Analysis of Alpina officinarum Hance,chemically and biologically

Alpinia officinarum Hance is one of the most commonly used herbs belongs to Family Zingiberaceae. The current work deals with the qualitative and quantitative chemical study of this plant rhizomes in addition to the investigation of its anticancer activities. The results of the qualitative analysis showed a variation of phytochemical contents in this plant. While quantitative analysis showed a very promising percentage of active materials and Pharmacopeial constants. Analysis of elements like Cu, Zn & Mg were variable chromium was the lowest (0.680 ppm). The active constituents showed the highest percentage of carbohydrate (20.25 ± 1.11) and the lowest was of lipid (2.79 ± 1.03), other constituents percentage ranged from 5.11 ± 1.31 to 18.26 ± 1.24 for protein and flavonoids respectively. The pharmacopeial constant determinations reported the highest in moisture content (11.02 ± 1.05), Total ash, water-soluble ash, and acid insoluble ash were varied in values (5.64 ± 1.31 to 2.01 ± 1.12).The evaluation of the antitumor activities (in vitro) of the investigated plant rhizomes extract showed that; it exhibited a direct cytotoxic effect on the growth of some cell lines compared to the standard drug vinblastine sulphate. The activities were recorded against two cell lines; A-549 (Lung carcinoma) and CACO (colorectal carcinoma) with IC50 6.72 ± 0.5 and 7.6 ± 0.3 µg/ml respectively, these effects were better than the standard drug vinblastine sulphate (IC₅₀ were 24.6 ± 0.7& 30.3 ± 1.4 µg/ml). Moreover, the effect of the investigated extract was also promising on the other three cell lines (HCT-116 (Colon carcinoma, Hela (Cervical carcinoma) & Pc3 (prostate cancer) the best effect was on Hela with IC₅₀ of 24.5 ± 1.1 µg/ml better than vinblastine sulphate (59.7 ± 2.1 µg/ml).     

Synthesis and anticancer activity of 13-membered cyclic enediynes

We herein describe the synthesis of 15 novel 13-membered cyclic enediyne derivatives using simple and straightforward approach. Representative examples were screened for their anticancer activities on 60 different human tumor cell lines representing various histologies viz. leukemia, melanoma, and cancers of lung, colon, kidney, ovary, breast, prostate, and central nervous system. The enediyne derivatives with halogen substitutions, especially fluorides were found to be active against most of the cell lines. The initial results indicates marginal to good inhibition for the growth of tumor cells for several cell lines, which shows the potential of these class of compound towards anticancer application.     

Anticancer,antioxidant and antibiotic activities of mushroom Ramaria flava

Ramaria flava is a species of edible mushroom with some bioactivity. The anticancer, antioxidant and antibiotic activities and chemical composition of R. flava ethanol extract (EE) were evaluated. The present study exhibited that the EE displayed the strongest inhibitory activity against tumor cell MDA-MB-231 with an IC₅₀ value of 66.54 μg/mL in three tested tumor cell lines, and the inhibition percent was 71.66% at the concentration of 200 μg/mL (MTT assay). The total phenolic compounds varied among four fractions of the EE from 6.66 to 61.01 mg gallic acid equivalent (GAE) per g dry weight. Water fraction exhibited high DPPH and OH radical-scavenging activities with low IC₅₀ values of 5.86 and 18.08 μg/mL, respectively. Meanwhile, three phenolic compounds from water fraction were also identified by HPLC. The antibiotic activities of the EE were evaluated against three microorganisms and three fungi strains by means of the agar well diffusion method and the poisoned medium technique, respectively. The EE also showed moderate antibiotic activities. These results suggest that R. flava could hold a good potential source for human health.     

研究开发中的海洋抗癌活性物质

海洋天然产物现已成为临床抗癌药物的重要来源，从didenmline B开始，进入临床研究的抗癌活性物质已经有二十多种。根据海洋来源抗癌活性物质的作用靶点不同，系统综述了正在研究中的十几种来源于海洋的天然抗癌活性物质的作用机制和研究开发情况等。     

Anticancer effect of Howiinol A and its mechanism of action

Howiinol A (GHM-10) is a kind of phenylethylene pyrone compounds isolated from Goniothalamus howii. By using the techniques of cell growth curve determination, MTT test, soft agar colony assay and experimental therapy of transplantable tumors in mice, it is found that GHM-10 exerts potent inhibitory effect on cancer cells but its influence on normal cells is relatively slight; the sensitivity of a drug-resistant cell line, KB/VCR 2000, to GHM-10 is similar to its parent cell line KB. Remarkable therapeutic effect can be seen in mice bearing H22 hepatoma and Lewis lung cancer and in mice with ascetic sarcoma 180 when GHM-10 is orally or intraperitoneally administered.

The IC₅₀s of L1210 cells treated with GHM-10 for 1 and 24 h are 6.85 and 3.32 μg·ml^-1 respectively. The ratio of IC₅₀ 1 h and IC₅₀ 24 h is only 2.06, indicating that the action of GHM-10 is conformed to a cell cycle non-specific cytotoxic agent. By using trypan blue exclusive test and morphological examination, it is demonstrated that the main effect of GHM-10 is to inhibit the cell proliferation. Flow cytometery technique is used to analyze the cell cycle of L1210 cells. The results show that to some extent, GHM-10 blocks the cell cycle transition from G1 phase to S phase. By using [³H] labeled precursor incorporation technique, it is shown that GHM-10 significantly suppresses the biosynthesis of DNA, RNA and protein in L1210 cells, and the DNA synthesis is mostly affected. At 1 h after the cells were treated with GHM-10, these inhibitory effects have already been irreversible, suggesting that GHM-10 may cause structural damage on DNA molecules. However, GHM-10 is unable to intercalate into DNA molecules or to destroy its structure directly. By using single cell gel electrophoresis and alkaline elution technology, it is confirmed that GHM-10 causes DNA molecule damage and single strand breakage in L1210 cells. Further studies show that GHM-10 markedly inhibits DNA dehelix induced by DNA topoisomerase II both inside and outside the cells, indicating that GHM-10 is acting as an inhibitor of DNA topoisomerase II.     

相思子毒素抑制肿瘤活性研究进展

采用手工检索和联机检索相结合，查阅了近年来国外有关相思子毒素抗肿瘤的文献资料，对相思子毒素的抗肿瘤活性研究进行了综述，认为相思子毒素对大多数肿瘤有抑制作用，应进一步深入研究，很可能为癌症的治疗开辟新的途径。     

In vitro Studies of Antimicrobial Activity of Crude Extracts of the Indian Grasses Dhaman (Cenchrus ciliaris) and Kala-Dhaman (Cenchrus setigerus)

The aim of present study was to investigate the antimicrobial activity of Cenchrus ciliaris and Cenchrus setigerus extracts in order to use it as a possible source for new antimicrobial substances against important human pathogens. Crude extracts of the stem of Cenchrus ciliaris and Cenchrus setigerus were evaluated against some medically important pathogens viz. Escherichia coli, Raoultella planticola, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Enterobacter aerogenes, Candida albicans and Aspergillus flavus. The dried and powdered stems were successively extracted with hexane, toluene, isopropyl alcohol, acetone and ethanol using soxhlet assembly. The antimicrobial activity assay was done by both disc diffusion and serial dilution methods. Isopropyl alcohol extract of Cenchrus setigerus showed highest activity against Escherichia coli. The test pathogens were more sensitive to the isopropyl alcohol, acetone and ethanol extracts than to the hexane and toluene extracts except against Bacillus subtilis. Result reveals that the most bioactive compound was cycloleucolenol-9,19-cycloergost-24 (28)-en-3-ol, 4, 14-dimethyl acetate in both the species of Cenchrus grass, (19.15%) in isopropanol extract of Cenchrus setigerus whereas, (14.03%) in acetone extract of Cenchrus ciliaris.     

洋葱挥发油抗肿瘤作用的实验研究

目的:研究洋葱挥发油离体对人肝癌细胞株(QCY-7703)、人胃癌细胞株(MGC-803)、人宫颈癌细胞株(Hela)、人肺腺癌细胞株(SPC-A-1)的增殖抑制作用和在体对小鼠肉瘤S180及小鼠艾氏腹水癌的抑制作用。方法:采用MTT法检测不同剂量的洋葱挥发油对4种肿瘤细胞增殖的影响,复制小鼠肉瘤S180和小鼠艾氏腹水癌模型,检测不同剂量(1000、500、250mg·kg-1)的洋葱挥发油对小鼠肿瘤的抑制作用,比较其抑制率。结果:洋葱挥发油离体和在体实验中对肿瘤细胞均具有较强的增殖抑制作用。结论:洋葱挥发油能抑制多种肿瘤细胞的增殖,对肿瘤细胞有明显的细胞毒性作用。     

具抗癌活性的鬼桕毒电子自旋标记物的生物学作用——研究Ⅰ.对细胞生长的抑制试验

用鬼桕毒自旋标记衍生物对子宫颈癌细胞(Hela)、乳地鼠肾传代细胞(BHK)和人胚肺成纤维细胞(KMB)进行了体外抑制试验,发现鬼桕毒自旋标记衍生物在用量为0.1mg时,对Hela、BHK细胞有较强的抑制作用。     

Anticancer activities of some arylcarbamoylalkyltriphenylphosphonium chlorides

A series of novel arylcarbamoylalkyltriphenylphosphonium chlorides were synthesized. The newly synthesized compounds, [R-(p-C₆H₄)-NH-CO-R₁P^⊕(C₆H₄)₃]Cl^θ, R = H (2), CH₃ (4), NO₂ (6), R₁ = –CH₂− (b), CH₃CH< (a), –CH₂CH₂− (c), –CH₂CH₂CH₂ (d), the analogs of an anticancer drug, were characterized by infrared (IR), ¹H nuclear magnetic resonance (NMR), ¹³C-NMR, ³¹P-NMR, mass spectrometry (MS), thermogravimetry (TG), and conductivity measurements. The anticancer activities of the obtained compounds were measured by MTT. The preliminary results indicated that some compounds showed potent anticancer activities against HCT-8, Bel-7402, A549, and S180.     

Antiproliferative effect of extracts and pyranonaphthoquinones obtained from Cipura paludosa bulbs

Context: Cipura paludosa Aubl. (Iridaceae) is widely used in folk medicine to treat several ailments. Experimental studies have confirmed its anti-inflammatory, antinociceptive, and neuroprotective effects.

Objective: This study evaluates the possible antiproliferative potential of the crude methanol extract and three isolated compounds from the bulbs of C. paludosa.

Materials and methods: Phytochemical analysis was carried out by conventional chromatographic techniques, and the resulting compounds were identified by NMR ¹H and ¹³C. The antiproliferative activity was analysed using the sulforhodamine B assay.

Results: Crude methanol extract of C. paludosa bulbs showed GI₅₀ values of between 1.6 and 30.8?μg/mL. The naphthoquinone derivatives (eleutherine, isoeleutherine, and eleutherol) isolated from the bulbs of C. paludosa exhibited promising cytotoxicity against several human tumour cell lines, especially the two main compounds, eleutherine and isoeleutherine, against glioma and breast cancer cell lines, with TGI values of between 2.6 and 13.8?μg/mL.

Conclusion: Cipura paludosa bulbs produce active principles with relevant antiproliferative potential, such as naphthoquinone derivatives, identified as eleutherine, isoeleutherine, and eleutherol. This is the first report indicating C. paludosa with antiproliferative potential.     

Protective effect of extract of Crataegus pinnatifida pollen on DNA damage response to oxidative stress

The protective effect of extract of Crataegus pinnatifida (Rosaceae) pollen (ECPP) on the DNA damage response to oxidative stress was investigated and assessed with an alkaline single-cell gel electrophoresis (SCGE) assay and pBR322 plasmid DNA breaks in site-specific and non-site-specific systems. Total phenolic content, total flavonoid content, individual phenolic compounds, antioxidant activities (1,1-diphenyl-2-picrylhydrazyl (DPPH), radical scavenging activity, FRAP, and chelating activity) were also determined. The results showed that ECPP possessed a strong ability to protect DNA from being damaged by hydroxyl radicals in both the site-specific system and the non-site-specific system. It also exhibited a cytoprotection effect in mouse lymphocytes against H₂O₂-induced DNA damage. These protective effects may be related to its high total phenolic content (17.65 ± 0.97 mg GAE/g), total flavonoid content (8.04 ± 0.97 mg rutin/g), strong free radical scavenging activity and considerable ferrous ion chelating ability (14.48 ± 0.21 mg Na₂EDTA/g).     

植物生物碱抗肿瘤作用机制的研究进展

对有关文献报道的植物生物碱对肿瘤细胞的几种不同作用机制，如直接杀伤作用、干扰细胞周期、诱导细胞分化、诱导细胞凋亡、逆转细胞抗凋亡作用等进行了综述，以期提供从天然产物中寻找优良的抗癌新药的信息和思路。     

白血病化疗药物研究

白血病是一类血液系统的恶性肿瘤，发病机制复杂，涉及到染色体易位、融合基因及融合蛋白的形成、基因拷贝数的改变、癌基因的活化、抑癌基因的失活等。针对不同白血病，从药物作用的分子机制分类综述国内外抗白血病药物的发展及治疗现状。     

Anticancer bioactivity of compounds from medicinal plants used in European medieval traditions

Since centuries, natural compounds from plants, animals and microorganisms were used in medicinal traditions to treat various diseases without a solid scientific basis. Recent studies have shown that plants that were used or are still used in the medieval European medicine are able to provide relieve for many diseases including cancer. Here we summarize impact and effect of selected purified active natural compounds from plants used in European medieval medicinal traditions on cancer hallmarks and enabling characteristics identified by Hanahan and Weinberg. The aim of this commentary is to discuss the pharmacological effect of pure compounds originally discovered in plants with therapeutic medieval use. Whereas many reviews deal with Ayurvedic traditions and traditional Chinese medicine, to our knowledge, the molecular basis of European medieval medicinal approaches are much less documented.     

抗癌治疗的VEGF靶向制剂的心血管安全性

2004年,一项治疗转移性结直肠癌的III期临床试验表明,一线使用贝伐单抗联合常规化疗获得患者生存收益,其中抑制肿瘤新生血管形成在治疗癌症中起到了关键的作用[1]。血管内皮生长因子（vascularendothelialgrowthfactor,VEGF）及其下游信号网络现在被确认为新的抗癌药物的假定目标。VEGF中和抗体以及一些小分子与细胞中的VEGF受体结合都进行了研究。     

海藻抗A-549和HL-60肿瘤细胞及抗菌活性研究

目的:为了从海藻中寻找天然药物活性前体。方法:对山东沿海的 39种海藻的甲醇提取物进行了抗肿瘤(肿瘤细胞A-549和HL-60)及抗菌(金葡菌、大肠杆菌和白色假丝酵母菌)活性筛选。结果:抗肿瘤活性研究中,海藻提取物表现出较好的活性,19种对HL-60有抑制作用,34种对A-549有抑制作用。其中,石花菜、萱藻和小粘膜藻对2种肿瘤细胞的抑制率均大于80％;而三叉仙菜和绳藻的抑制率均大于90％。在抗菌活性实验中,海藻提取物的最低抑菌浓度均大于 20mg·L~(-1)。结论:海藻作为抗肿瘤活性前体的来源,值得深入研究。     

静脉药物配置中心抗肿瘤药物处方审核方法的探讨

目的:为促进抗肿瘤药物临床使用的安全、有效提供参考。方法:结合本院静脉药物配置中心5年的实践经验,对抗肿瘤药物处方审核方法进行全面的分析、总结。结果与结论:通过对抗肿瘤药物处方剂量、溶媒、用药顺序、用药方法、特殊用法、联合使用的合理性以及超说明书用法情况等多方面进行审核,既保证抗肿瘤药物的质量,又保证其合理使用。     

抗癌药物紫杉醇的专利申请情况统计分析

目的:了解抗癌药物紫杉醇的研究状况。方法:收集世界传统药物专利数据库收录的267件紫杉醇专利申请信息,从申请的年代分布、申请的专利局分布、各国申请专利的数量等方面进行统计、分析。结果:紫杉醇2002～2007年的研究和应用进入高峰,2006年达到顶峰;我国紫杉醇专利申请的数量及职务专利占总申请数量也快速增加,且研究主要集中在药物制剂和临床应用方面。结论:我国应继续加强传统药物的科研投入和创新人才的培养。