[Preparation and qualitative control of compound Dyclonine's suspending mixture].

The paper deals with the composition, preparation and qualitative control of compound Dyclonine's suspending mixture, one of gastroscopic mucomembranous anesthetics. The content of Dyclonine hydrochloride was detected by ultraviolet spectrophotometry. It shows that the average rate of recovery is 100.80%, RSD = 1.32%(n = 6). At room temperature, the appearance and content of the preparation are not changed in 0, 30, 180, 365 days respectively. The preparation is widely and successfully used in clinics with easy procedure and excellent stability.

Hypocholesterolemic effects of mixture Da Huai on experimental rats and treatment of a homozygous FH child.

This study observes the hypocholesterolemic effects of Mixture Da Huai--a drug of enhancing monocyte macrophage system--on experimental rats, and the treatment of a homozygous familial hypercholesterolemia (FH) child. The results show that TC, VLDL-C and LDL-C in Mixture Da Huai group were significantly reduced and HDL-C was significantly increased. Fractional clearance rates for 125I-GLC-LDL, and the 125I-GLD-LDL uptake of rat peritoneal macrophages were significantly increased. Excretions of total sterol and acidic sterol in feces were also increased. After treatment for 3 months, serum TC and LDL-C of a homozygous FH child were significantly decreased. Tendon and cutaneous xanthomas were limited. This study indicates that by promoting the monocyte macrophage system to degrade LDL, a promising prevention and treatment of hypercholesterolemia and atherosclerosis might be provided, especially in the treatment of homozygous FH.

Familial hypercholesterolemia in China. Identification of mutations in the LDL-receptor gene that result in a receptor-negative phenotype.

Familial hypercholesterolemia (FH), caused by many different mutations in the low-density lipoprotein (LDL)-receptor gene, invariably leads to severe premature coronary heart disease (CHD) in homozygous individuals. Heterozygous FH patients are less severely affected but are still at increased risk of CHD in most populations. Although FH homozygotes in China are affected similarly to those elsewhere, heterozygotes are not detected in the general population and obligate heterozygotes are often not hypercholesterolemic by Western standards. Mutations in the LDL-receptor genes of 10 homozygous FH patients from the Jiang-su province of China and their heterozygous parents were analyzed. These include one large and two minor deletions and eight point mutations: four are predicted to introduce a premature stop codon, five to result in a single amino acid substitution or deletion, and one to produce a protein with an abnormal cytoplasmic tail. Expression of the mutant LDL-receptor cDNAs in vitro confirmed that these mutations impaired LDL-receptor function and that several would cause a receptor-negative phenotype. Thus, the lack of clinical expression in obligate FH heterozygotes is not due to unusually "mild" mutations in the LDL-receptor gene, and other genetic or environmental factors must therefore be important in determining phenotypic expression.

Effects of monocyte macrophages stimulation on hepatic lipoprotein receptors.

The first series of in vivo experiments were designed to investigate the effects of monocytic macrophages (MM phi) stimulation by zymosan in cholesterol-fed rats. We found that the MM phi stimulation significantly decreased plasma very-low-density lipoprotein-cholesterol, low-density lipoprotein-cholesterol but not high-density lipoprotein-cholesterol. The hepatic and aortic cholesterol levels were also significantly decreased; meanwhile, the biliary total bile acid and fecal sterol excretion were significantly enhanced. These results were beneficial to the prevention and regression of atherosclerosis. The second series of in vitro experiments led to the discovery that zymosan did not have effect on HDL and LDL binding, uptake and degradation of hepatic parenchymal and nonparenchymal cells isolated from normal rats, but did have significant effects on those isolated from cholesterol-fed rats. The experiments of Kupffer cells modulating hepatocytes also demonstrated that hepatocyte HDL receptor activity was significantly enhanced by conditioned medium from acetylated LDL plus zymosan added to Kupffer cells. Bmax of 125I-labeled HDL specific binding was increased from 237.8 to 295.2 ng/mg cell protein. The Ka value was not affected, indicating that there might be an increment in receptor number, but not receptor affinity. Cholesterol-loaded zymosan-stimulated Kupffer cells might secrete a soluble mediator affecting hepatocyte HDL receptor activity. Zymosan and other MM phi-stimulating reagents are promising in the exploration of a new approach for prevention and treatment of hypercholesterolemia and atherosclerosis.

Homozygous familial hypercholesterolemic patients in China.

Five homozygous patients with familial hypercholesterolemia (FH) are described. Their serum cholesterol levels were between 603 and 907 mg/dl, with an average of 714 mg/dl. The mean value of serum cholesterol levels of the obligate heterozygous parents was 270 mg/dl. In the patient group, 87% of the serum cholesterol was distributed in low density lipoprotein (LDL) and the mean LDL cholesterol level was about 8.4 times that in a control group. Phospholipids in HDL in the patient group were significantly lower than in the controls. Lipid assays of xanthoma tissues revealed that the major lipid was cholesterol and its esters. LDL receptor activity in fibroblasts from the homozygotes was markedly decreased. Two patients yielded less than 2% of normal receptor activity and were classified as receptor-negative. The other 3 revealed receptor activities greater than 2% but less than 25% of normal receptor activity and were classified as receptor-defective.

Serum high density lipoprotein cholesterol levels in Chinese healthy subjects and patients with certain diseases.

Serum high density lipoprotein cholesterol (HDL-C), total cholesterol (TC) and triglycerides (TG) were determined, and values of low density lipoprotein cholesterol (LDL-C), HDL-C/TC (%), and the LDL-C/HDL-C (ratio) were calculated in 1101 healthy Chinese men and women, 77 patients with coronary heart disease (CHD), 70 patients with cerebral vascular disease (CVD), 64 patients with diabetes mellitus (DM), 40 bilaterally oophorectomized women and 95 women using oral contraceptives. Serum HDL-C levels seemed higher and LDL-C levels lower in the healthy Chinese population as compared with those previously reported from European and American whites. Serum HDL-C was significantly higher in fertile females than in males of comparable ages. We failed to demonstrate any sharp fall in HDL-C after the menopause or bilateral oophorectomy. Serum HDL-C levels were significantly lower in both CHD and CVD patients than in healthy subjects of comparable sex and age. Concomitant increases in serum TC, LDL-C and TG, however, were found in CHD patients but not in CVD patients. No abnormality in the mean serum HDL-C level was found in DM patients. However, those complicated with CHD had significantly lower HDL-C than those without CHD. A striking serum HDL-C lowering effect was found with some kinds of oral contraceptives.

PIP: Serum high density lipoprotein cholesterol (HDL-C), total cholesterol (TC), and triglycerides (TG) were determined, and values of low density lipoprotein cholesterol (LDL-C), HDL-C/TC (%), and the LDL-C/HDL-C (ratio) were calculated in 1101 healthy Chinese men and women, 77 patients with coronary heart disease (CHD), 70 with cerebral vascular disease (CVD), 64 patients with diabetes mellitus (DM), 40 bilaterally oophorectomized women, and 95 women using oral contraceptives (OCs). Serum HDL-C levels seemed higher and LDL-C levels lower in the healthy Chinese population as compared with those previously reported from European and American whites. Serum HDL-C was significantly higher in fertile females than in males of comparable ages. The authors failed to demostrate any sharp fall in HDL-C after the menopause or bilateral oophorectomy. Serum HDL-C levels were significantly lower in both CHD and CVD patients than in healthy subjects of comparable sex and age. Concomitant increases in serum TC, LDL-C, and TG, however, were found in CHD patients but not in CVD patients. No abnormality in mean serum HDL-C level was found in DM patients. However, those complicated with CHD had significantly lower HDL-C than those without CHD. A striking serum HDL-C lowering effect was found with some kinds of OCs.