Biological activity of a fruit vegetable, "Anastasia green", a species of sweet pepper.

Russian green sweet pepper (Anastasia Green) was successively extracted with hexane, acetone, methanol and 70% methanol and the extracts were further separated into a total of twenty fractions by silica gel or ODS column chromatographies. The biological activities of these extracts and fractions were compared. The extracts and fractions showed higher cytotoxic activity against two human oral tumor cell lines than against normal human gingival fibroblasts, suggesting their tumor-specific action. Several fractions [H3, H4, A4] reversed the multidrug resistant gene (MDR1) against L5178 mouse T-cell lymphoma more effectively than (+/-) verapamil (positive control). All extracts and fractions showed no anti-human immunodeficiency virus (HIV) nor anti-Helicobacter pylori activity. These data suggest the medicinal importance of an Anastasia Green extract.

Biological activity of kiwifruit peel extracts.

Various bioactive substances in kiwifruit extracts were fractionated by organic solvent extractions, followed by silica gel and ODS chromatographies. Both cytotoxic activity and multi-drug resistance reversal activity were found in the less polar fractions. Cytotoxic activity was not always parallel the radical intensity. Antibacterial activity was distributed into various fractions and all fractions were inactive against Candida albicans and H. pylori. Only 70% methanol extracts showed anti-human immunodeficiency virus activity, and produced a broad ESR signal under alkaline conditions, in a fashion similar to lignin. These fractions also effectively scavenged O(2)(-) produced by the xanthine-xanthine oxidase reaction, suggesting a bimodal (pro-oxidant and antioxidant) action. These data suggest a medicinal efficacy of kiwifruit peel extracts.

In vitro biological activity of prenylflavanones.

The biological activity of ten prenylflavanones purified from Sophora tomentosa L., and Sophora moorcroftiana Benth. ex Baker (Leguminosae) was investigated. The flavanones with prenyl-, lavandulyl- or geranyl groups on A ring, and two bioactive flavonostilbenes on ring B and stilbene (resveratrol) showed tumor-specific cytotoxic activity, antimicrobial activity, and anti-HIV activity, radical generation, and O2- scavenging activity. There was a positive relationship between radical generation and O2- scavenging activity in these prenylflavanones. These data suggest the medicinal significance of prenylflavanones.

Antioxidative activity of Allium victorialis L. extracts.

Allium victorialis L. (Liliaceae, "Hon-Gyoujya Nin-Niku" in Japanese) was successively extracted with hexane, acetone, methanol and 70% methanol and the extracts were further separated into a total of twenty-five fractions by silica gel and ODS column chromatographies. The biological activities of these four extracts and 25 column fractions were compared. The cytotoxic activity of all extracts and fractions against two oral tumor cell lines was significantly higher than that against normal human gingival fibroblasts, suggesting their tumor-specific action. Three methanol column fractions [M2, M3, M6] and a 70% methanol column fraction [70M6] most effectively reversed the multidrug resistance (MDR) against L5178 mouse T cell lymphoma. The electron spin resonance (ESR) spectroscopy showed that methanol column fractions and 70% methanol extracts produced the highest amount of radical(s) and most efficiently scavenging O2*-, generated by the hypoxanthine-xanthine reaction system, suggesting that the same substances in these fractions display both prooxidant and antioxidant properties. They showed no anti-human immunodeficiency virus (HIV) or anti-Helicobacterpylori activity. These data suggest the medicinal efficacy of Allium victorialis extract.

Selective cytotoxic activity of grape peel and seed extracts against oral tumor cell lines.

Grape seed extracts were more cytotoxic than grape peel extracts. Methanol and 70% methanol extracts of grape seed selectively killed two human oral tumor cell lines, more efficiently than human gingival fibroblasts. ESR spectroscopy revealed that these extracts produced radicals under alkaline conditions and enhanced the radical intensity of sodium ascorbate at higher concentrations. On the other hand, lower concentration of these extracts slightly reduced the radical intensity of sodium ascorbate, and scavenged superoxide anion, generated by hypoxanthine and xanthine oxidase reaction. These properties of grape seed extracts suggest their possible application for cancer prevention.

Biological activity of feijoa peel extracts.

Fractionated extracts of Feijoa peels were studied for cytotoxic activity, anti-human immunodeficiency virus (HIV) activity and antibacterial activity. Two most cytotoxic fractions A3 of acetone extract and M2 of methanol extract had potent inhibitory activity against Gram-positive and Gram-negative bacteria as well as fungi tested. Fraction A4 of acetone extract showed multidrug resistance (MDR)-reversal activity comparable with that of verapamil (positive control). These results indicate the therapeutic value of Feijoa peel extracts as potential antimicrobial and MDR-modulating agents.

Relationship between radical intensity and biological activity of cacao husk extracts.

The relationship between radical intensity and biological activity of cacao husk extracts was investigated. Electron spin resonance (ESR) spectroscopy demonstrated that the radical intensity of hexane, acetone, methanol and 70% methanol extracts increased with water-solubility. Several fractions of these husk extracts, separated by different column chromatographies, significantly inhibited the cytopathic effect of human immunodeficiency virus (HIV) infection in parallel with their radical intensity. However, their cytotoxic activity against human leukemic and carcinoma cell lines is not always correlated with their radical intensity. Water-soluble and lipophilic compounds might induce cytotoxic activity by different mechanisms.

TJS-010, a new prescription of oriental medicine, antagonizes tetrabenazine-induced suppression of spontaneous locomotor activity in rats.

1. The authors have determined the effect of TJS-010, a new prescription of oriental medicine, on the locomotor activity in rats. 2. Tetrabenazine(TBZ) decreased the spontaneous locomotion in rats, and attenuated the contents of amines and increased their metabolism in various regions in rat brain. 3. TJS-010 inhibited the locomotor suppression induced by TBZ: however, neither amine contents nor their metabolism was not altered, which suggested that TJS-010 postsynaptically modulated the transmission or transduction. 4. Imipramine also inhibited the decrease in locomotion induced by TBZ. 5. These results suggest a possibility that TJS-010 has an antidepressive effect.

TJS-010, a new prescription of Kampo medicine with putative antidepressive and anxiolytic properties.--A behavioral study using experimental models for depression and anxiety.

We investigated the effect of TJS-010, a new prescription of Kampo or oriental medicine, on the locomotor activity and body temperature in rats in order to determine its antidepressive and anxiolytic effects. Tetrabenazine(TBZ), which sometimes induces depression in humans, decreased the spontaneous locomotion in rats, and attenuated the content of amines in several regions in the rat brain when intraperitoneally injected. TJS-010 was orally administered at a concentration of 750 mg/kg, and inhibited the locomotor suppression. The content of amines was not, however, altered. These results indicate that TJS-010 postsynaptically modulates the transmission or transduction. Imipramine, 5mg/kg, also enhanced locomotion in TBZ-treated rats, which was similar to the effect of TJS-010. These results suggest that TJS-010 has an antidepressive effect. TJS-010 also facilitated the hypothermia induced by subcutaneous injection of 0.1 mg/kg (+/-)-8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT), which is known to be mediated by serotonin-1A receptors. The hypothermia in the rats via an activation of serotonin-1A receptors is often observed with anxiolytic drugs. These results may raise the possibility that TJS-010 has an anxiolytic property. TJS-010 may serve as a useful drug for the treatment of those who suffer from depressive and anxiety disorders.

Chromatographic techniques used to determine benz[c]acridines in environmental samples.

Benz[c]acridine and many of its related compounds have been shown to exhibit carcinogenic activity. Unfortunately, these compounds are continually being found in many natural and environmental samples in widely divergent geographical locations. A review of chromatographic methods for mainly benz[c]acridine and its analogues is presented.

[A case of Nasu-Hakola's disease with T2-weighted MRI finding of reduced signal intensity in the thalamus and putamen].

A 30-year-old female received a head injury at the age of 22 years. Subsequently neurological and psychiatric symptoms, such as personality change, urinary incontinence, dementia and gait disturbance developed. On admission, her cognitive function was severely impaired. Brain CT disclosed cerebral atrophy, dilatation of the lateral ventricle and calcification of the basal ganglia. Pathologically membranous structures were recognized in bone marrow. On the basis of these clinical findings, a diagnosis of Nasu-Hakola's disease was made. In this case, a T2-weighted MRI finding of reduced signal intensity in the thalamus and putamen was characteristic. This finding may be related to intracranial calcification.

Concentration and degradation of hyaluronic acid in knee synovial fluid from carrageenin-induced rabbit arthritis.

The concentration and degradation of hyaluronic acid in the synovial fluid of carrageenin-induced arthritic joints of rabbits was studied. A 0.5-ml volume of 1% lambda-carrageenin was intra-articularly injected three times into a right knee joint, and saline into a left. After 5 d from the last injection, inflammatory changes were observed in the synovial membrane and synovial fluid, but not in the articular cartilage. In the inflammatory synovial fluid, lipid peroxide content, phosphatase activity and cell counts were significantly increased, but the copper concentration was not changed. Concentration of polymeric hyaluronic acid and total hyaluronic acid were determined by high-performance liquid chromatography using gel-permeation columns. Total hyaluronic acid was appreciably decreased in the inflammatory fluid. The polymeric hyaluronic acid determined was 38% of the total hyaluronic acid in the inflammatory fluid and 74% in the control fluid. This suggests that in the inflammatory fluid, molecular weights of hyaluronic acid are distributed in the broader range. The concentration of chondroitin sulphates was similar in both the inflammatory fluid and the control fluid, but the content ratio of chondroitin sulphates to hyaluronic acid was higher in the inflammatory fluid. In the inflamed synovial membrane, synthesis of hyaluronic acid as measured by incorporation of [14C]glucosamine into glycoconjugates was increased by about twice that in the control membrane.

Lesion of nucleus basalis magnocellularis decreases [3H]hemicholinium-3 binding (as measured by autoradiography) in the amygdala and frontal cortex of the rat.

The effects of a unilateral electrolytic lesion of the nucleus basalis magnocellularis on [3H]hemicholinium-3 binding sites in discrete brain regions of the rat were studied through the use of quantitative autoradiography. When compared to the contralateral side this lesion caused a decrease in the density of [3H]hemicholinium-3 binding sites in the medial prefrontal cortex, frontoparietal cortex and basolateral nucleus of the amygdala but not in the caudate-putamen, nucleus accumbens, olfactory tubercle, hippocampus and auditory cortex. These results add further weight to the view that the cholinergic innervation of the rostral cerebral cortex and amygdala originates from the nucleus basalis magnocellularis and suggest that [3H]hemicholinium-3 autoradiography is a suitable means of visualizing cholinergic nerve terminals.