To study the chemical constituents of the mycelia of the Endophytes YD-01, 2, 3-dihydroxy-quinoline-4-O-beta-D-glucopyranoside (1), 3-methyl-pyrrol opiperazine-2, 5-dione (2) and naringenin (3) were isolated from its acetone extracts by using silica gel column chromatography and Sephadex LH-20. Their structures were elucidated on the basis of spectroscopic analysis. Compound 1 is a new compound.
Alternaria ; chemistry ; Diketopiperazines ; chemistry ; isolation & purification ; Flavanones ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Hydroxyquinolines ; chemistry ; isolation & purification ; Molecular Structure ; Mycelium ; chemistry ; Pyrroles ; chemistry ; isolation & purification

AIM: To investigate the quinoline alkaloids from the roots of Dictamnus angustifolius G.Don ex Sweet (Rutaceae). METHOD: The quinoline alkaloids were isolated by various column chromatographic methods and their structures were elucidated on the basis of spectral analysis. RESULTS: A new quinoline alkaloid, 5-methoxylrobustine (1), along with five known quinoline alkaloids were obtained, and their structures were identified as dictamnine (2), robustine (3), isopteleine (4), γ-fagarine (5), and skimmianine (6). Cytotoxicity testing of these alkaloids showed that all of them had weak cytotoxic activities against human breast cancer cells (MCF7). CONCLUSION Compound 1 is a new quinoline alkaloid. Alkaloid 3 showed stronger anti-proliferation effect than the other alkaloids.
Antineoplastic Agents, Phytogenic ; isolation & purification ; pharmacology ; therapeutic use ; Breast Neoplasms ; drug therapy ; Cell Line, Tumor ; Dictamnus ; chemistry ; Humans ; Hydroxyquinolines ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Molecular Structure ; Phytotherapy ; Plant Extracts ; chemistry ; pharmacology ; therapeutic use ; Plant Roots ; chemistry ; Quinolines ; chemistry ; isolation & purification ; pharmacology ; therapeutic use

Diiodohydroxyquin introduced by Dillaha et al in 1953, had been the mainstay for the treatment of acrodermatitis enteropathica (A.E.). However, following the report by Moynahan and Barnes in 1973 of successful treatment with the oral administration of zinc sulfate, the clinical response to this treatment has been confirmed by different investigators in many countries. In Korean literature, Rhim et al reported two cases of A,E. in siblings successfully treated with oral zinc sulfate in 1980. In our case of cow's milk-fed, 7 month-old male infant, typical claasical features of total alopecia, diarrhea and periorificial dermatitis developed at about 3 months. of age and the zinc level in serum was 101 ug/dl at the first visit. Treatment first with diiodohydroxyquin was initiated at a dose of 315 mg/day by mouth for the first week and 630 mg/day for the second week, but this therapeutic regimen brought about little or no effect. Because of no definite improvement even with increasing dose of 1260 mg/day for another week, treatment was. changed to oral zinc sulfate. The patient began to receive zinc sulfate 50mg at first day by mouth and the dosage was immediately increased to l00mg daily from the next day. Within 72 hrs there found dramatic improvement in the skin lesions and diharrhea stopped. Twenty days after the start of zinc therapy, nearly all the skin lesions disappeared and the patient was discharged in satisfactory condition with only mild residual erythema. (countinued..)
Acrodermatitis* ; Administration, Oral ; Alopecia ; Dermatitis ; Diarrhea ; Erythema ; Humans ; Infant ; Iodoquinol ; Male ; Mouth ; Research Personnel ; Siblings ; Skin ; Zinc ; Zinc Sulfate

Clinical studies on five patients with acrodermatitis enteropathica visited during the period from March 1968 to September 1970 to the department of dermatology, Pusan national University hospital were made and the results obtained were summerized as follows; in addition, the literature was reviewed. 1) All of 5 patients aging from 3 months to 3 years, showed characteristic distributions of the cutaneous lesions which ranged in character from vesicobullous to heavily scaled psoriasiform and moniliasis-like lesions. 2) Of these, the nearly full clinical pictures were presented in two cases with the gradual onset in early infancy, dermatitis predominantly involving the periorficial areas and extremities, which followed by recurrent attacks of greenish yellow-colored diarrhea, partial and diffuse loss of the scalp hairs, stomatitis and monilial infections, whereas the rest thtee cases seemed to be "forme fruste" of this disease with the absence of hair and nail abnormalities. 3) There found no speeific histologic findings in two biopsies performed but showed somewhat the pictures of sub-acute dermatoses. 4) Candida albicans were demonstrated from the skin lesions in two cases, 5) Treatment with local application of gentian violet solution, nystatin ointment for the skin lesions and stomatitis were temporarily favorable in all cases and in case 1 and 5, diodoquin, each 300mg and 600mg were administered orally in divided doses for two weeks, with the result of satisfactory responses. However, the latter died, on the 3rd hospitalized day, of acute glomerulonephritis and upper respiratory infection. 6) Though it is generally accepted that there is definite familial occurrence in this disorder but we recognized no evidence of familial incidence in our five cases.
Acrodermatitis* ; Aging ; Biopsy ; Busan ; Candida albicans ; Dermatitis ; Dermatology ; Diarrhea ; Extremities ; Gentian Violet ; Glomerulonephritis ; Hair ; Humans ; Incidence ; Iodoquinol ; Nails, Malformed ; Nystatin ; Scalp ; Skin ; Skin Diseases ; Stomatitis

No abstract available.
Animals ; Cerebral Cortex* ; Glutamic Acid* ; Glycine* ; Kynurenic Acid* ; Perfusion* ; Rats*

BACKGROUND AND OBJECTIVES: Locacorten Vioform (Novartis UK) is frequently prescribed for otomycosis. Its component, Clioquinol, also has anti-bacterial properties. Up to this point, its ototoxic potential has not been evaluated. Our objective aims to evaluate Locacorten Vioform’s potential ototoxicity when applied directly to the middle ear cavity. MATERIALS AND METHODS: We performed an experimental prospective animal study in our animal research center with 20 Hartley guinea pigs divided into 2 groups. The first group (experimental) was treated with Locacorten Vioform in one ear and with a physiologic saline solution in the other. The second group (positive control) was treated with concentrated gentamycin in one ear and physiologic saline in the other. Auditory brainstem response measurements were obtained before and after three sets of injections. Statistics were analyzed using a variance analysis with repeated measures. The histological state of cochlear outer hair cells was compared between the two groups using scanning electron microscopy. RESULTS: Average hearing loss in ears treated with Locacorten Vioform was 32.1 dB, compared with a 2.5 dB average loss in the saline-treated ears. Ears treated with gentamycin lost an average of 33.0 dB. There were clinically and statistically significant differences between the two ears of the guinea pigs in both groups (p < 0.001). Scanning electron microscopy revealed severe pericochlear and cochlear inflammation and ossification in the Locacorten Vioform-treated ears. Gentamycin caused significant destruction of outer hair cell architecture. CONCLUSIONS: Locacorten Vioform induces a hearing loss similar to that caused by gentamycin when applied directly to the middle ear of a guinea pig model. Electron microscopy indicates a pericochlear and cochlear inflammatory reaction with ossification.
Animal Experimentation ; Animals ; Clioquinol ; Ear ; Ear, Middle ; Evoked Potentials, Auditory, Brain Stem ; Gentamicins ; Guinea Pigs ; Guinea ; Hair ; Hair Cells, Auditory, Inner ; Hair Cells, Auditory, Outer ; Hearing Loss ; Inflammation ; Microscopy, Electron ; Microscopy, Electron, Scanning ; Otomycosis ; Prospective Studies ; Sodium Chloride

To investigate the mechanism of the excitatory signal transmission, the effects of N-methyl-D-aspartate(NMDA, ionotropic glutamate agonist) and kynurenic acid(glutamate antagonist) on catfish retinal neurons were explored using conventional intracellular recording techniques. Horizontal cells were depolarized by glutamate, kainate, quisqualate, and NMDA but gyperpolarized by kynurenate. Transient components of both ON-and OFF-bipolar cells were reduced either by glutamate or by NMDA. Kynurenate suppressed sustained components of the third-order neurons or OFF-bipolar cells. Furthermore, kynurenate blocked the depolarizing actions of NMDA on horizontal cells and ON-sustained cells with large ON-transient components. The results suggest that NMDA would exert a tonic depolarization in the horizontal cells and the 3rd-order neurons, and there might be a preferential suppression on the a NMDA receptors by kynurenic acid in the catfish retina.
Catfishes ; Glutamic Acid ; Kainic Acid ; Kynurenic Acid* ; N-Methylaspartate ; Neurons* ; Quisqualic Acid ; Receptors, N-Methyl-D-Aspartate ; Retina* ; Retinal Neurons

The basic mechanism for the excitation of the peripheral vestibular receptors following acute hypotension induced by sodium nitroprusside (SNP) or hemorrhage was investigated in anesthetized rats. Electrical activity of the afferent vestibular nerve was measured after pretreatment with kynurenic acid, an NMDA receptor antagonist. The activity of the vestibular nerve at rest following acute hypotension induced by SNP or simulating hemorrhage was a greater increase than in control animals. The gain of the vestibular nerve with sinusoidal rotation following acute hypotension increased significantly compared to control animals. The acute hypotension induced by SNP or hemorrhage did not change the activity of the afferent vestibular nerve after kynurenic acid injection. These results suggest that acute hypotension produced excitation of the vestibular hair cells via glutamate excitotoxicity in response to ischemia.
Animals ; Glutamic Acid ; Hair Cells, Vestibular ; Hemorrhage ; Hypotension* ; Ischemia ; Kynurenic Acid ; N-Methylaspartate ; Nitroprusside ; Rats* ; Vestibular Nerve*

Tryptophan metabolites regulate a variety of physiological processes, and their downstream metabolites enter the kynurenine pathway. Age-related changes of metabolites and activities of associated enzymes in this pathway are suggestable and would be potential intervention targets. Blood levels of serum tryptophan metabolites in C57BL/6 mice of different ages, ranging from 6 weeks to 10 months, were assessed using high-performance liquid chromatography, and the enzyme activities for each metabolic step were estimated using the ratio of appropriate metabolite levels. Mice were subjected to voluntary chronic aerobic exercise or high-fat diet to assess their ability to rescue age-related alterations in the kynurenine pathway. The ratio of serum kynurenic acid (KYNA) to 3-hydroxylkynurenine (3-HK) decreased with advancing age. Voluntary chronic aerobic exercise and high-fat diet rescued the decreased KYNA/3-HK ratio in the 6-month-old and 8-month-old mice groups. Tryptophan metabolites and their associated enzyme activities were significantly altered during aging, and the KYNA/3-HK ratio was a meaningful indicator of aging. Exercise and high-fat diet could potentially recover the reduction of the KYNA/3-HK ratio in the elderly.
Aged ; Aging ; Animals ; Chromatography, Liquid ; Diet, High-Fat* ; Exercise* ; Humans ; Infant ; Kynurenic Acid ; Kynurenine* ; Mice ; Physiological Processes ; Tryptophan*

The decrease in maternal plasma total (free + albumin-bound) tryptophan (Trp) during the third pregnancy trimester is attributed to induction of indoleamine 2,3-dioxygenase (IDO). When measured, free [Trp] is increased because of albumin depletion and non-esterified fatty acid elevation. The Trp depletion concept in pregnancy is therefore not supported because of incorrect interpretation of changes in Trp disposition and also for not addressing mouse strain differences in Trp-related responses and potential inhibition of Trp transport by the IDO inhibitor 1-methyl tryptophan. Application of the Trp utilization concept in pregnancy offers several physiological advantages favoring fetal development and successful outcome, namely provision of Trp for fetal protein synthesis and growth, serotonin for signaling pathways, kynurenic acid for neuroprotection, quinolinic acid for NAD+ synthesis, and other kynurenines for suppression of T cell responses. An excessive increase in Trp availability could compromise pregnancy by undermining T cell suppression, e.g., in pre-eclampsia.
Animals ; Female ; Fetal Development ; Humans ; Indoleamine-Pyrrole 2,3,-Dioxygenase ; Kynurenic Acid ; Mice ; Plasma ; Pre-Eclampsia ; Pregnancy Trimester, Third ; Pregnancy* ; Quinolinic Acid ; Serotonin ; Tryptophan*