Sp) Octyl 8 chloroadenosine 3′5′cyclophosphate (OCC), a newly synthesized 8 Cl c AMP derivative, strongly induced inhibition and differentiation in human leukemia HL 60 cells. In flow cytometry, OCC brought a...Sp) Octyl 8 chloroadenosine 3′5′cyclophosphate (OCC), a newly synthesized 8 Cl c AMP derivative, strongly induced inhibition and differentiation in human leukemia HL 60 cells. In flow cytometry, OCC brought about a block at the G1 phase of HL 60 cell cycle. OCC inhibited strongly the synthesis of DNA without affecting the synthesis of RNA and protein in HL 60 cells and also activated the c AMP dependent protein kinase in the cytosol of HL 60 cells. 8 Chloroadenosine is the active metabolite of OCC and inhibited significantly the growth of tumour in vitro and in vivo tests. 8 Chloroadenosine can induce differentiation of gastric mucoid adenocarcinoma cell line MGc80 3 and induce apoptosis in the MOLT 4 cells. The mechanism of the antitumour effects of 8 chloroadenosine was discussed.展开更多
Chitosans reacted with selenious acid to prepare chitosan hydrogen selenites, which were found to be growth-inhibitory against sarcoma 180 solid tumor. The results indicated that the activity also depended on the mol...Chitosans reacted with selenious acid to prepare chitosan hydrogen selenites, which were found to be growth-inhibitory against sarcoma 180 solid tumor. The results indicated that the activity also depended on the molecular weight of chitosan supports.展开更多
Carboxymethylpachyman(Ⅰ)was formed by carboxymethylation of β-pachyman.The antitumour activity of carboxymethylpachyman(Ⅰ)against S_(180)、EAC、 MA、U_(14)was measured.The structure of carboxymethylpachyman(Ⅰ)was ...Carboxymethylpachyman(Ⅰ)was formed by carboxymethylation of β-pachyman.The antitumour activity of carboxymethylpachyman(Ⅰ)against S_(180)、EAC、 MA、U_(14)was measured.The structure of carboxymethylpachyman(Ⅰ)was proved by IR ^(13)CNMR spectroscopy.展开更多
The effect of enterotoxins is to induce the production of endogenous IF. St. aureus enteropathogenic proteins (enterotoxins) possess an antitumour effect. After intraperitoneal inoculation, they decrease the size and,...The effect of enterotoxins is to induce the production of endogenous IF. St. aureus enteropathogenic proteins (enterotoxins) possess an antitumour effect. After intraperitoneal inoculation, they decrease the size and, in some cases, prevent the development of the human hypernephroma in the cheek pouch of golden hamsters. The effect of enteropathgenic proteims may possibly consist in inducing the production of endogenous immune interferon which activates the host immune system and enhances the rejection of heterologous tumour cells.展开更多
Fourteen new di n butyltin(IV) complexes of hydroxamic acids of the formula Bu 2 SnL 2 (HL=hydroxamic acids) were synthesized by the reaction of Bu 2 SnO and hydroxamic acids in dry toluene and ...Fourteen new di n butyltin(IV) complexes of hydroxamic acids of the formula Bu 2 SnL 2 (HL=hydroxamic acids) were synthesized by the reaction of Bu 2 SnO and hydroxamic acids in dry toluene and ethanol media. The compounds were characterized by elemental analyses, molecular weight, IR and 1 H NMR spectroscopy. The results indicate that n Bu 2 SnL 2 have distorted trans octahedral structure. The antitumor activity in vitro against human A 549 tumor cells and P388 leukemia was presented, and their structure activity relationship was discussed.展开更多
Based on the consistency of the in vivo and in vitro interactions of drugs with DNA, a fluorimetric method has been developed as a new in vitro method for preliminary screening of antitumour agents. This method was te...Based on the consistency of the in vivo and in vitro interactions of drugs with DNA, a fluorimetric method has been developed as a new in vitro method for preliminary screening of antitumour agents. This method was tested using Schiff bases synthesized from salicylaldehyde with 1-alanine, 1-asparagine and 1-histidine, and complexes of these Schiff bases with Cu(Ⅱ), Zn(Ⅱ), Ni(Ⅱ) and Sn(Ⅳ) as potential antitumour agents.The study of the interaction of the complexes with DNA by a fluorescence probe ethidium bromide (EthBr)-DNA system indicated the parallelism between the binding constants and antineoplastic ratios. The relationship between structure and antitumonr activity was investigated.展开更多
Oncrasin-1类衍生物对来自肺癌、结肠癌等多种癌细胞系都具有高度活性,其中NSC-743380活性最佳。然而,它在结构上存在问题,易形成二聚体而失活,限制了进一步的研究发展。因此,本文以Oncrasin-1为先导化合物,设计了13种衍生物,通过引入...Oncrasin-1类衍生物对来自肺癌、结肠癌等多种癌细胞系都具有高度活性,其中NSC-743380活性最佳。然而,它在结构上存在问题,易形成二聚体而失活,限制了进一步的研究发展。因此,本文以Oncrasin-1为先导化合物,设计了13种衍生物,通过引入氨基和酰胺基,尝试提高化合物稳定性并保留活性。化合物结构经1 H NMR,13 C NMR,HR-MS(ESI)表征,并通过细胞增殖实验(CCK-8实验)测定其对人胰腺癌细胞(PANC-1)、人宫颈癌细胞(HeLa)和人肝癌细胞(HepG2)的抗肿瘤活性。结果表明,13个Oncrasin-1类衍生物中,有10个表现出更好的活性,其中化合物4((4-(((1-(4-氯苄基)-1 H-吲哚-3-基)甲基)氨基)丁基)氨基甲酸叔丁酯)对HeLa的IC 50达到了3.98μM。展开更多
文摘Sp) Octyl 8 chloroadenosine 3′5′cyclophosphate (OCC), a newly synthesized 8 Cl c AMP derivative, strongly induced inhibition and differentiation in human leukemia HL 60 cells. In flow cytometry, OCC brought about a block at the G1 phase of HL 60 cell cycle. OCC inhibited strongly the synthesis of DNA without affecting the synthesis of RNA and protein in HL 60 cells and also activated the c AMP dependent protein kinase in the cytosol of HL 60 cells. 8 Chloroadenosine is the active metabolite of OCC and inhibited significantly the growth of tumour in vitro and in vivo tests. 8 Chloroadenosine can induce differentiation of gastric mucoid adenocarcinoma cell line MGc80 3 and induce apoptosis in the MOLT 4 cells. The mechanism of the antitumour effects of 8 chloroadenosine was discussed.
基金This work was supported by the National Natural Science Foundation of China (grant No. 29977014) and China Capital Investment, Ltd., in Shanghai.
文摘Chitosans reacted with selenious acid to prepare chitosan hydrogen selenites, which were found to be growth-inhibitory against sarcoma 180 solid tumor. The results indicated that the activity also depended on the molecular weight of chitosan supports.
文摘Carboxymethylpachyman(Ⅰ)was formed by carboxymethylation of β-pachyman.The antitumour activity of carboxymethylpachyman(Ⅰ)against S_(180)、EAC、 MA、U_(14)was measured.The structure of carboxymethylpachyman(Ⅰ)was proved by IR ^(13)CNMR spectroscopy.
文摘The effect of enterotoxins is to induce the production of endogenous IF. St. aureus enteropathogenic proteins (enterotoxins) possess an antitumour effect. After intraperitoneal inoculation, they decrease the size and, in some cases, prevent the development of the human hypernephroma in the cheek pouch of golden hamsters. The effect of enteropathgenic proteims may possibly consist in inducing the production of endogenous immune interferon which activates the host immune system and enhances the rejection of heterologous tumour cells.
基金ProjectsupportedbytheNationalNaturalScienceFoundationofChina (No .2 97710 2 3)andtheNaturalScienceFoundationofShanxiProvince
文摘Fourteen new di n butyltin(IV) complexes of hydroxamic acids of the formula Bu 2 SnL 2 (HL=hydroxamic acids) were synthesized by the reaction of Bu 2 SnO and hydroxamic acids in dry toluene and ethanol media. The compounds were characterized by elemental analyses, molecular weight, IR and 1 H NMR spectroscopy. The results indicate that n Bu 2 SnL 2 have distorted trans octahedral structure. The antitumor activity in vitro against human A 549 tumor cells and P388 leukemia was presented, and their structure activity relationship was discussed.
基金Project supported by the State Education Commission Foundationthe National Natural Science Foundation of China.
文摘Based on the consistency of the in vivo and in vitro interactions of drugs with DNA, a fluorimetric method has been developed as a new in vitro method for preliminary screening of antitumour agents. This method was tested using Schiff bases synthesized from salicylaldehyde with 1-alanine, 1-asparagine and 1-histidine, and complexes of these Schiff bases with Cu(Ⅱ), Zn(Ⅱ), Ni(Ⅱ) and Sn(Ⅳ) as potential antitumour agents.The study of the interaction of the complexes with DNA by a fluorescence probe ethidium bromide (EthBr)-DNA system indicated the parallelism between the binding constants and antineoplastic ratios. The relationship between structure and antitumonr activity was investigated.
文摘Oncrasin-1类衍生物对来自肺癌、结肠癌等多种癌细胞系都具有高度活性,其中NSC-743380活性最佳。然而,它在结构上存在问题,易形成二聚体而失活,限制了进一步的研究发展。因此,本文以Oncrasin-1为先导化合物,设计了13种衍生物,通过引入氨基和酰胺基,尝试提高化合物稳定性并保留活性。化合物结构经1 H NMR,13 C NMR,HR-MS(ESI)表征,并通过细胞增殖实验(CCK-8实验)测定其对人胰腺癌细胞(PANC-1)、人宫颈癌细胞(HeLa)和人肝癌细胞(HepG2)的抗肿瘤活性。结果表明,13个Oncrasin-1类衍生物中,有10个表现出更好的活性,其中化合物4((4-(((1-(4-氯苄基)-1 H-吲哚-3-基)甲基)氨基)丁基)氨基甲酸叔丁酯)对HeLa的IC 50达到了3.98μM。
