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An experimental study of 300 mice exposed to pitch(3 gm.dissolved in 10 ml.of 80% benzene solution)obtained from 4 different sources,name- ly Anshan coal-tar pitch,Yu-men petroleum pitch,Dairen petroleum pitch or commonly known as Russian crude oil and the Asia Oil Company, USA,was carried out over a period of 350 days. From the beginning a group of these experimen- tal animals was exposed to artificial sun-ray for 2 hours a day.The results of our experiment indicate that pathological changes of different degrees...

An experimental study of 300 mice exposed to pitch(3 gm.dissolved in 10 ml.of 80% benzene solution)obtained from 4 different sources,name- ly Anshan coal-tar pitch,Yu-men petroleum pitch,Dairen petroleum pitch or commonly known as Russian crude oil and the Asia Oil Company, USA,was carried out over a period of 350 days. From the beginning a group of these experimen- tal animals was exposed to artificial sun-ray for 2 hours a day.The results of our experiment indicate that pathological changes of different degrees of severity,such as chronic dermatitis and tumor formation,were the commonest effect of pitch on skin both in the exposed and non-ex- posed groups while the control group(exposed to 80% benzene only)showed only slightly acute dermatitis. The pathological changes as observed both in gross appearances and histological findings are given in detail. The course of tumor formation as found in both the exposed and the non-exposed groups may be classified in the order of time sequence as benign squamous papilloma,malignant squamous papilloma and finally squamous-celled carcinoma; also a few cases of sarcoma and a few cases of so- called“Myoblastoma”. Through the action of photosensitivity to the exposed group,the prolongation of the latent period of tumor formation,the effectiveness in the development of dermatitis and malignant changes in tumors were clearly observed in the process of the pathological changes. The relative potency of the carcinogenic pitch obtained from the above sources has been calculated by means of the statistical analysis of both the incidence and the length of time for the development of the cutaneous tumors.

(一)四种来源不同的沥青(鞍山煤焦油沥青、西北玉门石油沥青、大连石油沥青、和美国亚细亚公司石油沥青)经涂抹小白鼠的实验证明具有引起皮肤各种的病理变化的作用。其中包括慢性渗出性皮炎;慢性炎性上皮结缔组织增生;良性皮肤乳头状瘤;皮肤鳞状细胞。此外也引起了少数的肉瘤和“肌母细胞痛”。皮肤瘤发生的潜伏期由62天至406天不等。(二)光感作用可以加剧及加速煤焦油沥青皮肤炎的进展,和发炎皮肤的角化现象。至于对沥青致作用本实验未能证实其有显著的影响。(三)根据四种来源不同的沥青所引起皮肤良性与恶性病变的发病率和潜伏期的长短,可将其毒性的强弱顺序排列如下:(1)鞍山煤焦油沥青,(2)美国亚细亚公司石油沥青,(3)大连石油沥青(苏联原油),(4)西北玉门石油沥青。即煤焦油沥青毒性远较石油沥青为强。国产石油沥青的毒性较外产石油沥青的毒性为弱。

The antitumor activity of Sb-derivatives of complexones has not yet been reported in the literature.In this work we found that Sb-26 (Sb Na ethylenediamine tetraacetate 15—20 mg/kg), Sb-57(Sb Na propylenediamine tetraacetate 30—50 mg/kg),Sb-66(Sb β-hydroxyethyl imino- diacetic acid 25—30 mg/kg)and Sb-71(Sb ammonia triacetic acid 20—40 mg/kg)could significantly inhibit the growth of Ehrlich ascites carcinoma of mice and prolonged the survival time for 4—22 days(36—147%,P<0.05)in comparison with the control group.These...

The antitumor activity of Sb-derivatives of complexones has not yet been reported in the literature.In this work we found that Sb-26 (Sb Na ethylenediamine tetraacetate 15—20 mg/kg), Sb-57(Sb Na propylenediamine tetraacetate 30—50 mg/kg),Sb-66(Sb β-hydroxyethyl imino- diacetic acid 25—30 mg/kg)and Sb-71(Sb ammonia triacetic acid 20—40 mg/kg)could significantly inhibit the growth of Ehrlich ascites carcinoma of mice and prolonged the survival time for 4—22 days(36—147%,P<0.05)in comparison with the control group.These com- pounds at the above mentioned dosages inhibited also the growth of Guerin’s carcinoma.The degree of inhibition was about 58—70%(P<0.05).The survival time of mice bearing spindle cell sarcoma(in ascitic form)was also prolonged for 5—16 days(50—160%,P<0.05)by treatment with the latter three drugs,among which Sb-71 was most active. Experiments were carried out on mice bearing sarcoma 180 or sarcoma AK treated with Sb-26,Sb-57,Sb-71 or Sb-66 and on mice bearing Ehrlich carcinoma or lymphatic leucemia (solid form)treated with the former three drugs.It was found that only Sb-71 possessed certain inhibitory action on sarcoma 180. In the present study,Sb-8,Sb-11,Sb-42,Sb-15,Sb-64 and Sb-85 were all lacking in inhibitory effect on Ehrlich ascites carcinoma of mice. In mice,the acute LD_(50)levels after intraperitoneal injections of Sb-57 and Sb-71 were found to be 131 and 62 mg/kg respectively;the subacute LD_(50)(10 injections)were equal to 75 and 58 mg/kg respectively.

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...

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.

p-[Bis-(2-chloroethyl)-amino]-phenylalanine (Ⅰ,Sarcolysine, Melphalen) shows pronounced activity against certain tumours. Recently, m-[bis-(2-chloroethyl)-amino]-phenylalanine (Ⅱ) was reported to be more favorable in chemotherapeutic index. β-{p-[Bis-(2-chloroethyl)-amino]-phenyl}-β-amino-propionic acid (Ⅲ) possesses activity against certain tumour cells.In the present investigation, the synthesis of some o-substituted p-[bis-(2-chloroethyl)-amino]-phenylalanine (Ⅳ:Ⅳa,Ⅳb,Ⅳc,Ⅳd andⅣe) from corresponding o-substituted-p-nitrotoluene(Ⅴ)...

p-[Bis-(2-chloroethyl)-amino]-phenylalanine (Ⅰ,Sarcolysine, Melphalen) shows pronounced activity against certain tumours. Recently, m-[bis-(2-chloroethyl)-amino]-phenylalanine (Ⅱ) was reported to be more favorable in chemotherapeutic index. β-{p-[Bis-(2-chloroethyl)-amino]-phenyl}-β-amino-propionic acid (Ⅲ) possesses activity against certain tumour cells.In the present investigation, the synthesis of some o-substituted p-[bis-(2-chloroethyl)-amino]-phenylalanine (Ⅳ:Ⅳa,Ⅳb,Ⅳc,Ⅳd andⅣe) from corresponding o-substituted-p-nitrotoluene(Ⅴ) was described. Compound Ⅴ was brominated with N-bromo-succinimide to give Ⅵ. The latter was condensed with ethyl formamido (or acetamido) malonate, forming ethyl formamido-(or acetamido)-o-substituted p-nitrobenzyl-malonate (Ⅶ). Compound Ⅶ was reduced to the corresponding amino compound Ⅷ by catalytic hydrogenation, the latter was then hydroxy-ethylated with ethylene oxide to give bis-(2-hydroxyethyl)-amino compound Ⅸ, which was converted to Ⅹ on treatment with thionyl chloride or phosphorus oxychloride. Compound Ⅹ was subjected to hydrolysis and decarboxylation in boiling hydrochloric acid to yield Ⅳ.The preparation of two dipeptides, Ⅺ and Ⅻ, has also been described.o-Methoxy-p-[bis-(2-chloroethyl)-amino]-phenylalanine(Ⅳa) exhibited marked inhibition against sarcoma 180, Ehrlich ascites carcinoma, Guerin's carcinoma, etc. The pharmacological examination of the other compounds is in progress.

1.本文叙述自邻位取代-对硝基甲苯(Ⅴ)开始经过六步反应合成了邻位取代-对-[双-(2-氯乙基)-氨基]苯丙氨酸(Ⅳ);取代基是:甲氧基,氟,氯,溴和碘. 2.合成了二肽衍生物:α-甲酰氨基-β-{邻甲氧基-对-[双-(2-氯乙基)-氨基]-苯}丙酰-苯丙氨酸乙酯(Ⅻ)和α-甲酰氨基-β-{邻甲氧基-对-[双-(2-氯乙基)氨基]苯}丙酰-缬氨酸乙酸(Ⅷ). 3.邻甲氧基-对-[双-(2-氯乙基)-氨基]苯丙氨酸(Ⅳa)对肉瘤180、梭形细胞肉瘤、艾氏腹水瘤、Yoshida腹水瘤、Guerin和Walker瘤都有显著的抑制作用.

 
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