Effect of several d-morphinans on ascites tumors in mice

Dextromethorphan and its analogues (DM 16, DM 34, DM 72, DM 75 and DM 96) were examined for their effect on Ehrlich ascites carcinoma or ascites sarcoma-180 in female mice of the ddY strain. The suspension of Ehrlich carcinoma cells or sarcoma-180 cells was prepared from mice at 10 days after i.p. inoculation of the cells, using Hanks' balanced salt solution, and the cell suspension was inoculated i.p. into mice (2 X 10(6) viable cells/mouse). The chemicals dissolved in physiological saline containing 5% HCO-60 were then injected i.p. into the mice once daily for 5 successive days (5-40 mg/kg/day). In addition, mice given the tumor cells were treated with the saline containing 5% HCO-60 alone for 5 days (untreated mice). In groups of mice bearing Ehrlich ascites carcinoma or ascites sarcoma-180, the mean survival time of mice treated with 20-40 mg/kg/day of DM 96 was more than twice that of the corresponding untreated mice. The mean survival time of mice treated with 20 mg/kg/day of DM 96 was also longer than that of mice treated with 40 mg/kg/day of the other chemicals, irrespective of the ascites tumors. Concerning these survival times, the LD50 (i.p.) of DM 96 in mice differed slightly from that of other chemicals (88 mg/kg and 77-106 mg/kg). These results indicate that DM 96 is more active than the other chemicals against the ascites tumors in mice.     

从海南哥纳香中分离的一种新化合物──海南哥纳香醇甲的抗肿瘤作用

体外用细胞生长曲线测定法、MTT试验、软琼脂集落形成分析法,及体内对移植性肿瘤实验,研究了海南哥纳香醇甲(GHM-10)的抗肿瘤作用,结果表明:GHM-10对肿瘤细胞有较强的抑制作用,IC₅₀在2μg·ml^-1左右;对正常细胞影响较小,骨髓祖细胞的敏感性则更低;耐药的KB/VCR200细胞及其亲本KB细胞具有相似的敏感性。GHM-10对HL-60细胞无分化诱导作用。GHM-10对实体型肝癌H22小鼠、Lewis肺癌小鼠及腹水型S180小鼠均有明显的治疗作用。     

Inhibitory effects of naringenin on tumor growth in human cancer cell lines and sarcoma S-180-implanted mice

We have investigated the effect of naringenin (NGEN) on tumor growth in various human cancer cell lines and sarcoma S-180-implanted mice. NGEN showed cytotoxicity in cell lines derived from cancer of the breast (MCF-7, MDA-MB-231), stomach (KATOIII, MKN-7), liver (HepG2, Hep3B, Huh7), cervix (Hela, Hela-TG), pancreas (PK-1), and colon (Caco-2) as well as leukemia (HL-60, NALM-6, Jurkat, U937). NGEN-induced cytotoxicity was low in Caco-2 and high in leukemia cells compared to other cell lines. NGEN dose-dependently induced apoptosis, with hypodiploid cells detected in both Caco-2 and HL-60 by flow cytometric analysis. In vivo, NGEN inhibited tumor growth in sarcoma S-180-implanted mice, following intraperitoneal or peroral injection once a day for 5 d. Naringin (NG) also inhibited tumor growth by peroral injection but not intraperitoneal injection. NGEN, one of the most abundant flavonoids in citrus fruits, may have a potentially useful inhibitory effect on tumor growth.     

昂立品山抑瘤口服液抗小鼠肿瘤实验研究

目的：评价昂立品山抑瘤口服液对小鼠H22肝癌和S180肉瘤的抑瘤作用。方法：小鼠预先给予昂立品山抑瘤口服液每天10，20，30ml/kg，连用21天，然后皮下接种肿瘤，继续给予口服液7天。疗效评价采用瘤体称重法。结果：昂立品山抑瘤口服液能够明显抑制以上肿瘤的生长，它对小鼠H22肝癌和S180肉瘤的抑制率分别达到41％和44％（30ml/kg)，并增加小鼠体重。结论：在本试验条件下，昂立品山抑瘤口服液能够明显抑制小鼠H22肝癌和S180肉瘤的生长，改善小鼠的营养状态。     

赖氨酸锗和环磷酰胺合用对小鼠S-180肉瘤抑瘤作用

赖氨酸锗(Ge401)是国内新近研制的含微量元素锗有机物。测得小鼠gi LD_(50)为9.26g/kg,ip LD_(50)为5.62g/kg;采用ig、ip、iv途径给药,对小鼠S-180肉瘤均有显著抑瘤作用,其中iv给药的抑瘤率(55%)最高;Ge401(30mg/kg·5d~(-1))和环磷酰胺(30mg/kg·2d~(-1))合用具有明显增强抑瘤作用。     

The potentiation of the antitumor activity but not toxicity of bleomycin by 3-aminobenzamide

Our previous studies have demonstrated that 3-aminobenzamide (3AB), an inhibitor of adenosine diphosphate-ribosyl transferase (ADPRT) could enhance the cytotoxicity (in vitro) and antitumor activity (in vivo) of bleomycin (BLM) A5 and peplomycin (PEP) against S-180, hepatoma and Ehrlich ascites carcinoma (EAC). In this study, it was shown that the inhibition rates (INR's) of S-180 in two experiments were increased from 42.5 and 46.1% to 66.2 and 75.9% when BLM 2.5 mg/kg/day x 8 was combined with 3AB 385.4 mg/kg/day x 8, while the decrease of body weight could not be enhanced. BLM at a dose of 5 mg/kg/day x 8 gave INR's of 64.8 and 75%, similar to the combined group but decreased the body weight more significantly. However, the addition of 3AB 385.4 mg/kg/day to BLM did not increase the acute toxicity of BLM alone. There was no significant difference of change of the body weight and subacute toxicity between the BLM and BLM + 3AB group. There was no difference of peripheral blood white cell count and the pathomorphological and ultrastructural change, wet weight and hydroxyproline content (to reflect the collagen content) of the lung of the mice between BLM alone and BLM + 3AB group. Therefore, the study provided experimental evidences for the reasonable use of nontoxic ADPRT inhibitors in adjunct to the chemotherapy of BLM in cancers.     

抗肿瘤药物的研究Ⅲ. 数种锑胺羧螯合物对实验肿瘤的作用

1.锑胺羧螯合物是一种新型的抗肿瘤药物,应用Sb-26(EDTA-SbNa)、Sb-57(PDTA-SbNa)、Sb-66(HEDT-Sb)和Sb-71(ATA-Sb)分别为15—20、30—50、25—30和20—40毫克/公斤剂量时,均能显著地抑制小白鼠Ehrlich 腹水瘤的生长,平均延长生存时间4—22天,延长率36—147%.上述剂量对大白鼠Guerin 氏癌也有抑制作用,抑制率为58—70%.后3个药物,还能使小白鼠梭形细胞肉瘤腹水型的生存时间延长5—16天,延长率50—160%,其中以Sb-71的疗效最著.Sb-26、Sb-57、Sb-71、Sb-66对肉瘤180和AK 肉瘤及前3者对Ehrlich 固体瘤和淋巴白血病固体型的实验结果,除Sb-71对肉瘤180有抑制作用外,其他均无疗效.2.4 类锑化合物:3个(月弟)酸化合物(Sb-8,Sb-11和Sb-42)及1个酒石酸锑(Sb-15),与螯合的间苯二酚锑(Sb-64)和8羟基喹啉锑(Sb-85)各1个,对Ehrlich 腹水瘤的实验结果,均无明显疗效.3.小白鼠的急性半数致死量,Sb-57和Sb-71分别为131和62毫克/公斤,亚急性半数致死量分别为75和58毫克/公斤.