Reversed siderophores act as antimalarial agents.

We describe here a family of biomimetic iron carriers that display high binding efficiency for ferric ions and favorable permeation properties across erythrocytic membranes. These carriers inhibit in vitro growth of Plasmodium falciparum by scavenging intracellular iron. The chemical features were realized by reproducing the iron-binding cavities of natural iron carriers (siderophores) and by systematic substitutions of their hydrophilic envelopes for more hydrophobic ones. In contrast to natural carriers, which participate in receptor-mediated iron uptake in cells and act as growth promoters, our synthetic carriers were designed to penetrate cellular membranes by diffusion, scavenge intracellular iron, and thereby act as growth inhibitors. Based on these properties we designate the compounds reversed siderophores and refer to the specific analogs of the natural ferrichrome as synthetic ferrichromes. The antimalarial activity of the synthetic ferrichromes correlated with their lipophilicity, and this antimalarial activity was averted when the chelators were applied as iron (III) complexes. The sites of synthetic ferrichrome action reside in the intraerythrocytic parasite and not in serum or on normal erythrocyte components. The agents were effective against all stages of parasite growth and against a variety of multidrug-resistant strains of P. falciparum. The most potent agent of this synthetic ferrichrome series, SF1-ileu, was not toxic to mammalian cells in culture and was 15-fold more potent and 20-fold faster acting than desferrioxamine. Taken in toto, these agents constitute a series of promising candidates for future use in malaria chemotherapy.     

一些保肝药物对原代培养大鼠肝细胞糖原合成功能的影响

本文参照PO Seglen的方法并加以修改,建立了原代培养大鼠肝细胞糖原合成功能的测定体系。观察到联苯双酯既能使正常肝细胞合成糖原增加88%,又能保护肝细胞完全拮抗四氯化碳对其功能的损伤;银耳多糖能使四氯化碳对肝细胞糖原合成功能的损伤减轻57%;去甲斑蝥素10μg/ml能增加肝细胞糖原合成,浓度增加到100μg/ml时,此作用减弱,1000μg/ml则明显抑制糖原的合成,而且在10～100μg/ml浓度时,即能加强四氯化碳的损伤作用;100μg/ml CL₁₅₀₀和熊果酸二钠单独应用可增加肝细胞糖原合成,但与四氯化碳同时应用,反而加重对糖原合成的抑制作用。     

Early ocular hypertension after cataract extraction

The intraocular pressure (IOP) course during the first postoperative month was measured with Goldmann applanation tonometry in 93 eyes. The patients include 30 eyes of intracapsular cataract extraction (ICCE), 32 eyes of extracapsular cataract extraction (ECCE) and 31 eyes of ECCE combined with posterior chamber intraocular lens (PC-IOL) implantation. The preoperative average IOP was 13.30 +/- 3.24 mmHg in 93 eyes. The first day after cataract extraction was 25.33 +/- 8.18 mmHg and 59 eyes (63.44%) had an IOP higher than 23 mmHg. On the second day it was 16.03 +/- 7.54 mmHg. On the third day it was 14.69 +/- 5.45 mmHg. On the seventh day it was 13.32 +/- 3.44 mmHg and only 2 eyes (2.14%) IOP was higher than 23 mmHg. The first postoperative month average IOP was 12.93 +/- 1.31 mmHg and it was above 23 mmHg in only one eye. When compared with preoperation a significant increase in IOP was found postoperatively. But on the seventh day and after the first month there was no significant difference (P greater than 0.05). The IOP rise among ICCE group, ECCE group and PC-IOL group did not differ significantly.     

肝内HBcAg与血清学指标的关系及慢性乙型肝炎发病机理的探讨

We detected the presence and distribution of HBcAg in the liver by immunohistochemistry (ABC method) and the presence of HBV-DNA in serum (spot hybridization) and anti-HBe in serum (ELISA) from 59 cases of hepatitis B hospitalized in our hospital, including 47 cases of CAH, 5 cases of CPH, and 7 cases of subacute fulminant hepatitis. 1. HBcAg in the liver was detected in 25 out of 47 cases (53%) of CAH, in 2 out of 5 cases of CPH and in 4 out of 7 cases of subacute fulminant hepatitis. The total percentage was 53% (31/59). 2. There was no positive correlation between HBV replication activity and liver disease activity (P greater than 0.05). Our results did not support the hypothesis that suggests a direct cytopathic effect of HBV. Oppositely, the fact was that the presence, the amount and the patterns of HBcAg in the liver, and the presence of HBV-DNA in serum were predominant in mild CAH compared with those in severe CAH, predominant in CAH without cirrhosis compared with those in CAH with cirrhosis. There was a tendency of inverse correlation between HBV replication activity and liver disease activity. The results above were in line with the concept that HBcAg expressed on the surface of infected hepatocytes may be relevant target for T lymphocyte cytotoxicity. The results have suggested that an immune response to HBV is present, leading to the destruction of most infected cells. 3. There was a positive correlation between HBV-DNA in serum and HBcAg in the liver (P less than 0.005), indicating that HBV-DNA in serum can represent HBV replication.(ABSTRACT TRUNCATED AT 250 WORDS)