Composition of flavonoids and phenolic acids in lychee (Litchi Chinensis Sonn.) Flower extracts and their antioxidant capacities estimated with human LDL, erythrocyte, and blood models.

Lychee (Litchi chinensis Sonn.) flower is a major nectar source in Taiwan. Antioxidant activities of acetone, ethanol, and hot-water extracts of the flower were estimated through three biochemical models: inhibition of Cu(2+) -induced oxidation of human low-density lipoprotein, scavenging ability of oxygen radicals in human blood, and inhibition of human erythrocyte hemolysis induced by peroxyl radicals. Composition and content of flavonoids and phenolic acids in these extracts were also determined by high-performance liquid chromatography. Results showed that antioxidant effects of all test models as well as contents of flavonoids and phenolic acids for the lychee flower extracts were in the order: acetone extract > ethanol extract > hot-water extract. Gentistic acid and epicatechin were the major phenolic acid and flavonoid in the extracts, respectively.

Dietary sodium deprivation evokes activation of brain regional neurons and down-regulation of angiotensin II type 1 receptor and angiotensin-convertion enzyme mRNA expression.

Previous studies have indicated that the renin-angiotensin-aldosterone system (RAAS) is implicated in the induction of sodium appetite in rats and that different dietary sodium intakes influence the mRNA expression of central and peripheral RAAS components. To determine whether dietary sodium deprivation activates regional brain neurons related to sodium appetite, and changes their gene expression of RAAS components of rats, the present study examined the c-Fos expression after chronic exposure to low sodium diet, and determined the relationship between plasma and brain angiotensin I (ANG I), angiotensin II (ANG II) and aldosterone (ALD) levels and the sodium ingestive behavior variations, as well as the effects of prolonged dietary sodium deprivation on ANG II type 1 (AT1) and ANG II type 2 (AT2) receptors and angiotensin-convertion enzyme (ACE) mRNA levels in the involved brain regions using the method of real-time polymerase chain reaction (PCR). Results showed that the Fos immunoreactivity (Fos-ir) expression in forebrain areas such as subfornical organ (SFO), paraventricular hypothalamic nuclei (PVN), supraoptic nucleus (SON) and organum vasculosum laminae terminalis (OVLT) all increased significantly and that the levels of ANG I, ANG II and ALD also increased in plasma and forebrain in rats fed with low sodium diet. In contrast, AT1, ACE mRNA in PVN, SON and OVLT decreased significantly in dietary sodium depleted rats, while AT2 mRNA expression did not change in the examined areas. These results suggest that many brain areas are activated by increased levels of plasma and/or brain ANG II and ALD, which underlies the elevated preference for hypertonic salt solution after prolonged exposure to low sodium diet, and that the regional AT1 and ACE mRNA are down-regulated after dietary sodium deprivation, which may be mediated by increased ANG II in plasma and/or brain tissue.

Effect of Kumhwang-San on anaphylactic reaction in a murine model.

We investigated the effect of Kumhwang-San on anaphylactic reaction. Kumhwang-San dose-dependently inhibited mast cell-mediated systemic anaphylactic reaction induced by compound 48/80. Kumhwang-San significantly inhibited plasma histamine levels induced by compound 48/80. Kumhwang-San dose-dependently inhibited histamine release from the rat peritoneal mast cells activated by compound 48/80 or substance P. The level of cAMP in rat peritoneal mast cells, when Kumhwang-San was added, transiently and significantly increased about 3-fold compared with that of basal cells. These results suggest that Kumhwang-San will be beneficial in the treatment of anaphylactic reaction.

Synthesis and evaluation of water-soluble polyethylene glycol-paclitaxel conjugate as a paclitaxel prodrug.

Water-soluble paclitaxel may cause less side effects and be less costly to administer in comparison to a taxol formulation using a cremophor EL/alcohol vehicle. In this study, polyethylene glycol (PEG; MW 5000) was conjugated to the 2' position of paclitaxel through a spacer succinyl group. PEG-paclitaxel as a non-ionic paclitaxel prodrug was highly water soluble (> 20 mg equiv. paclitaxel/ml). The release of paclitaxel from phosphate-buffered solution was pH dependent. The half-life of PEG-paclitaxel was 7.6, 54 and 311 min at pH 9.0, 7.4 and 6.0, respectively. PEG-paclitaxel inhibited the growth of B16 melanoma cells to an extent similar to that of paclitaxel. In MCA-4 mammary tumor-bearing mice, a single dose of PEG-paclitaxel (40 mg equiv. paclitaxel/kg body weight) significantly delayed tumor growth. The average number of days for the tumor to reach 12 from 8 mm in diameter increased from 6.5 days for control animals to 8.5 days for PEG-paclitaxel-treated animals and 9.4 days for paclitaxel-treated animals. These studies demonstrated that PEG may be used as an effective solubilizing carrier for paclitaxel.

Preparation, characterization, and evaluation of ioxilan carbonate particles for computed tomography contrast enhancement of liver.

RATIONALE AND OBJECTIVES: To prepare and characterize a new particulate contrast medium, cyclic carbonate of ioxilan (IX-C) particles, as a macrophage imaging agent for computed tomography (CT) enhancement of the liver. METHODS: Cyclic carbonate of ioxilan was synthesized from ioxilan, a nonionic water-soluble contrast agent. The IX-C particles prepared by a solvent extraction-evaporation method were characterized by size distribution, degradability, suspension stability, and median lethal dose. Pharmacokinetics of IX-C particles and their effectiveness in enhancing liver attenuation and in detecting hepatic tumors were evaluated using normal and VX2-tumor-bearing rabbits. RESULTS: The IX-C particles were biodegradable, with ioxilan and carbon dioxide as the degradation products. The particles had an average size of 1 to 2 microns and were stable in saline suspension. The median lethal dose determined for IX-C particles was 2.6 and 3.1 g/kg body weight for female and male rabbits, respectively. A dose of 200 mg iodine/kg body weight caused an increase of 38 Hounsfield units in liver attenuation. In rabbit, hepatic clearance of the contrast medium occurred in 2 days. A tumor barely visible in precontrast scans could be detected after contrast injection. CONCLUSIONS: Development of particulate contrast medium from nonionic contrast agents represents a new approach. Ioxilan carbonate particles have suitable physicochemical properties that warrant further studies before clinical evaluation.

[Studies on the sweet principles from the leaves of Cyclocarya paliurus (Batal.) Iljinskaya].

Four intensely sweet compounds (I-IV) were obtained from the leaves of Cyclocarya paliurus (Batal.) Iljinskaya. The structure of compound I was elucidated by chemical and spectroscopic methods as 20,24-epoxy-dammarane-(3 beta,12 beta,24R)-12-O-alpha-L-rhamnopyranosyl-25- hydroxyl-3-O-alpha-(5'-O-acetyl)-L-arabinofuranoside. It is a new natural product, named cyclocarioside A, and is the main sweet principle of this plant, possessing about 200 times the sweetness intensity of sugar.

[Tinnitus treated with combined traditional Chinese medicine and Western medicine].

Cases of annoying tinnitus were selected for this observation. They were examined by general physical examination, otoscopy and some of them by audiometry and tinnitus masking patterns test, and/or Ecoch G and BSER. Two groups, TCM-WM and controls, were designed with patient's sexes, ages, severity of tinnitus almost evenly distributed. Different kinds of medicines were given to the patients of 2 groups with single blind trial. For the controls, only western medicines such as valium, nicotinic acid, mixture bromides, vitamin B Co, ATP and carbamazepine (if 100 mg of lidocaine added to 50% glucose solution intravenously was effective) were taken orally. For TCM-WM group patients, besides the drugs used above, herbal decoctions were given twice a day, and observed for 5 days per therapeutic course. The medicinal herbs consist of: Rhizoma Gastrodiae, Ramulus Uncariae cum Uncis, Poria cocos, Flos Chrysanthemi, Akebia quinata, Radix Polygoni Multiflori, Fructus Liquidambris, Radix Rehmanniae, Rhizoma Alismatis, Radix Scrophulariae, Fructus Lycii, Radix Glycyrrhizae, Semen Plantaginis and Semen Vaccariae. Of the therapeutic results in 32 cases of TCM-WM group, 11 cases (34.4%) showed absence of tinnitus, 16 (50%) improved, and 5 (15.6%) failed. The total effective rate was 84.4%. In 27 cases of the controls, 5 cases (18.6%) showed absence of tinnitus, 10 (37%) improved, and 12 (44.4%) failed. The total effective rate was 55.6%. It showed that the therapeutic results of TCM-WM group was better than those of the controls (P less than 0.05).