respectively).     

Analyzing the Impact of Ramalina digitellata,R. fastigiata,R. fraxinea,and R. polymorpha's Usnic Acid Concentration on Antioxidant,DNA-Protective,Antimicrobial, and Cytotoxic Properties

The present study is focused on the antimicrobial, antioxidant, cytotoxic, and DNA protective effects of methanol extract obtained from R. digitellata, R. fastigiata, R. fraxinea, and R. polymorpha species that are distributed in Turkey. The highest total phenol content was determined in R. digitellata (144.6 mgGAE/g_extract), and the highest total amount of flavonoids was found in R. fastigiata (20.40 mgGAE/g_extract). The content of usnic acid was determined by High-Performance Liquid Chromatography (HPLC) and the highest amount was found in R. digitellata. DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS [2,2’-azinobis(3-ethylbenzathiazoline-6-sulfonic acid)] radical scavenging methods were used for antioxidant activity. R. fraxinea showed the highest DPPH⋅ and ABTS⁺⋅ scavenging activity. In addition, the DNA protective effect was investigated using pBR322 plasmid DNA, and; all studied species were found to have DNA protective effects. The antibacterial activity was investigated using the disc diffusion method, and the R. digitellata methanol extract showed the best results with a 12.35 mm zone on Proteus mirabilis. On the human lung cancer (A549) and breast cancer (MDA-MB-231) cell lines, cytotoxic activity was assessed using an MTT assay. All lichen extracts were found to have a significant cytotoxic effect on both cancer cell lines at 1000 μg/mL concentration. These results suggest that Ramalina species may be potential candidates for developing new phytopharmaceuticals and functional components.     

Phytochemical Screening,Antioxidant Assay and Cytotoxic Profile for Different Extracts of Chrysopogon zizanioides Roots

The Chrysopogon zizanioides plant possesses multiple traditional uses, especially in therapeutics, but only a few articles have reported its biological activity. Hence, the present study was planned to explore the phytochemical constituents, cytotoxic potential, radical scavenging activity, and GC/MS (Gas chromatography & Mass spectrometry) analysis of the vetiver root extracts. The roots extracted with different solvents exhibited more significant phytochemical constituents in polar solvents in comparison to non-polar ones, favoring the extraction of a greater number of components in highly polar solvents. All the extracts were tested for their cytotoxicity using SRB (Sulforhodamine B) assay. They confirmed ethanolic extract as a potent extract with GI₅₀ 56±0.5 μg/ml in oral cancer (SCC-29B) along with no cytotoxicity in healthy cells (Vero cells), making it a safer therapeutic option in comparison to standard Adriamycin. This extract was also analyzed for its antioxidant potential by DPPH (1,1-Diphenyl-2-picrylhydrazyl) assay with IC₅₀ value 10.73 μg/ml, which was quite comparable to Ascorbic acid having IC₅₀ value 4.61 μg/ml. The quantitative analysis of ethanolic extract exhibited 107 compounds amongst which Khusenic acid, Ascorbic acid, Junipen, gamma-Himachalene, alpha-Guaiene were the majorly occurring compounds that can be explored further for their cytotoxic activity.     

Caffeoylquinic Acids,Cytotoxic, Antioxidant,Acetylcholinesterase and Tyrosinase Enzyme Inhibitory Activities of Six Inula Species from Bulgaria

Chlorogenic (5‐CQA), 1,5‐, 3,5‐, 4,5‐ and 3,4‐dicaffeoylquinic (DCQA) acids were identified and quantified in the methanol extracts of Inula oculus‐christi L., I. bifrons L., I. aschersoniana Janka var. aschersoniana, I. ensifolia L., I. conyza (Griess .) DC. and I. germanica L. by HPLC analysis. The amount of 5‐CQA varied from 5.48 to 28.44 mg/g DE and the highest content was detected in I. ensifolia. 1,5‐DCQA (4.05–55.25 mg/g DE) was the most abundant dicaffeoyl ester of quinic acid followed by 3,5‐DCQA, 4,5‐DCQA and 3,4‐DCQA. The extract of I. ensifolia showed the highest total phenolic content (119.92±0.95 mg GAE/g DE) and exhibited the strongest DPPH radical scavenging activity (69.41±0.55 %). I. bifrons extract was found to be the most active sample against ABTS^.+ (TEAC 0.257±0.012 mg/mL) and the best tyrosinase inhibitor. The studied extracts demonstrated a low inhibitory effect towards acetylcholinesterase and possessed low cytotoxicity in concentration range from 10 to 300 μg/mL toward non‐cancer (MDCK II) and cancer (A 549) cells.     

Essential Oils of Polyalthia suberosa Leaf and Twig and Their Cytotoxic and Antimicrobial Activities

Essential oils from the leaf and twig of Polyalthia suberosa (Roxb.) Thwaites were analyzed using GC/MS/FID. A total of sixty-three constituents were namely identified accounting for 96.03 and 94.12 % in the hydrodistilled oils of the leaf and twig, respectively. Monoterpenes, monoterpenoids, sesquiterpenes, and sesquiterpenoids were characteristic derivatives of P. suberosa essential oils. Sesquiterpenes bicyclogermacrene (26.26 %) and (E)-caryophyllene (7.79 %), and monoterpene β-pinene (12.71 %) were the major constituents of the leaf oil. Sesquiterpenes (E)-caryophyllene (17.17 %) and α-humulene (9.55 %), sesquiterpenoid caryophyllene oxide (9.41 %), and monoterpenes camphene (8.16 %) and tricyclene (6.35 %) were to be main components in the twig oil. The leaf oil indicated cytotoxic activity against three cancer cell lines HepG2, MCF7 and A549 with the IC₅₀ values of 60.96–69.93 μg/mL, while the twig oil inhibited MCF7 with the IC₅₀ value of 66.70 μg/mL. Additionally, the twig oil successfully suppressed the growth of the negative Gram bacterium Pseudomonas aeruginosa, fungus Aspergillus niger, and yeast Candida albicans with the same MIC value of 50 μg/mL, whereas the leaf oil had the same result on the negative Gram bacterium Escherichia coli.     

Profiling the Lipophilic Fractions of Pithecellobium dulce Bark and Leaves Using GC/MS and Evaluation of Their Antioxidant,Antimicrobial and Cytotoxic Activities

Pithecellobium dulce has been used in traditional medicine to treat various ailments owing to its restorative properties. The biological activities and chemical profiles of the lipophilic fraction of P. dulce bark and leaves were assessed herein. Fatty acid methyl esters (FAME) and unsaponifiable matter (USM) were prepared and analyzed by GC/MS. A total of 40 compounds were identified in the bark saponifiable fraction, whereas 9 compounds were annotated in the leaves. Palmitic acid methyl ester was the major compound identified accounting for 41.48 % of the bark and 19.03 % of the leaves composition. Besides, linolenic acid methyl ester (22.40 %) and linoleic acid (12.69 %) were annotated in the leaves saponifiable fraction. A total of 63 compounds were detected in the bark USM and 4 compounds were identified in the leaves. Phytol represented the major component in the leaves (52.57 %) followed by lupeol (20.68 %) and lupenone (8.60 %). Meanwhile, n‐dodecane dominated in the bark USM accounting for 24.69 % of the total composition. The leaves and bark lipophilic fractions revealed moderate antioxidant and antibacterial activities. Both extracts showed no antifungal activity. No cytotoxicity was observed for both lipophilic fractions. P. dulce offers a good source of antioxidant compounds that can be introduced to food and pharmaceutical industry.     

白背三七大孔树脂富集物化学成分及抗氧化活性研究

本文采用HPLC-ESI-MS分析白背三七醇提液经HPD-100树脂富集分离后的黄酮类化合物,并采用化学和生物模型对富集物的抗氧化活性进行研究.实验结果表明该富集物主要黄酮成分为槲皮素和山奈酚的糖苷类化合物,且以山奈酚-3 -O-β-D-葡萄糖苷的含量最高;白背三七醇提液经富集后总黄酮含量提高了6倍.在试验模型中,除螯合能力外,富集后产物抗氧化能力较富集前均有显著提高,说明黄酮类化合物是白背三七抗氧化活性的主要物质基础.     

Antioxidant,Anti‐inflammatory and Cytotoxic Activities of Polyphenols Extracted from Chroogomphus rutilus

Chroogomphus rutilus is a rare fungal species that grows under pine trees and is now widely used as a functional food and pharmaceutical product. However, the chemical constituents and biological activities of Chroogomphus rutilus have been relatively limited. The present study aimed at determining the total polyphenols and flavonoids contents, biological activities and main phenolic compounds of Chroogomphus rutilus from different geographical origins at the stipe and pileus. The results suggested that Chroogomphus rutilus polyphenol extracts revealed a higher antioxidant, anti‐inflammatory, and cytotoxic activities, and there were significant differences between samples from different locations and regions. Correlation analysis showed that the contents of total polyphenols and flavonoids were significantly correlated with antioxidant and anti‐inflammatory activities. However, only the content of total flavonoids was significantly correlated with cytotoxicity, which means that the cytotoxicity of Chroogomphus rutilus polyphenol extracts may be regulated by flavonoids or other compounds. HPLC‐DAD analysis revealed that the main phenolic compound was protocatechuic acid, followed by baicalin, p‐hydroxyphenylacetic acid and p‐hydroxybenzoic acid, but comparing with the pileus extracts, the stipe extracts can be considered as a higher concentration of phenolic compounds. Therefore, antioxidant, anti‐inflammatory and cytotoxic activities of Chroogomphus rutilus polyphenol extracts could be due to the identified compounds. This study investigated a deep knowledge about the constituents and activities of Chroogomphus rutilus and provided the reference for its application in food and pharmaceutical.     

竹叶提取物的体外抑菌及抗氧化活性的研究

本文用水提取竹叶有效成分,将提取液浓缩至含生药量约1.0 g/mL,经醇沉后取清液浓缩,再经石油醚、三氯甲烷、乙酸乙酯、正丁醇分步萃取,得不同极性的各部分提取物。以金黄色葡萄球菌和大肠杆菌为供试菌,采用抑菌圈法(琼脂扩散法)和最低抑菌浓度(MIC)法测定其抑菌效果。结果显示,石油醚、三氯甲烷、乙酸乙酯部分均表现抑菌活性。各供试样对两种菌的抑菌圈直径达9.8～18.4 mm,最低抑菌浓度分别为1.25 mg/mL2,.50 mg/mL和5.00 mg/mL。最后采用亚硝基红盐-Co2+褪色法研究了竹叶提取物对.OH的清除作用,结果表明三氯甲烷和乙酸乙酯部分萃取物的抗氧化性明显优于水提物,其中乙酸乙酯部分萃取物的IC50值为1.06 mg/mL。     

Cytotoxic,antioxidant, and antimicrobial activities of Celery (Apium graveolens L.)

Celery (Apium graveolens Linn, Family: Apiaceae) is a common edible herb used as a spice in the traditional medicine of several nations since time immemorial. The whole plant is extensively used in cooking as soups and salads. A. graveolens has various pharmacological properties such as anticancer, anti-obesity, anti-hepatotoxic, and antihypertensive agents. Hence, it is of interest to document the in vitro cytotoxic, antioxidant, and antimicrobial activity of A. graveolens. The plants were collected in the local market, shade dried, and different parts of the plants were extracted with 70% ethanol using a cold maceration process. Antioxidant tests were performed based on the various radical scavenging methods. Antimicrobial activity and MIC were completed using the respective cup-plate and two-fold serial dilution method. In vitro cytotoxic studies were achieved by the MTT; Sulphorhodamine B assayed total cell protein content. DLA and ESC cells determined the short-term toxicity. The leaf extract exhibited significant antioxidant properties against NO, DPPH, ABTS, LPO, and HPO methods. Thus, potential inhibition against Gram-positive, Gram-negative, and fungal strains within the MIC ranges of 250-500 µg/ml was observed. All the extracts of the plant presented in the study revealed greater cytotoxicity effects against five respective cancer cell lines, L6, Vero, BRL 3A, A-549, L929, and L-929 with the ranging of 443-168.5 µg/ml. Thus, we show that A. graveolens possess a potential cytotoxic, antioxidant, and antimicrobial activity.     

Comparative Evaluation of Polyphenol Contents and Biological Activities of Five Cistus L. Species Native to Turkey

In this study phytochemical compounds and antioxidant capacity, cytotoxic, antimicrobial and anti-biofilm activities of hydroethanolic extracts of five Cistus species (C. creticus L., C. laurifolius L., C. monspeliensis L., C. parviflorus Lam. and C. salviifolius L.) distributed in Turkey were investigated. (+)-catechin, epigallocatechin gallate, quercetin-3-O-rutinoside, quercetin-3-O-glucoside, kaempferol-3-O-glucoside, luteolin were detected in different amounts. Strongest antioxidant capacities were observed with C. creticus, and C. parvifolius (0.476 and 0.452, respectively). Minimum inhibitory concentrations (MIC) of the extracts were determined between 32 and 128 μg/mL against different bacteria and Candida strains. C. monspeliensis and C. laurifolius extracts were inhibited the biofilm production levels of three Gram-negative bacteria (E. coli, S. enterica, P. aeruginosa), two Gram-positive bacteria (S. aureus, B. subtilis) and three Candida strains (C. albicans, C. parapsilosis, C. krusei). C. creticus extract showed strongest cytotoxic activity against human breast adenocarcinoma (MCF-7) and prostate cell lines (PC-3) (IC₅₀: 14.04±2.78 μg/mL and 34.04±2.74 μg/mL, respectively) among all plants tested.     

川芎粗多糖抗氧化和细胞毒活性研究

通过川芎粗多糖(LCP)对DPPH离子、超氧阴离子、.OH、总抗氧化能力、螯合能力、还原性和脂质过氧化能力的抗氧化效果和对肝癌细胞HepG2的抑制作用研究。结果显示:LCP具有较强的还原力,对超氧阴离子自由基、脂质过氧化产物有良好的抑制作用,其对肝癌细胞HepG2也具有一定的抑制作用。LCP有望作为天然抗氧化剂及功能性食品得到开发与应用。     

Essential Oil Compositions and Antibacterial and Antioxidant Activities of Five Lavandula stoechas Cultivars Grown in Thailand

The essential oils of five Lavandula stoechas cultivars grown in Thailand were characterized for their volatile compounds using GC‐FID and GC/MS methods as well as screened for antibacterial and antioxidant activities. Dried aerial parts, including flowers and stems from each cultivar, were subjected to hydrodistillation for 4 h. The essential oil yields were 0.18 %–0.82 % w/w. Of the 95 compounds detected and identified, 1,8‐cineole, fenchone, and camphor were considered the major compounds. Essential oil from each cultivar demonstrated different patterns of antibacterial activity and a variety of antioxidant properties. The highest antibacterial activity, MIC=0.39 mg mL^?1, was observed from the essential oil of L. stoechas ‘major’ (against Klebsiella pneumoniae and Salmonella typhimurium) and the essential oil of L. stoechas ‘white lavender’ (against S. typhimurium). The essential oil of L. stoechas×viridis ‘St. Brelade’ possessed the highest antioxidant capacity, as determined by the DPPH and ABTS assays (IC₅₀ of 67.65 and 89.26 mg mL^?1, respectively). The results indicated that some of these essential oils could be used as key ingredients in lavender oil products in Thailand to increase their therapeutic efficacy, depending on their intended application.     

白皮锦鸡儿黄酮醇类化合物及其抗菌和抗氧化活性(英文)

从豆科植物白皮锦鸡儿(Caragana leucophloea Pojark.)地上部分分离到3个黄酮醇类化合物,经理化和波谱分析鉴定为3-O-甲基山奈酚(1)、3-O-甲基槲皮素(2)和槲皮素(3)。活性测定表明,1表现出较强的抗细菌活性,对大肠杆菌和番茄疮痂病菌的半抑制浓度分别为9.00μg/mL和7.42μg/mL,最低抑制浓度均为12.5μg/mL;而2和3则表现出较强的抗氧化活性,对DPPH还原的半抑制浓度分别为14.39μg/mL和13.64μg/mL;对β-胡萝卜素-亚油酸氧化的半抑制浓度分别为10.26μg/mL和9.87μg/mL。上述黄酮醇类化合物均为首次从白皮锦鸡儿中分离得到。     

Evaluation of Antioxidant,Antibacterial and Enhancement of Antibiotic Action by Punica granatum Leaves Crude Extract and Enriched Fraction against Multidrug-Resistant Bacteria

The aim of this study was to evaluate the phytochemical composition, antioxidant, and antimicrobial potential of crude extract and fractions of Punica granatum leaves. The extract was produced by turbo extraction, after which hexanic, ethyl acetate, and aqueous fractions were obtained by partitioning. The chemical analyses were performed by thin layer chromatography and high-performance liquid chromatography, and the antioxidant activities were assayed by DPPH^. and ABTS^.+. Minimal inhibitory and bactericidal concentrations (MIC/MBC) were applied to twenty-two bacteria. Most strains susceptible to extract/fractions and resistant to antibiotics were selected, and ampicillin, azithromycin, ciprofloxacin, and gentamicin were associated with the ethyl acetate fraction (EAF) against multidrug-resistant strains in modulatory and checkboard models. The data from chromatographic analyses showed flavonoids and tannins in the extract, as well as the enrichment of EAF in phenols, mainly flavonoids. The flavonoids were connected to the electron transfer activity demonstrated in the DPPH^. and ABTS^.+ assays. Gram-positive strains are more susceptible to EAF. The subinhibitory concentrations of P. granatum enhanced the antimicrobial activity of the agents and reduced the EAF individual MIC, and the combination of EAF and antibiotics demonstrated a synergistic effect. These results present a promising approach for developing a therapy in which antioxidant extracts and fractions can be used in combination with antibiotics.     

野葛花醇提物中异黄酮含量及其抗氧化活性测定

以葛花苷为标准品,对野葛花醇提物的氯仿、乙酸乙酯、正丁醇萃取物及水溶物4部分中的异黄酮含量进行测定,并采用DPPH·法对各萃取物进行自由基清除实验.结果显示,(1)氯仿、乙酸乙酯、正丁醇萃取物及水溶物4部分的异黄酮含量分别为35.27%、53.42%、52.13%和2.34%.(2)抗氧化实验显示, 4 部分清除DPPH·的IC50值分别为252、49、197和344 μg/mL.(3)相关性分析表明,野葛花醇提物各萃取部分的抗氧化活性主要来自于其中含有的异黄酮类化合物.研究表明野葛花醇提物的乙酸乙酯和正丁醇萃取部分异黄酮含量较高;氯仿、乙酸乙酯、正丁醇萃取物及水溶物4部分对DPPH自由基均有一定的清除作用,其中以乙酸乙酯萃取物的效果最佳;表明异黄酮是一种天然的抗氧化剂,具有较强的抗氧化作用.     

Analytical Profiling of Phenolic Compounds in Extracts of Three Cistus Species from Sardinia and Their Potential Antimicrobial and Antioxidant Activity

The Cistaceae family is well represented in Sardinia, and the Cistus genus is widely used in traditional medicine. Nowadays only few studies have been performed on this genus vegetating in Sardinia in spite of its ethnobotanical importance. Moreover, in the past there have been conflicting opinions among botanists for the exact assignment of the species growing in Sardinia. We started several years ago to carried out studies on this genus and in the present study was to evaluate the in vitro activity of several samples of Cistus salvifolius L., Cistus monspeliensis L., and Cistus albidus L. collected in Sardinia as antimicrobial agents against Escherichia coli, Staphylococcus aureus, and four Candida species and their antioxidant activity using DPPH, ABTS, and FRAP assays. Furthermore, the phenolic content and composition of the extracts were first evaluated. Using statistical multivariate analysis on the complete metabolomics profile of all Cistus species growing wild in Sardinia, we confirmed the botanical classification, and we observed an interesting correlation between metabolomics profile and antioxidant activity.     

不同来源中国蜂胶水提物的化学组成及抗氧化性

本文研究了季节和地理来源对中国蜂胶水提物的化学成分和抗氧化性的影响。分别采集了来自山东、湖北和海南三个省份不同季节的蜂胶,采用改进的提取方法,得到蜂胶水提物(Water extract of propolis,WEP)。分光光度法测定了WEP的主要化学组成,普鲁士兰法和清除DPPH自由基活性法评价了WEP的抗氧化性。研究结果表明,中国WEP含有总酚和总黄酮等化学成分,具有较好的抗氧化性。季节对中国WEP化学成分和抗氧化性有显著影响。山东和湖北WEP化学成分比较接近,但同海南WEP有显著差异,抗氧化活性也显著强于海南WEP。不同产地和不同采收季节的中国WEP存在化学组成及生物活性多样性,在生产实践中需注意这一特性。