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Biomedical subjects

C F Chen

Publications and source records attributed to C F Chen.

At least 199 records · Page 11Linked to original sources

Aspirin inhibits collagen-induced platelet serotonin release, as measured by microbore high-performance liquid chromatography with electrochemical detection.

A sensitive microbore high-performance liquid chromatographic method with electrochemical detection has been developed for the measurement of small quantities of serotonin (5-hydroxytryptamine; 5-HT) and its metabolite 5-hydroxyindoleacetic acid (5-HIAA) in rabbit platelets. The limit of detection of 5-HT is 0.1 ng/ml. To evaluate the 5-HT release from platelet suspension, the aggregating agent collagen was added at concentrations of 10, 30 and 100 micrograms/ml and the 5-HT concentrations rose from the base level (11.80 +/- 0.42 ng/ml) to 123.97 +/- 11.02, 361.96 +/- 17.90 and 470.45 +/- 35.46 ng/ml, respectively. Further results demonstrated that aspirin inhibits collagen-induced 5-HT release from platelet suspension significantly.

Animals↗

High-performance liquid chromatographic determination of evodiamine in rat plasma: application to pharmacokinetic studies.

A previously published simple and sensitive high-performance liquid chromatographic method for determination and identification of rutaecarpine in rat plasma was used for evodiamine determination. However, the ultraviolet detection was not 344 nm, but 227 nm. The method was applied to a pharmacokinetic study of evodiamine in rats after 2 mg/kg intravenous administration. A biphasic phenomenon with a rapid distribution followed by a slower elimination phase was observed from the plasma concentration-time curve. Compartmental analysis yielded a two-compartment model.

Animals↗

Modulatory effects of magnolol on potassium-stimulated 5-hydroxytryptamine release from rat cortical and hippocampal slices.

Magnolol, a phenolic constituent of magnolia bark, is a known central nervous system depressant. To examine the possibility that magnolol may elicit its depressant effect by modulating central serotonergic activity, its effect on 35 mM K(+)-stimulated 5-[3H]HT release from rat hippocampal and frontal cortical slices were examined. Inclusion of magnolol (1-100 microM) had no effect on 5-HT release in hippocampal slices but elicited a dose-related inhibition on 5-HT release from cortical slices. The inhibitory effect of magnolol on K(+)-stimulated 5-HT release from the cortex was not affected by either antagonists (metergoline, propranolol, and cyproheptadine) (0.01-10 microM) of various 5-HT receptor subtypes or the voltage-dependent sodium channel blocker tetrodotoxin (1 microM). It is concluded that the suppression of brain 5-HT release by magnolol is site-specific, and the suppression of cortical 5-HT release by magnolol is not via the 5-HT autoreceptors at the 5-HT terminals.

Animals↗

Concentration and regional distribution of propofol in brain and spinal cord during propofol anesthesia in the rat.

We evaluated the pharmacokinetics and regional distribution of propofol in the brain and spinal cord during propofol anesthesia in Sprague-Dawley rats, using high-performance liquid chromatographic determination of propofol concentration in brain, whole blood and plasma. We found that the concentration of propofol in the brain increased and decreased expeditiously during and after a 15-min and 30-min period of i.v. infusion of an anesthetic dose (60 mg/kg per h) of propofol. Furthermore, propofol was evenly distributed in the brain and spinal cord during infusion, with a significant inter-individual variation. Upon the establishment of anesthesia 15 and 30 min following intravenous infusion of propofol, the concentration of propofol in the brain, whole blood and plasma was respectively 15.7 +/- 1.9 and 39.4 +/- 2.7 micrograms/g, 4.5 +/- 1.2 and 13.6 +/- 1.3 micrograms/ml and 1.8 +/- 0.5 and 5.1 +/- 0.9 micrograms/ml (mean +/- SEM, n = 6 or 7). These high brain/blood and brain/plasma ratios during anesthesia suggest that propofol manifests a pharmacokinetic profile that is different from at least thiopental.

Anesthesia↗

Cytotoxicity and antimicrobial activity of some naphthol derivatives.

2-Hydroxymethyl-1-naphthol diacetate (TAC) and sixteen Mannich base derivatives of naphthol were prepared and examined for cytotoxicity and antimicrobial activity. Cytotoxicity was examined against four human carcinoma cell lines. Several derivatives were effective at concentrations < 4 micrograms/ml. TAC showed the highest cytotoxicity. Inhibition of DNA-, RNA-, and protein synthesis by TAC was also studied and discussed. TAC also exhibits potent antimicrobial activity against Enterobacter clocae 23355, Klebsiella pneumonia 13883, Proteus vulgaris 13315, Pseudomonas aeruginosa 27853, Candida parapsilosis, Candida tropicalis, Trichosposon beigelli, and Rhodotorul spp. with minimum inhibitory concentrations of 0.1-0.4 microM. These results indicate that esterification by Bruson reaction of 1-naphthol Mannich base to TAC enhances the cytotoxicity and antimicrobial activity.

Anti-Bacterial Agents↗

Power spectral analysis of electroencephalographic desynchronization induced by cocaine in rats: correlation with evaluation of noradrenergic neurotransmission at the medial prefrontal cortex.

We applied continuous, on-line and real-time spectral analysis of electroencephalographic (EEG) signals and microdialysis to evaluate the possible participation of noradrenergic neurotransmission at the medial prefrontal cortex (mPFC) in EEG desynchronization induced by cocaine. Male Sprague-Dawley rats that were under chloral hydrate anesthesia were used. Intravenous administration of cocaine (1.5 or 3.0 mg/kg) dose-dependently induced EEG desynchronization, as represented by a decrease in root mean square (RMS) and an increase in mean power frequency (MPF) value of the EEG signals. Power spectral analysis further revealed that whereas both doses of cocaine promoted a reduction in the alpha (8-13 Hz), theta (4-8 Hz), and delta (1-4 Hz) components, the lower dose of cocaine decreased, and the higher dose increased the beta band (13-32 Hz). Microdialysis data indicated an elevation in extracellular concentration of norepinephrine at the mPFC that paralleled temporally and correlated positively with the maximal effect of cocaine on EEG activity. Bilateral microinjection of the selective noradrenergic neurotoxin, DSP4 (50 micrograms), or equimolar concentration (500 pmol) of the alpha 1-adrenoceptor antagonist, prazosin, or alpha 2-adrenoceptor antagonist, yohimbine, into the mPFC significantly blunted the decrease in delta component (prazosin) or both delta and theta components (DSP4 or yohimbine) of EEG activity by the lower dose of cocaine. On the other hand, the same pretreatments appreciably antagonized the increase in beta band by cocaine at 3.0 mg/kg. The potency of the antagonism by yohimbine, however, was higher than prazosin. These results suggest that cocaine may elicit EEG desynchronization via noradrenergic neurotransmission, and that alpha 2-adrenoceptors, and to a lesser extent, alpha 1-adrenoceptors, at the mPFC may be involved in the subtle dose-dependent changes in individual EEG spectral components.

Adrenergic Agents↗

Fructus aurantii reduced portal pressure in portal hypertensive rats.

The purpose of this study was to investigate the effects of Fructus Aurantii (the unripe fruits of Citrus aurantium L.) on portal hypertensive rats. Portal hypertension was induced by partial portal vein ligation (PVL) in Sprague-Dawley rats. Sham-operated (Sham) rats served as controls. Hemodynamic and in vitro contractile studies were performed at 14 days after surgery. Both the aqueous extract of Fructus Aurantii and synephrine, one of its purified principles with pressor activity, were infused into the conscious PVL and Sham rats via a syringe pump. Fructus Aurantii (1.25, 2.5, & 5.0 mg/kg/min) dose-dependently reduced portal pressure in PVL and Sham rats, with the percentage change in portal pressure more pronounced in PVL rats. Mean arterial pressure was dose-dependently elevated by Fructus Aurantii. Synephrine (0.095, 0.19, & 0.38 mg/kg/min) also dose-dependently reduced portal pressure and elevated mean arterial pressure in PVL and Sham rats. Fructus Aurantii (2.8-280 micrograms/ml) induced dose-dependent contractile responses mainly in aorta and mesenteric artery, but little response in portal vein. The results showed that Fructus Aurantii infusion reduced portal pressure, possibly by way of arterial vasoconstriction.

Animals↗

Constituents and cytotoxic principles of Nothapodytes foetida.

A new naturally occurring alkaloid, acetylcamptothecin, together with 17 known compounds, (+)-1-hydroxypinoresinol, omega-hydroxypropioguaiacone, p-hydroxybenzaldehyde, scopoletin, uracil, thymine, sitosterol, sitosteryl-beta-D-glucoside, 3 beta-hydroxy-stigmast-5-en-7-one, stigmast-5-en-3 beta,7 alpha-diol, 6 beta-hydroxystigmast-4-en-3-one, sitost-4-en-3-one, linoleic acid, trigonelline, camptothecin, 9-O-methoxycamptothecin and pumiloside were isolated and characterized from the stem of Nothapodytes foetida. Among them, scopoletin, camptothecin, 9-O-methoxycamptothecin and O-acetylcamptothecin showed significant cytotoxic activity.

Antineoplastic Agents, Phytogenic↗

Capsaicin pretreatment attenuates chronic hypoxic pulmonary hypertension.

Capsaicin pretreatment was used to deplete tachykinins in order to study the role of tachykinins in chronic hypoxia-induced pulmonary hypertension. Forty three young Wistar rats weighing 235 +/- 4 g were randomly divided into four groups: control (n = 10); capsaicin pretreatment (n = 10); intermittent chronic hypoxia (n = 10); and capsaicin pretreatment + intermittent chronic hypoxia (n = 13). Control animals breathed room air. Rats in the capsaicin pretreatment groups were given capsaicin via subcutaneous injection over a three-day period. Hypobaric hypoxia was intermittently applied by placing animals into a hypobaric chamber with a barometric pressure of 380 Torr for two weeks. In the capsaicin pretreatment + intermittent chronic hypoxia group, rats were exposed to intermittent hypoxia for two weeks immediately after the last dose of capsaicin. Subsequently, pulmonary vascular function, as well as substance P (a tachykinin) level and neutral endopeptidase (NEP, the major degradation enzyme for tachykinins) activity in the lungs were measured. Chronic hypoxia caused significant increases in pulmonary artery pressure, right ventricle/(left ventricle + septum) weight ratio, hematocrit, and lung substance P level, as well as a significant decrease in lung NEP activity. All these chronic hypoxia-induced changes were significantly lessened by capsaicin pretreatment. Capsaicin pretreatment alone did not induce any significant alteration in vascular function. These results suggest that the chronic hypoxia causes an increase in lung tachykinin levels which, in turn, enhance the development of pulmonary hypertension.

Animals↗

Thermoregulatory effects of alkaloids isolated from Wu-chu-yu in afebrile and febrile rats.

Dehydroevodiamine (DeHE) and evodiamine (EVO), alkaloids isolated from a Chinese medicinal herb, Wu-chu-yu, exhibit calcium antagonistic activity. Intraperitoneal injections of DeHE (5-20 mg/kg) and EVO (2.5-10 mg/kg) caused a dose-related hypothermia in afebrile rats at an ambient temperature (Ta) of 20 degrees C. Because the heat production of alkaloid-injected rats did not differ from that of the controls, the hypothermic effect likely resulted from increased peripheral heat loss. This suggestion is supported by the finding that both DeHE and EVO did not affect the thermoregulatory response of rats exposed to a Ta of 35 degrees C, at which heat loss was maximized. Injection of the same doses of DeHE and EVO attenuated the febrile response in a dose-related manner, induced by intrahypothalamic injection of exogenous pyrogen. The attenuation of the febrile response was associated with a reduction in heat production. Because DeHE and EVO did not affect HP in afebrile rats at a Ta of either 20 or 35 degrees C, but suppressed the metabolic rate of febrile rats at 20 degrees C, the thermoregulatory effect of DeHE and EVO could involve both a calcium-dependent increase in heat loss and a suppression in heat production; the latter may only be manifested when the set point for thermoregulation is elevated.

Alkaloids↗

Interleukin-1 receptor antagonist attenuates the heat stroke-induced neuronal damage by reducing the cerebral ischemia in rats.

The effects of interleukin-1 receptor antagonist (IL-Ira) on both local cerebral blood flow and neuronal damage of the hypothalamus, corpus striatum, cortex or thalamus were assessed in rats with heat stroke. Heat stroke was induced by exposing the urethane-anesthetized rats to a high ambient temperature (42 degrees C). Damage to the hypothalamus, corpus striatum, cortex or thalamus was scored on a scale of zero to three modified from the grading system of Pulsinelli and colleagues in which: 0 = normal, 1 = few neurons damaged, 2 = many neurons damaged, and 3 = all neurons damaged. During the onset of heat stroke, as compared to those of normothermia controls, the heat stroke rats displayed a higher value of colonic temperature or neuronal damage score, as well as a lower value of local cerebral blood flow or mean arterial blood pressure. In addition, compared to those of normothermic, control rats, the heat stroke rats had increased interleukin-1 and tumor necroting factor production in the diencephalon, brain stem and cortex. The heat stroke-induced neuronal damage and diminished local cerebral blood flow in different brain structures, as well as the systemic hypotension, were attenuated in animals pretreated with IL-1ra (200 micrograms/kg, iv) 30 min before the onset of heat stroke. The results indicate that IL-1ra attenuates the heat stroke-induced cerebral neuronal damage by reducing cerebral ischemia in rats.

Animals↗

Celahinine A, a new sesquiterpene pyridine alkaloid from Celastrus hindsii.

A new sesquiterpene pyridine alkaloid, celahinine A [1], and the related known polyester celahin A, as well as the known cytotoxic sesquiterpene pyridine alkaloid emarginatine A [2], were isolated from Celastrus hindsii. The structure of 1 was determined by 2D nmr techniques and was also confirmed by spectral comparison with the related 2.

Antineoplastic Agents, Phytogenic↗

Effects of honokiol and magnolol on acetylcholine release from rat hippocampal slices.

To study the possible mechanism through which honokiol and magnolol elicit their central depressant effects, we examined the influence of these two phenolic compounds on 25 mM K(+)-stimulated release of [3H]acetylcholine (ACh) from the rat's hippocampal slices. Honokiol, but not magnolol, elicited a concentration-dependent enhancement of K+-evoked ACh release. Addition of either tetrodotoxin, pilocarpine, or methoctramine had no effect on honokiol-enhanced ACh release. These results suggest that honokiol enhanced K(+)-evoked ACh release directly on hippocampal cholinergic terminals via receptors other than the M2 cholinergic subtypes.

Acetylcholine↗

Purification of chlorpromazine-sensitive GTPase from rat cerebral cortex.

The chlorpromazine-sensitive GTPase from the cell membrane of rat cerebral cortex was purified to homogenity by using DEAE Bio-Gel A agarose, hydroxyapatite and heparin agarose chromatography. The purified chlorpromazine-sensitive GTPase was purified 370-fold to obtain a final specific activity of 40 mumol GTP hydrolyzed2min/mg protein. The purified enzyme was inhibited by chlorpromazine but not by compound 48/80. Magnesium was required for its activity instead of calcium. The purified enzyme had an apparent pH optimum of 8.0, and molecular weight was estimated to be 58,000.

Animals↗

Characterization of a novel 350-kilodalton nuclear phosphoprotein that is specifically involved in mitotic-phase progression.

A gene assigned to human chromosome 1q32-41 encodes a novel protein of 3,113 amino acids containing an internal tandem repeat of 177 amino acids. The protein, which we have named "mitosin," was identified by direct binding to purified retinoblastoma protein in vitro with a region distantly related to the retinoblastoma protein-binding site of E2F-1. Mitosin is expressed throughout S, G2, and M phases of the cell cycle but is absent in G1. Its localization is dramatically reorganized from a rather homogeneous nuclear distribution in S phase to paired dots at the kinetochore/centromere region, to the spindle apparatus, and then to the midbody during M-phase progression. This spatial reorganization coincides closely with the temporal phosphorylation patterns of mitosin. Overexpression of N-terminally truncated mutants blocks cell cycle progression mainly at G2/M. These results suggest that mitosin may play an important role in mitotic-phase progression.

Amino Acid Sequence↗

The anti-inflammatory effects of Chinese crude drug prescriptions on experimental arthritis.

San-Miao-Warn (SMW), Tuhwo-Jih-Shen-Tang (TJS) and Dang-Quei-Nian-Tong-Tang (DGT) are Chinese traditional prescriptions. In this study, we evaluated the anti-inflammatory activities of these crude drug prescriptions in carrageenan-induced acute arthritis and complete Freund's adjuvant (CFA)-induced chronic arthritis in rats. It was found that pretreatment with SMW, TJS or DGT at a dosage of 100 mg/kg or 300 mg/kg, significantly inhibited carrageenan-induced acute arthritis. Moreover, these crude drugs also significantly suppressed the development of chronic arthritis induced by CFA. These results suggest that SMW, TJS and DGT are potential anti-inflammatory agents and may be considered as alternatives for non-steroid anti-inflammatory drugs (NSAID).

Administration, Oral↗