Penidioxolanes A and B, 1,3-Dioxolane Containing Azaphilone Derivatives from Marine-derived Penicillium sp. KCB12C078

Two new azaphilone derivatives containing 1,3-dioxolane moiety, penidioxolanes A (1) and B (2), were isolated from marine-derived fungus Penicillium sp. KCB12C078, together with four known compounds (3-6) by chemical investigation. Compounds 1 - 6 were isolated by combination of silica gel, ODS column chromatography and preparative HPLC. Their structures were determined by analysis of spectroscopic data including 1D-, 2D-NMR, and MS techniques. The isolates were evaluated against cancer cell growth inhibition effects and antimicrobial activity.

The Effect of Polygalasaponins in Polygalae Tenuifolia on Apomorphine-Induced Hyperlocomotions in Mice / 대한정신약물학회지

OBJECTIVE: This study was to investigate in vivo antidopaminergic activities of polygalasaponins which included in the roots of Polygalae tenuifolia, one of the natural plants prescribed to treat psychotic disorders in traditional medicine. METHODS: The chemical separations were conducted by chromatographies with various columns and the chemical structures were identified using spectroscopy, NMR and so on. The apomorphine-induced stereotyped behaviors and climbing behaviors in mice as animal models of psychotic disorders were applied to explore the antidopaminergic activity. RESULTS: The active compounds with antidopaminergic effects in the roots of Polygalae tenuifolia were identified as polygalasaponin A-D. The polygalasaponins showed to suppress the apomorphine-induced stereotyped behaviors and climbing behaviors in dose-related fashions. CONCLUSION: This study suggests that polygalasaponins might have antipsychotic activities. The natural products need to be explored extensively as sources of new medications in psychiatric fields. Further explorations for chemical and pharmacological properties of polygalasaponins are required.

Alpha-2 Adrenoceptor Binding Profile of Natural Products Used to Treat Psychotic illnesses / 대한정신약물학회지

Natural products have long been major sources of pharmaceutical products in medicine. We have undertaken a series of studies designed to characterize the pharmacologic profiles of natural products used to treat psychotic illnesses in Korean traditional medicine. In our previous screening assays, we found that three of plant extracts (Coptidis j, Citrus u, and Phellodendron a) contain active components which show relatively potent binding to alpha-2 adrenoceptors. The present study is to explore pharmacologic activities of extracts as agonism or antagonism by G-protein modulations in radioligand receptor binding study. We have found that two extracts(Coptidis j and Phellodendron a) contain active ingredients which have antagonistic properties to alpha-2 adrenoceptors, whereas one plant extract (Citrus u) has agonistic properties. The demonstration of three plant extracts used to treat psychotic illnesses in Korea may help in the elucidation or their pharmacologic characteristics and provide insights for the development of new psychotropic drugs.

Effects of Polygalae Radix on Apomorphine-Induced Stereotyped Behaviors in Mice / 신경정신의학

OBJECTIVES: This study was to investigate in vivo activities of Polygalae Radix, a natural plant including active components having affinities to central nervous system receptors, using an animal model for psychotic disorders in terms of behavioral psychopharmacology. METHODS: The extracts of Polygalae Radix in two concentrations of 5.0mg/g and 0..5mg/g were administered to mice in order to explore the suppression of apomorphine-induced stereotyped behaviors visually and to compare with the effects of haloperidol and control. 10 mice were tested in each groups. RESULTS: The capacities of suppressing the apomorphine-induced stereotyped behaviors were observed in decreasing order of haloperidol, Polygalae Radix 5.0mg/g, Polygalae Radix 0..5mg/g and control. The extracts of Polygalae Radix in both concentrations suppressed apomorphine- induced stereotyped behaviors significantly, and Polygalae Radix 5.0mg/g was as potent as haloperidol. CONCLUSION: This suggests that Polygalae Radix contain some effective ingredients to influence the central dopamine pathway in vivo. The identification of the chemical structures and the exploration of the biochemical and pharmacological characteristics of active components are to be required through further studies.