In vitro anticancer activity of twelve Chinese medicinal herbs

Aqueous extracts of 12 Chinese medicinal herbs, Anemarrhena asphodeloides, Artemisia argyi, Commiphora myrrha, Duchesnea indica, Gleditsia sinensis, Ligustrum lucidum, Rheum palmatum, Rubia cordifolia, Salvia chinensis, Scutellaria barbata, Uncaria rhychophylla and Vaccaria segetalis were evaluated for their antiproliferative activity on eight cancer cell lines as well as on normal human mammary epithelial cells. Five human and three murine cancer cell lines representing different tissues (breast, lung, pancreas and prostate) were used. All the crude aqueous extracts demonstrated growth inhibitory activity on some or all of the cancer cell lines, but only two showed activity against the normal mammary epithelial cells. Overall, the murine cell lines tended to be more sensitive to most of the extracts compared with the human cell lines. Among the human cell lines, cell type specificity was observed for two extracts. These results indicate the potential use of traditional Chinese medicinal herbs as antineoplastic agents and suggest that further studies evaluating their mechanism(s) of action and the isolation of active antitumor compounds are warranted.     

黄芩不同极性溶剂提取物抗氧化活性研究

目的比较黄芩不同溶剂提取物的抗氧化活性,并测定其黄酮含量。方法利用比色法测定黄芩不同溶剂提取物中的总黄酮含量,利用1,1-二苯基-2-苦苯肼(DPPH)自由基体系对黄芩不同溶剂提取物的抗氧化活性进行评价。结果黄芩不同溶剂提取物均具有一定的抗氧化活性,其中乙醇提取物清除DPPH自由基的能力最强,且总黄酮含量最高。结论黄芩的抗氧化活性受到不同溶剂的影响,并且与其含的黄酮含量成正相关。     

Molecular and pharmacodynamic properties of estrogenic extracts from the traditional Chinese medicinal herb, Epimedium

The Chinese medicinal herb, Epimedium, used traditionally for bone health exerts estrogenic activity (EA) in vitro. A genetically characterized Epimedium brevicornum (EB) extract induced biphasic responses in the mRNA and protein expression of the estrogen-regulated progesterone receptor gene in breast cancer (MCF-7) cells. These changes were mirrored changes in estrogenic receptor (ERalpha) content. In male Sprague-Dawley rats, administration of the estrogenic prodrug, estradiol valerate increased area-under-curve of serum effects for ERalpha (AUC difference: 18,900EA(ERalpha) min; 95% CI: 0-37,800; p = 0.05) and breast cancer cell (MCF-7) growth (AUC difference: 30,200EA(MCF-7) min; 95% CI: 24,200-36,200; p<0.001), compared to placebo. Oral administration of Epimedium brevicornum increased ERalpha activity (1320EA(ERalpha) min, p<0.01). Our data indicate that estrogen-responsive bioassays can measure the pharmacokinetic/pharmacodynamics of estrogenic activity in serum. Epimedium brevicornum extract increases estrogenic activity in serum and human studies are required to evaluate whether Epimedium extracts have utility for estrogen replacement therapy.     

Cytoprotective effect of Scutellaria baicalensis in CA1 hippocampal neurons of rats after global cerebral ischemia

Based on the use of Scutellaria baicalensis for the treatment of stroke in traditional Oriental medicine, the current study was carried out to evaluate neuroprotective effects of S. baicalensis after transient global ischemia using rat 4-vessel occlusion model. Methanol extracts from the dried roots of S. baicalensis (0.1-10 mg/kg) administered intra-peritoneally significantly protected CA1 neurons against 10 min transient forebrain ischemia as demonstrated by measuring the density of neuronal cells stained with Cresyl violet. Methanol extract of S. baicalensis inhibited microglial tumor necrosis factor-alpha (TNF-alpha) and nitric oxide production, and protected PC12 cells from hydrogen peroxide-induced toxicity in vitro.     

黄芩的本草考证

通过对黄芩历代本草的系统考证,结合目前黄芩的产销情况,证实我国历代药用黄芩的品种是以黄芩(Scutellaria baicalensis Georgi)为主的黄芩属的多种植物。道地产区的记载古今有差异。黄芩的功效及主治古今基本一致。     

In vitro cytotoxic activity of Thai medicinal plants used traditionally to treat cancer

The SRB assay was used to test cytotoxicity against three human cancer cell lines and one normal cell line of 11 Thai medicinal plant species used by traditional doctors in treating cancer patients. The extraction procedures used were similar to those practised by Thai traditional doctors (ethanolic and water extracts). Extracts were tested against the human large cell lung carcinoma cell line COR-L23, the human breast adenocarcinoma cell line MCF-7 and human colon adenocarcinoma cell line LS-174T and normal human keratinocytes SVK-14. The results showed that three plants; Dioscorea membranacea Pierre ex Prain & Burkill, Dioscorea birmanica Prain & Burkill (Dioscoreaceae) and Siphonodon celastrineus Griff. (Celastraceae), exhibited high cytotoxic activity showing a certain degree of selectivity against the different cell types.     

Extracts from the roots of Lindera strychifolia induces apoptosis in lung cancer cells and prolongs survival of tumor-bearing mice

Lindera strychifolia, a scandent shrub Lauraceous medicinal plant, has been used in Chinese traditional medicine as a palliative and an anti-spasmodic. It also shows cytotoxic effects against several tumor cell lines and inhibits marcromolecule biosynthesis. This study investigated the anti-tumor effects of L. strychifolia extract against lung cancer cells using in vitro and in vivo models. Two human lung cancer cell lines A549 (adenocarcinoma) and SBC-3 (small cell carcinoma), and a non-tumor cell line 3T3-L1 (mice fibroblasts) were subjected to L. strychifolia extract treatment. On lung cancer cells, L. strychifolia induced cell growth inhibition in a dose-dependent manner. Conversely, the extract did not show any significant cytotoxic effect on 3T3-L1 cells. Therefore, the extract is specific for tumor cells. Tumor cells treated with L. strychifolia extract showed typical morphological appearance of apoptosis including nuclei fragmentation and cell condensation. The in vivo effects of L. strychifolia extract were investigated in C57BL/6 mice transplanted with Lewis lung cancer (LL-2) cells, and in BALB/c nude mice transplanted with A549 or SBC-3 human lung cancer cells. Oral administration of L. strychifolia extract prolonged survival time and inhibited tumor growth in a dose-dependent manner by inducing apoptosis in the LL-2 cell mice model. Furthermore, in A549 or SBC-3 cell nude mice models, oral administration of L. strychifolia extract also significantly inhibited tumor growth at the 5.0 mg/ml concentration. These findings suggested that the components of L. strychifolia have anticancer activity and may contribute to clinical applications in the prevention and treatment of lung cancer.     

Cytotoxicity of some medicinal plant extracts used in Tanzanian traditional medicine

Using the ethnomedical data approach, some Tanzanian plants that are used in Tanzanian traditional medicine for cancer or non-cancer diseases were collected and evaluated for cytotoxic activity. The antiproliferative effect of the methanolic extracts (10 and 100 microg/ml) of 47 plants was evaluated in vitro on three human cell lines (HeLa, cervical carcinoma; HT29, colon adenocarcinoma; and A431, skin carcinoma). From the nine plants that are used to treat cancer, two plants (22%) exhibited pronounced cytotoxic effect (<25% cell proliferation) at least in one of the tested cell lines. For the 38 plants that are used to treat non-cancer diseases, 14 plants (37%) exhibited pronounced cytotoxic effect (<25% cell proliferation). Cell type cytotoxic specificity was observed in some extracts. Overall, the A431 cells were much more sensitive to most of the extracts than the other cell lines. For the plants that are used as anticancer herbal drugs, our results indicate that there is no correlation between the reported use of these plants and their cytotoxic activity obtained in this study. However, plants that have shown pronounced cytotoxic activity will be evaluated further for the possible isolation of active antitumor compounds.     

Cytotoxicity of plants from Malaysia and Thailand used traditionally to treat cancer

The SRB cytotoxicity assay was used to screen extracts and isolated constituents of some traditional medicinal plants from Malaysia and Thailand against two human cancer cell lines, COR L23 lung cancer cell line and MCF7 breast cancer cell line and the non-cancer MCF5 cell line. Five out of the seven species tested, i.e. Thai Alpinia galanga, Alpinia officinarum, Cayratia japonica, Physalis minima, Tabernaemontana divaricata, exhibited interesting cytotoxicity activity and this is the first report of cytotoxicity from any Cayratia species. Following bioassay-guided fractionation, 1′-acetoxychavicol acetate (48 h exposure against COR L23 cells, IC₅₀ 7.8 μM against MCF7 cells, IC₅₀ 23.9 μM) was isolated as the major cytotoxic component of the Alpinia species, physalin F as the major cytotoxic component of Physalis minima (48 h exposure against COR L23 cells IC₅₀ 0.4 μM against MCF7 cells, IC₅₀ 0.59 μM). The Malaysian Alpinia galanga showed weak activity compared with the Thai sample and this was shown to be due to the relatively high amounts of 1′-acetoxychavicol acetate present in the Thai sample.     

Effects of maple (Acer) plant part extracts on proliferation, apoptosis and cell cycle arrest of human tumorigenic and non-tumorigenic colon cells

Phenolic‐enriched extracts of maple sap and syrup, obtained from the sugar and red maple species (Acer saccharum Marsh, A. rubrum L., respectively), are reported to show anticancer effects. Despite traditional medicinal uses of various other parts of these plants by Native Americans, they have not been investigated for anticancer activity. Here leaves, stems/twigs, barks and sapwoods of both maple species were evaluated for antiproliferative effects against human colon tumorigenic (HCT‐116, HT‐29, Caco‐2) and non‐tumorigenic (CCD‐18Co) cells. Extracts were standardized to total phenolic and ginnalin‐A (isolated in our laboratory) levels. Overall, the extracts inhibited the growth of the colon cancer more than normal cells (over two‐fold), their activities increased with their ginnalin‐A levels, with red > sugar maple extracts. The red maple leaf extract, which contained the highest ginnalin‐A content, was the most active extract (IC₅₀ = 35 and 16 µg/mL for extract and ginnalin‐A, respectively). The extracts were not cytotoxic nor did they induce apoptosis of the colon cancer cells. However, cell cycle analyses revealed that the antiproliferative effects of the extracts were mediated through cell cycle arrest in the S‐phase. The results from the current study suggest that these maple plant part extracts may have potential anticolon cancer effects. Copyright © 2011 John Wiley & Sons, Ltd.     

In vitro estrogenic activities of Chinese medicinal plants traditionally used for the management of menopausal symptoms

The estrogenic activity of 70% EtOH extracts of 32 traditional Chinese medicinal plants, selected according to their reported efficacy for the treatment of menopausal symptoms, was assessed using a recombinant yeast system with both a human estrogen receptor expression plasmid and a reporter plasmid. Among them, 11 (34%) species proved to be active. Polygonum cuspidatum had the highest estrogenic relative potency (RP) (3.28 x 10(-3)), followed by Rheumpalmatum (3.85 x 10(-4)), Cassia obtusifolia (3.49 x 10(-4)), Polygonum multiflorum (2.87 x 10(-4)), Epimedium brevicornum (2.30 x 10(-4)), Psoralea corylifolia (1.90 x 10(-4)), Cynomorium songaricum (1.78 x 10(-4)), Belamcanda chinensis (1.26 x 10(-4)), Scutellaria baicalensis (8.77 x 10(-5)), Astragalus membranaceus (8.47 x 10(-5)) and Pueraria lobata (6.17 x 10(-5)). The EC(50) value of 17beta-estradiol used as the positive control was 0.205+/-0.025 ng/ml (RP=100). This study gave support to the reported efficacy of Chinese medicines used for hormone replacement therapy.     

Screening for antimycotic properties of 56 traditional Chinese drugs

In the present study we screened extracts of 56 widely used dried Chinese medical plants or their parts (TCD) for their antimycotic properties against pathological phyla of Aspergillus fumigatus, Candida albicans, Geotrichum candidum and Rhodotorula rubra. The highest activity against Aspergillus fumigatus was shown by Carthamus tinctorius L. (flos) and Rheum palmatum L. (radix et rhizoma) and against Candida albicans, Scutellaria baicalensis Georgi (radix) had the highest activity. The highest activity against Geotrichum candidum was shown by Agastache rugosa (Fisch et Mey.) O. Ktze. Herba Menthae has moderate antimycotic properties.     

柴胡、黄芩及其配伍提取物含药血清对CVB3m感染乳鼠心肌细胞的保护作用研究

目的:探讨柴胡、黄芩及其配伍提取物保护细胞的不同作用环节和机制。方法:应用"通法"制取3种提取物含药血清,体外培养乳鼠心肌细胞,观察其形态学变化,细胞病变及搏动百分比;MTT法检测CVB3m感染的心肌细胞保护率;检测3天、5天各孔上清液中乳酸脱氢酶(LDH)及天冬氨酸氨基转移酶(AST)的释放量。结果:3组含药血清均不同程度的减轻心肌细胞病变,提高搏动百分比;OD值均明显高于正常对照组(P<0.05);感染CVB3m后3～5天,空白血清组各孔培养液中LDH及AST的释放量迅速上升,含药血清组其释放量明显降低(P<0.05)。结论:3种含药血清均有不同程度的保护细胞作用,黄芩和配伍提取物含药血清对病毒感染后的细胞具有明显保护作用。等量配伍提取物含药血清在体外保护细胞方面没有表现出作用增强的优势。     

In vitro cytotoxicity of some medicinal plants from Georgian Amaryllidaceae

Using an ethnomedical data approach, some Georgian plants, which are used in Georgian traditional medicine for cancer or non-cancer diseases, were collected and evaluated for cytotoxic activity. The cytotoxic effect of the methanol extracts of species from the genera Galanthus and Leucojum was evaluated in vitro on three human cell lines (Hela, ephitheloid cervix carcinoma; HCT-116, colon carcinoma; HL-60, acute myeloid leukaemia). Cell type cytotoxic specificity was observed for some extracts. Overall, the HCT-116 cells were much more sensitive to most of the extracts than were the other cell lines. Plants that showed pronounced cytotoxic activity will be further evaluated for the possible isolation of active antitumour compounds.     

Antimalarial and cytotoxic activities of ethnopharmacologically selected medicinal plants from South Vietnam

Malaria is a major global public health problem and the alarming spread of drug resistance and limited number of effective drugs now available underline how important it is to discover new antimalarial compounds. An ethnopharmacological investigation was undertaken of medicinal plants traditionally used to treat malaria in the South Vietnam. Forty-nine plants were identified, 228 extracts were prepared and tested for their in vitro activity against Plasmodium falciparum, and assessed for any cytotoxicity against the human cancer cell line HeLa and the embryonic lung MRC5 cell line. In a first screening at a concentration of 10 microg/ml, 92 extracts from 46 plants showed antiplasmodial activity (parasite growth inhibition >30%). The IC(50) values of the most active extracts were determined as well as their selectivity towards Plasmodium falciparum in comparison to their cytotoxic effects against the human cell lines. Six plants showed interesting antiplasmodial activity (IC(50) ranging from 0.4 to 8.6 microg/ml) with a good selectivity: two Menispermaceae, Arcangelisia flava (L.) Merr. and Fibraurea tinctoria Lour., and also Harrisonia perforata (Blanco) Merr. (Simaroubaceae), Irvingia malayana Oliv. ex Benn. (Irvingiaceae), Elaeocarpus kontumensis Gagn. (Elaeocarpaceae) and Anneslea fragrans Wall. (Theaceae).     

Evaluation of in vitro antiviral activity in methanol extracts against in fl uenza virus type A from Korean medicinal plants

Methanol extracts from 101 Korean medicinal plants were tested for inhibitory activity against influenza virus type A by means of a modified haemagglutination inhibition (HI) test. MM-57, MM-72, MM-104 and MM-110, four of 101 extracts tested exhibited strong anti-influenza virus type A activity at concentration ranges of 0.78-6.25 mg/mL, 0.78-3.13 mg/mL, 0.78-1.56 mg/mL and 0.0975-0.39 mg/mL, respectively. The extracts MM-57, MM-72 and MM-110 showed very strong anti-influenza virus type A activity in the range 1.56-6.25 mg/mL, 1.56-3.13 mg/mL and 195-390 micro g/mL, respectively. The four methanol extracts were weakly cytotoxic to red blood cells. These results demonstrated that four methanol extracts of Korean medicinal plants exhibit strong anti-influenza virus type A activity, and weak cytotoxic effects. They may inhibit attachment of the virus to the cell and may therefore be used for prophylaxis.     

Cytotoxic activities of flavonoids from two Scutellaria plants in Chinese medicine

The effects of 17 flavonoids, isolated from two flavonoid-rich Scutellaria species (Scutellaria baicalensis Georgi and Scutellaria rivularis Wall) used in traditional Chinese medicine, on HL-60 cells were assessed by WST-8. Ten of the flavonoids inhibited the proliferation of HL-60, as shown by IC50 values used as indexes of the inhibition. 2',3',5,7-tetrahydroxy flavone (IC50=9.5 microM), apigenin (15.0 microM), viscidulin III (17.4 microM), wogonin (17.4 microM) and luteolin (18.4 microM) were more effective than baicalein (23.0 microM) which reportedly inhibits the proliferation of some cancer cell lines. Others were less effective, and oroxylin A stimulated the proliferation. Scutellaria rivularis, used for the treatment of tumors in the clinic, contained flavonoids that were more inhibitive than those in Scutellaria baicalensis. These results are demonstrative of some reasons for the use of Scutellaria rivularis as a crude antitumor drug.     

Identification of chrysoplenetin from Vitex negundo as a potential cytotoxic agent against PANC-1 and a panel of 39 human cancer cell lines (JFCR-39)

Human pancreatic cancer is known to be the most deadly disease with the lowest 5‐year survival rate and is resistant to well known conventional chemotherapeutic drugs in clinical use. Screening of medicinal plants from Myanmar utilizing antiausterity strategy led to the identification of Vitex negundo as one of the medicinal plants having potent preferential cytotoxic activity against PANC‐1 human pancreatic cancer cells. Bioactivity‐guided phytochemical investigation led to the isolation of chrysoplenetin (1) and chrysosplenol D (2) as the active constituents with a PC₅₀ value of 3.4 μg/mL and 4.6 μg/mL, respectively, against PANC‐1 cells. Both these compounds induced apoptosis‐like morphological changes in PANC‐1 cells. Chrysoplenetin was further tested against a panel of 39 human cancer cell lines (JFCR‐39) at the Japanese Foundation for Cancer Research, and 25 cell lines belonging to lung, breast, CNS, colon, melanoma, ovarian, prostate cancer and stomach cancer cell lines were found to be highly sensitive to chrysoplenetin at a submicromolar range. In the JFCR‐39 panel, lung NCI‐H522, ovarian OVCAR‐3 and prostate PC‐3 cells were found to be most sensitive with GI₅₀ of 0.12, 0.18 and 0.17 μm , respectively. The COMPARE analysis suggested that the molecular mode of action of chrysoplenetin was unique compared with the existing anticancer drugs. Copyright © 2011 John Wiley & Sons, Ltd.     

Screening of plants used in Mayan traditional medicine to treat cancer-like symptoms

Aim of the study

To investigate the potential of plants used in Mayan traditional medicine to treat cancer-like symptoms using the Mayan ethnobotany literature, and evaluate their organic extracts for in vitro cytotoxic activity on cancer cell lines.

Materials and methods

The selection of the plants studied in this investigation was based on the Mayan ethnobotanical information provided by different literature sources. Extracts were obtained by maceration with methanol for 72 h of each plant part used and evaporated in vacuo to give the corresponding dried extract. Each methanol extract was tested for its cytotoxicity using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay performed in 96-well tissue plates on seven cancer cell lines, lung carcinoma (A549), cervix adenocarcinoma (HeLa), laryngeal carcinoma (Hep-2), nasopharynx carcinoma (KB), breast adenocarcinoma (MCF-7), prostate adenocarcinoma (PC-3), and cervix squamous carcinoma cells (SiHa), as well as normal human embryonic kidney cell line (HEK-293). Cell proliferation/viability was spectrophotometrically assessed at 540 nm after addition of MTT.

Results

51 plants were found in the literature to be used for the treatment of symptoms suggestive of cancer, 21 were chosen to evaluate the cytotoxic activity. Aeschynomene fascicularis root bark extract showed a pronounced cytotoxic activity on Hela and KB cell lines and Bonellia macrocarpa stem and root bark extracts showed similar prominent activities on KB cells.

Conclusion

21 plants were selected according to their use in the treatment of cancer-like symptoms recorded in the ethnobotanical literature. Plant extracts prepared from Aeschynomene fascicularis root bark and Bonellia macrocarpa stem and root bark have been selected for extensive studies leading to the isolation of the active constituents.     

黄芩的炮制与临床效用分析

归纳和分析黄芩的常用炮制方法及其临床效用。认为生黄芩长于清热泻火,炒黄芩长于清热燥湿安胎,酒黄芩长于清肺凉肝,黄芩炭长于清热凉血。