裂蹄木层孔菌乙酸乙酯萃取物对人肝癌细胞SMMC-7721的抑制作用研究

目的：探讨裂蹄木层孔菌乙酸乙酯萃取物在体外的抗肝癌活性。方法：采用磺酰罗丹明染色法（SRB法）,对人肝癌细胞SMMC-7721进行体外抗肿瘤实验。结果：裂蹄木层孔菌乙酸乙酯萃取物对人肝癌细胞SMMC-7721表现出比较明显的高浓度杀死和中低浓度抑制的效果,且抑制率随萃取物浓度的升高而增大,呈剂量效应关系;其半数抑制浓度（IC50）为21.5μg.mL-1。结论：裂蹄木层孔菌乙酸乙酯萃取物对人肝癌细胞SMMC-7721具有比较明显的抑制作用。     

柿叶不同极性部位对H22腹水瘤及H22,S180实体瘤小鼠的抑瘤作用

目的:研究柿叶不同极性部位对小鼠H22及S180抑瘤作用的影响。方法:柿叶乙醇提取物分别用三氯甲烷、乙酸乙酯、正丁醇萃取,得到相应不同极性部位;乙醇提取后的柿叶晾干后水煮,得水提部位。分别建立H22腹水瘤小鼠模型和H22,S180实体瘤小鼠模型,将荷瘤小鼠随机分为空白组,模型组,环磷酰胺组(0.1 g·kg-1),不同极性部位(柿叶三氯甲烷、柿叶水提、柿叶乙酸乙酯、柿叶正丁醇)高、中、低剂量组,连续ig 10 d。观察各用药组对H22腹水瘤小鼠腹围、腹水抑制率和肝组织病理学形态的影响,以及对H22和S180实体瘤小鼠摄食量、体重、抑瘤率、生命延长率、胸腺和脾脏系数等的影响。结果:与模型组比较,柿叶乙酸乙酯部位、水提部位和正丁醇部位能明显减少H22腹水瘤小鼠的腹水量,不同程度改善肝细胞肿胀、溶解等状况;不影响H22和S180实体瘤小鼠的摄食量,能明显提高荷瘤小鼠的抑瘤率、延长生命延长率,增加胸腺系数和脾脏系数(P<0.01,P<0.05)。结论:柿叶乙酸乙酯部位、水提部位和正丁醇部位对H22和S180荷瘤小鼠有不同程度的抑瘤作用,可为柿叶抑瘤作用的有效部位。柿叶乙酸乙酯部位对肝癌H22小鼠(包括实体瘤和腹水瘤)的影响比对肉瘤S180小鼠更显著。     

Study of the antitumor potential of Bidens pilosa (Asteraceae) used in Brazilian folk medicine

AIM OF THE STUDY: Bidens pilosa (L.) (Asteraceae) is a medicinal plant traditionally used in Brazil for treating conditions that can be related to cancer. Therefore the present study was carried out to evaluate the antitumor activity of extracts obtained from the aerial parts of this plant species. MATERIALS AND METHODS: The crude hydroalcoholic extract (HAE) (water:alcohol, 6:4) and solvent fractions (chloroform=CHCl3,ethyl acetate=EtOAc, methanol=MeOH) were assessed for cytotoxicity assay by the brine shrimp and hemolytic, MTT and NRU assays. The antiproliferative potential of the crude extract and fractions was investigated in vivo using the Ehrlich ascites carcinoma (EAC) in isogenic Balb/c mice that were administered intraperitoneally 150 and 300 mg/kg body weight per day for nine days beginning 24 h after tumor inoculation. RESULTS: In in vitro cytotoxicity using Ehrlich ascites carcinoma cell line assay CHCl3 extract proved to be more toxic than the crude HAE with an IC(50) of 97+/-7.2 and 83+/-5.2 microg/mL to NRU and MTT, respectively. Histomorphological evaluations indicated that the treatment with CHCl3 and HAE extracts significantly reduced (P<0.05) body weight, abdominal circumference, tumor volume, packed cell volume and viable cell count, when compared to EAC control group. Furthermore, nonviable tumor cell count increased significantly (P<0.01) only under treatment with CHCl3 or HAE, and this was accompanied by a marked percentage increase in life span (54.2 and 41.7%, respectively). Biochemical assays revealed that CHCl3 and HAE extracts were also able to decrease serum LDH activity (39.5 and 30.6%) and GSH concentration (94.6 and 50.7%) in ascitic fluid, respectively. CONCLUSION: The chloroform fraction showed the best and methanolic the worst antitumor activity.     

Antioxidant and antihepatotoxic activities of Phellinus rimosus (Berk) Pilat

The antioxidant and antihepatotoxic activities of a wood inhabiting macrofungus, Phellinus rimosus were studied. The superoxide anion scavenging, Fe(2+)-ascorbate induced lipid peroxidation inhibiting, hydroxyl radical scavenging and nitric oxide scavenging activities of the ethyl acetate extract were determined. The results indicated that ethyl acetate extract of P. rimosus exhibited significant in vitro antioxidant activity. The ethyl acetate extract of P. rimosus also showed potent antihepatotoxic activity against carbontetrachloride-induced acute toxicity in rat liver. The amelioration of liver toxicity by the ethyl acetate extract was evident from its significant effect on the levels of serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT) and serum alkaline phosphatase (ALP). The results suggest that hepatoprotective effect of P. rimosus is possibly related to the free radical scavenging activity.     

Immunomodulatory and antitumor activity of Piper longum Linn. and piperine

Alcoholic extract of the fruits of the plant Piper longum and its component piperine was studied for their immunomodulatory and antitumor activity. Alcoholic extract of the fruits was 100% toxic at a concentration of 500 microg/ml to Dalton's lymphoma ascites (DLA) cells and 250 microg/ml to Ehrlich ascites carcinoma (EAC) cells. Piperine was found to be cytotoxic towards DLA and EAC cells at a concentration of 250 microg/ml. Alcoholic extract and piperine was also found to produce cytotoxicity towards L929 cells in culture at a concentration of 100 and 50 microg/ml, respectively. Administration of alcoholic extract of Piper longum (10 mg/dose/animal) as well as piperine (1.14 mg/dose/animal) could inhibit the solid tumor development in mice induced with DLA cells and increase the life span of mice bearing Ehrlich ascites carcinoma tumor to 37.3 and 58.8%, respectively. Administration of Piper longum extract and piperine increased the total WBC count to 142.8 and 138.9%, respectively, in Balb/c mice. The number of plaque forming cells also enhanced significantly by the administration of the extract (100.3%) and piperine (71.4%) on 5th day after immunization. Bone marrow cellularity and alpha-esterase positive cells were also increased by the administration of Piper longum extract and piperine.     

Potent in vitro cytotoxic and antioxidant activity of Careya arborea bark extracts

Careya arborea is used in traditional medicine for the treatment of tumors and other ailments. The successive chloroform and ethyl acetate extracts and crude 50% methanol extract exhibited potent cytotoxicity against cancerous RD, HEp-2 and HeLa cell lines. They were found to be safe against the normal Vero cell line. The methanol and aqueous extracts possessed strong antioxidant activity against many oxidants in the in vitro antioxidant screening. The total phenol content of these extracts was found to be high. The results suggest strong cytotoxic and antioxidant properties and support the ethnomedical claims for the plant.     

Antitumor activity of Hypericum hookerianum against DLA induced tumor in mice and its possible mechanism of action

A large number of plants belonging to the genus Hypericum and their phytoconstituents are known to possess potent anticancer nature. Earlier studies from our laboratories indicated a strong cytotoxic nature of the methanol extract of Hypericum hookerianum stem (MEHH). In the present study, the in vivo antitumor activity of MEHH against the Dalton's lymphoma ascitic (DLA) model was determined at 100 and 200 mg/kg body weight given orally for 10 days. The results indicate that administration of the extract not only increased the survival of animals with ascites tumor, decreased the body weight induced by the tumor burden and reduced the packed cell volume and viable tissue cell count, but also altered many hematological parameters changed during tumor progression indicating the potent antitumor nature of the extract. Hematological and biochemical analysis were carried out to prove the anticancer and antioxidant nature of the extract.     

青龙衣不同萃取部位抗肿瘤活性研究

目的研究青龙衣乙醇提取物及不同溶剂萃取部位对肿瘤细胞的体外抑制作用，筛选青龙衣抗肿瘤活性部位。方法采用四甲基偶氮唑蓝（MTT）法，选用4种细胞株（SGC-7901，HepG-2，HCT-8，Capan-2）进行体外实验，对青龙衣不同萃取部位的抗肿瘤活性进行筛选。结果青龙衣乙醇提取物、石油醚部位、氯仿部位、乙酸乙酯部位对肿瘤细胞均有不同程度的抑制作用。其中青龙衣乙醇提取物对SGC-7901，HepG-2，HCT-8，Capan-2的IC50分别为47．18，31．12，35．45，27．81mg／L；石油醚部位对SGC-7901，HepG．2，HCT．8，Capan-2的IC50分别为56．72，57．14，25．96，15．21mg／L；氯仿部位对SGC-7901，HepG-2，HCT-8，Capan-2的IC50分别为32．08，29．59，32．47，60．72mg／L；乙酸乙酯部位对SGC-7901，HepG-2，HCT-8，Capan-2的IC50分别为35．79，35．48，24．48，25．46mg／L。正丁醇部位和水溶性部位对各肿瘤细胞无抑制作用。结论青龙衣的乙醇提取物、石油醚部位、氯仿部位、乙酸乙酯部位有一定的细胞毒作用，石油醚部位、氯仿部位、乙酸乙酯部位初步确定为青龙衣抗肿瘤活性部位。     

山核桃外果皮提取物抗肿瘤活性研究

目的研究山核桃外果皮抗肿瘤活性部位。方法利用系统溶剂分离法,对山核桃外果皮进行部位分离,采用MTT法分别检测水提取物、甲醇提取物、石油醚提取物、醋酸乙酯提取物对小鼠肺癌细胞3LL、人乳腺癌细胞MCF-7、人肝癌细胞QGY-7701、人胃癌细胞BGC-823等4种肿瘤细胞株的生长抑制情况。结果水提取物对上述肿瘤细胞抑制作用均不明显,甲醇和石油醚提取物对4种肿瘤细胞有抑制作用,醋酸乙酯提取物对4种肿瘤细胞有明显的抑制效果,且呈一定的浓度-效应关系。结论山核桃外果皮的甲醇提取物、石油醚提取物及醋酸乙酯提取物具有一定的体外抗肿瘤作用。     

Antitumor activity of extracts and compounds from the rhizomes of Veratrum dahuricum

The antitumor activity of six extracts (ethanol extract, petroleum ether fraction, CHCl(3) fraction, ethyl acetate fraction, n-butanol fraction and total alkaloids) from the rhizomes of Veratrum dahuricum, and six compounds (veratramine (1), jervine (2), germine (3), veramitaline (4), veratrosine (5) and cyclopamine (6)) from the ethanol extract were investigated in vitro. The 12 samples exhibited cytotoxic activity against human tumor cell lines A549, PANC-1, SW1990 and NCI-H249. Among these samples, CHCl(3) fraction, the total alkaloids, compounds 1 and 6 showed higher inhibitory activity, compound 3 selectively exhibited significant cytotoxicity to SW1990 and NCI-H249.     

海南龙血树抗肿瘤新用途研究

目的:筛选海南龙血树的抗肿瘤活性部位.方法:分别用溶剂萃取法和大孔吸附树脂柱层析法对海南龙血树的95%乙醇提取物进行分段处理,利用MTT法测定各提取部位体外抗肿瘤活性.结果:氯仿提取物、乙酸乙酯提取物和正丁醇提取物对体外肿瘤细胞表现出较强的抑制活性,甲醇洗脱物显示了弱活性,水提取、水洗脱物和50%甲醇-水洗脱物则没有活性.在各提取物中氯仿提取物活性最强.结论:氯仿提取部位是海南龙血树主要的体外抗肿瘤活性部位.     

Antibacterial activity of Curcuma longa L. against methicillin-resistant Staphylococcus aureus

Methicillin-resistant Staphylococcus aureus (MRSA) has been emerging worldwide as one of the most important hospital and community pathogens. Therefore, new agents are needed to treat MRSA associated infections. The present study investigated the antimicrobial activity of ethyl acetate, methanol and water extracts of Curcuma longa L. (C. longa) against MRSA. The ethyl acetate extract of C. longa demonstrated a higher antibacterial activity than the methanol extract or water extract. Since the ethyl acetate extract was more active than the other extracts, the study examined whether the ethyl acetate extract could restore the antibacterial activity of beta-lactams and alter the MRSA invasion of human mucosal fibroblasts (HMFs). In the checkerboard test, the ethyl acetate extract of C. longa markedly lowered the MICs of ampicillin and oxacillin against MRSA. In the bacterial invasion assay, MRSA intracellular invasion was significantly decreased in the presence of 0.125-2 mg/mL of C. longa extract compared with the control group. These results suggest that the ethyl acetate extract of C. longa may have antibacterial activity and the potential to restore the effectiveness of beta-lactams against MRSA, and inhibit the MRSA invasion of HMFs.     

In vitro antiproliferative and antioxidant activities and total phenolic contents of the extracts of Melastoma malabathricum leaves

The present study aims to determine the in vitro antiproliferative and antioxidant activities of various extracts from the leaves of Melastoma malabathricum using various established in vitro assays. The aqueous extract inhibited the proliferation of Caov-3 and HL-60 cell lines, while the chloroform extract exhibited antiproliferative activity against the Caov-3, HL-60, and CEM-SS cell lines. The methanol extract demonstrated antiproliferative activity against more cell lines, including the MCF-7, HeLa, Caov-3, HL-60, CEM-SS, and MDA-MB-231 cancer cell lines. Interestingly, all extracts did not inhibit the proliferation of 3T3 cells, thus indicating their noncytotoxic properties. Unlike the chloroform extracts, the aqueous and methanol extracts of M malabathricum (20, 100, and 500 μg/ml) produced high antioxidant activity for the superoxide scavenging assay with only the 500 μg/ml aqueous and methanol extracts exhibited high activity for the 2,2-diphenyl -1-picrylhydrazyl radical scavenging assay. The total phenolic content recorded for the aqueous, methanol, and chloroform extracts were 3344.2 ± 19.1, 3055.1 ± 8.7, and 92.5 ± 7.3 mg/100 g of gallic acid, respectively. The M malabathricum leaves possessed potential antiproliferative and antioxidant activities that could be attributed to its high content of phenolic compounds.     

Antioxidant activity of Aporosa lindleyana root

Four successive and two crude extracts of Aporosa lindleyana Baill. root were tested for antioxidant activity using standard in vitro and in vivo models. The successive methanol and ethyl acetate and crude 50% methanol extracts showed antioxidant activity with IC50 values 3.51+/-0.27, 6.09+/-1.00 and 7.34+/-0.46 microg/ml, respectively, in DPPH method. In the nitric oxide radical inhibition method, the successive ethyl acetate, petroleum ether and methanol extracts showed antioxidant activity. The successive methanol extract at 100 and 200 mg/kg body weight administered for 5 days prior to CCl4 treatment caused a significant increase in the levels of catalase and SOD and a significant decrease in the level of TBARS in liver, kidney and blood, when compared to CCl4 treated control. These results indicate strong antioxidant nature of Aporosa lindleyana root. The in vitro cytotoxicity studies against normal Vero cell lines indicate non-toxic nature of the root extracts. The study provides a proof for the ethnomedical and reported biological activities.     

人工虫草菌HK-1与天然虫草提取物的抗肿瘤活性比较

目的比较人工虫草菌HK-1与天然虫草提取物抗肿瘤活性及主要化学成分。方法人工虫草菌HK-1与天然虫草分别用石油醚、醋酸乙酯、乙醇和水提取。用MTT法测定各提取物对小鼠黑色素瘤细胞B16、人肝癌细胞HepG2、人乳腺癌细胞MCF-7和类前骨髓白血病细胞HL-60的细胞毒作用。对活性提取物进一步用动物模型检测其体内抗肿瘤作用。高效液相色谱法测定提取物中的化学成分。结果对于小鼠黑色素瘤细胞B16,所有虫草菌HK-1提取物的细胞毒作用均比天然虫草提取物的作用强,其中以醋酸乙酯提取物的细胞毒作用最强。虫草菌HK-1醋酸乙酯提取物对4种肿瘤细胞的细胞毒作用均比天然虫草醋酸乙酯提取物的作用强;体内实验也表明虫草菌HK-1醋酸乙酯提取物可以抑制肿瘤的生长。对提取物化学成分的分析表明麦角甾醇和腺苷可能是虫草菌HK-1中具有抗肿瘤活性的成分。结论人工虫草菌HK-1比天然虫草具有更强的抗肿瘤活性,是有开发潜力的抗肿瘤候选药物。     

蒲葵根提取物的体外抗肿瘤实验研究

目的:用体外细胞培养法研究蒲葵根提取物对七种肿瘤细胞株生长的抑制作用。方法:采用MTT法、细胞集落形成法、生长曲线法测定蒲葵根提取物对白血病细胞株L1210和P388D1、宫颈癌细胞株Hela、人胃癌细胞株SGC7901、黑色素瘤细胞株B16、神经性肿瘤细胞株NG108-15、人肝癌细胞株Hele 7404生长的抑制情况。结果:MTT法、细胞集落形成法、生长曲线法测定的结果均显示,当蒲葵根提取物浓度在5.0μg/m l以上时,7类肿瘤细胞株的生长均受到明显抑制。结论:蒲葵根提取物在体外具有抗肿瘤作用。     

Evaluation of anticancer activity of ethanol extract of Sesbania grandiflora (Agati Sesban) against Ehrlich ascites carcinoma in Swiss albino mice

Ethno pharmacological relevance

The plant Sesbania grandiflora (Fabaceae) is commonly known as “Sesbania” and “agathi” in ayurvedic system of medicine and reputed in the indigenous medicine in India. It is also known as “Agati Sesban” or “humming bird tree” in English. All parts of this unique plant are useful and have a wide spectrum of medicinal properties. The plant has various uses in folk and traditional medicines for headache, swellings, anemia, bronchitis, pains, liver disorders and tumors.

Aim of the study

The objective of the present study was to explore the anticancer activity of the ethanol extract of Sesbania grandiflora against Ehrlich ascites carcinoma (EAC)-bearing Swiss albino mice.

Materials and methods

Anticancer activity of ethanol extract of Sesbania grandiflora (EESG) of both leaves and flowers were evaluated in Swiss albino mice against Ehrlich Ascites Carcinoma (EAC) cell line at the doses of 100 and 200 mg/kg body weight intraperitoneally. The extracts were administered for 14 consecutive days. Twenty-four hours of last dose and 18 h of fasting, the mice were sacrificed and the anticancer effect of EESG was assessed by evaluating tumor volume, viable and nonviable tumor cell count, tumor weight, hematological parameters and biochemical parameters of EAC bearing host.

Results

Sesbania grandiflora extracts showed significant decrease in (p < 0.01) tumor volume, viable cell count, tumor weight and elevated the life span of EAC bearing mice. Hematological profile such as RBC, hemoglobin and lymphocyte count reverted to normal level in EESG treated mice. The extracts significantly (p < 0.05) decreased the levels of lipid peroxidation and significantly (p < 0.05) increased the levels of GSH, SOD and CAT.

Conclusion

The results showed that the ethanol extract of Sesbania grandiflora was effective in inhibiting the tumor growth in ascitic models and that is comparable to 5-Fluorouracil.     

In vitro cytotoxicity and antitumour properties of Hypericum mysorense and Hypericum patulum

The methanol extracts of the aerial parts of Hypericum mysorense and Hypericum patulum were tested for in vitro cytotoxicity on HEp-2, RD and Vero cell lines and antitumour activity using DLA and HEp-2 cell lines. The cell viability and morphological changes were assessed. Of these extracts, Hypericum patulum (stem) extract showed strong cytotoxicity against all the cell lines used. The CTC50 of the Hypericum patulum (stem) extract was 1.71 microg/mL for HEp-2, 1.53 microg/mL for RD and 2.23 microg/mL for Vero cell lines. The Hypericum patulum (leaves) and Hypericum mysorense (aerial parts) extracts showed moderate cytotoxicity and Hypericum patulum (aerial parts) extract did not show any cytotoxicity up to 1,000 microg/mL concentration. In the clonogenic assay, no colony formation was observed at a concentration of 300 micro g/mL and above for Hypericum mysorense (aerial parts), 400 microg/mL and above for Hypericum patulum (leaves) and 500 microg/mL and above for Hypericum patulum (stem) extracts. In the short term antitumour studies using DLA cells, 50% viability was observed in the concentration range 100-200 microg/mL for Hypericum patulum (leaves and stem) and 200-400 microg/mL for Hypericum mysorense (aerial) extract. In the long term antitumour activity using the HEp-2 cell line, no colony formation was observed over a concentration of 1.6 microg/mL for the Hypericum patulum (stem) extract.     

Antibacterial activity of Quercus ilex bark's extracts

The antibacterial activity of different extracts of Quercus ilex bark (Fagaceae) was studied in vitro against seven reference strains of bacteria by using a disc-diffusion method and agar-dilution method. The ethyl acetate extract (QE), n-butanol extract (QB) and final aqueous layer (QA) were effective against all bacterial strains tested at MICs ranging from 128 to 512 microg/ml. The n-hexane extract (QH) and dichloromethane extract (QD) showed no activity.     

Evaluation of antitumor activity and in vivo antioxidant status of Anthocephalus cadamba on Ehrlich ascites carcinoma treated mice

Ethnopharmacological relevance

Anthocephalus cadamba (Roxb.) Miq. (Family: Rubiaceae) is commonly known as “Kadamba” in Sanskrit and Hindi in India. Various parts of this plant have been used as a folk medicine for the treatment of tumor, wound healing, inflammation and as a hypoglycemic agent.

Aim of study

The purpose of this investigation was to evaluate the antitumor activity and antioxidant status of defatted methanol extract of A. cadamba (MEAC) on Ehrlich ascites carcinoma (EAC) treated mice.

Materials and methods

In vitro cytotoxicity assay has been evaluated by using the trypan blue method. The determination of in vivo antitumor activity was performed by using different EAC cells (2×10⁶ cells, i.p.) inoculated mice groups (n=12). The groups were treated for 9 consecutive days with MEAC at the doses of 200 and 400 mg/kg b.w. respectively. After 24 h of last dose and 18 h of fasting, half of the mice were sacrificed and the rest were kept alive for assessment of increase in life span. The antitumor potential of MEAC was assessed by evaluating tumor volume, viable and nonviable tumor cell count, tumor weight, hematological parameters and biochemical estimations. Furthermore, antioxidant parameters were assayed by estimating liver and kidney tissue enzymes.

Results

MEAC showed direct cytotoxicity on EAC cell line in a dose dependant manner. MEAC exhibited significant (P<0.01) decrease in the tumor volume, viable cell count, tumor weight and elevated the life span of EAC tumor bearing mice. The hematological profile, biochemical estimations and tissue antioxidant assay were reverted to normal level in MEAC treated mice.

Conclusion

Experimental results revealed that MEAC possesses potent antitumor and antioxidant properties. Further research is going on to find out the active principle(s) of MEAC for better understanding of mechanism of its antitumor and antioxidant activity.