Paniculacin, a new coumarin derivative from Murraya paniculata

Paniculacin (1), a new coumarin derivative, has been isolated from the ethyl acetate soluble fraction of the ethanolic extract of Murraya paniculata along with umbelliferone, scopoletin, 4-hydroxybenzoic acid, trans-cinnamic acid, and β-sitosterol. Their structures were elucidated on the basis of spectral data.     

Paniculacin,a new coumarin derivative from Murraya paniculata

Paniculacin (1), a new coumarin derivative, has been isolated from the ethyl acetate soluble fraction of the ethanolic extract of Murraya paniculata along with umbelliferone, scopoletin, 4-hydroxybenzoic acid, trans-cinnamic acid, and β-sitosterol. Their structures were elucidated on the basis of spectral data.     

Selaginellin M, a new selaginellin derivative from Selaginella pulvinata

A new selaginellin derivative, selaginellin M (1), together with one known compound, selaginellin E (2), was isolated from Selaginella pulvinata. The structure of the new compound was elucidated and named as (R,S)-4-((4'-hydroxy-4-((2-hydroxyethoxy)methyl))-3-((4-hydroxyphenyl)ethynyl)biphenyl-2-yl)(4-hydroxyphenyl)methylene)cyclohexa-2,5-dienone on the basis of the spectroscopic data including UV, IR, 1D, and 2D NMR as well as HR-ESI-MS analysis.     

Cyclobakuchiol C, a new bakuchiol derivative from Psoralea coryllfolia

A new compound, cyclobakuchiol C (1), together with four known bakuchiol derivatives, 2-5, was isolated from the non-polar fraction of the seeds of Psoralea corylifolia, and compounds 3-5 were identified from this plant for the first time. The structure of 1 was determined by spectroscopic methods, especially 2D NMR experiments.     

Selaginellin M,a new selaginellin derivative from Selaginella pulvinata

A new selaginellin derivative, selaginellin M (1), together with one known compound, selaginellin E (2), was isolated from Selaginella pulvinata. The structure of the new compound was elucidated and named as (R,S)-4-((4′-hydroxy-4-((2-hydroxyethoxy)methyl))-3-((4-hydroxyphenyl)ethynyl)biphenyl-2-yl)(4-hydroxyphenyl)methylene)cyclohexa-2,5-dienone on the basis of the spectroscopic data including UV, IR, 1D, and 2D NMR as well as HR-ESI-MS analysis.     

Griseusin D, a new pyranonaphthoquinone derivative from a alkaphilic Nocardiopsis sp

A new pyranonaphthoquinone antibiotic, griseusin D (1) was isolated from the cultural fluid of the alkaphilic Nocardiopsis sp. The structure was determined as 5'-one-4-hydroxy-12-methoxygriseusin by spectroscopic methods, comparison with reported data and single-crystal X-ray analysis. 1 displayed strong cytotoxicity against human leukemia cells (HL60) and modest cytotoxicity against human lung adenocarcinoma cell lines (AGZY) with IC(50) values of 0.23 and 19.6 microg/ml, respectively. It also exhibited weak antifungal activity against Alternaria alternate with MIC of 140 microg/ml.     

A new cinnamoylphenethylamine derivative from a Mongolian Allium species,Allium carolinianum

Journal of Natural Medicines - A new cinnamoylphenethylamine derivative, compound 1, was isolated as the main HPLC peak after partitioning the methanol extract of bulbs of a Mongolian onion...     

Kakispyrol, a new biphenyl derivative from the leaves of Diospyros kaki

A new biphenyl derivative, 4',5-dimethoxy-3-beta-D-glucopyranosyloxy-4-hydroxy-biphenyl, named kakispyrol (1), has been isolated from the leaves of Diospyros kaki, together with three known compounds, vitexin (2), 2'-O-rhamnosyl vitexin (3) and isorhamnetin-3-O-beta-D-glucopyranoside (4). The structure of compound 1 has been determined on the basis of spectroscopic evidence.     

Two new guaianolides and a new daucene derivative from Sinodielsia yunnanensis

From the roots and rhizomes of Sinodielsia yunnanensis, three new sesquiterpenes were isolated and their structures were established as 5alpha,6beta- H-1(10),3,7(11)-guaiatrien-12,6alpha-olide ( 1), 5alpha,6beta,7beta- H-1(10),3-guaiadien-12,6alpha-olide ( 2) and 5beta-hydroxy-10alpha- O-angeloyl-3-oxodauc-8-ene ( 3) by means of spectroscopic analyses and single-crystal X-ray experiment (for compound 1).     

Alliumonoate: a new cyclopentane derivative from Allium victorialis

Alliumonoate (1), a new cyclopentane derivative, has been isolated from the chloroform-soluble fraction of the ethanolic extract of Allium victorialis, along with β-amyrin acetate (2), β-sitosterol acetate (3), 22-cyclohexyl-1-docosanol (4), β-amyrin (5), β-sitosterol (6), and β-sitosterol 3-O-β-d-glucopyranoside (7), reported for the first time from this species. Their structures were elucidated on the basis of spectral data including mass spectra and 2D NMR experiments.     

Alliumonoate: a new cyclopentane derivative from Allium victorialis

Alliumonoate, a new cyclopentane derivative, has been isolated from the chloroform-soluble fraction of the ethanolic extract of Allium victorialis, along with β-amyrin acetate, β-sitosterol acetate, 22-cyclohexyl-1-docosanol, β-amyrin, β-sitosterol, and β-sitosterol 3-O-β-D-glucopyranoside, reported for the first time from this species. Their structures were elucidated on the basis of spectral data including mass spectra and 2D NMR experiments.     

Ethaverine, a derivative of papaverine, inhibits cardiac L-type calcium channels.

Ethaverine is a derivative of papaverine used in the treatment of peripheral vascular disease and is thought to cause vasodilation by reducing intracellular Ca2+ concentrations in vascular smooth muscle cells. We tested its effects on single, dihydropyridine-sensitive, L-type calcium channels from porcine cardiac muscle, incorporated into planar lipid bilayers. L-type calcium channels were activated by step depolarizations from a holding potential of -60 mV to a test potential of 0 mV, and unitary currents carried by 100 mM BaCl2 were recorded. Channel activity was enhanced by the presence of the dihydropyridine agonist (+)-202-791 (0.5 microM) and the activated alpha subunit of the stimulatory GTP-binding protein, Gs. We found that 0.3-30 microM ethaverine on either side of the channel caused a reduction in the channel open probability (EC50 approximately 1 microM), with the higher concentrations inhibiting channel activity almost completely. In addition, the ethaverine caused a small reduction in the unitary current amplitude of single open channels (approximately 20%). To test whether the effect of ethaverine on open probability was due to a displacement of the dihydropyridine agonist, we studied the effect of ethaverine on the binding of [3H]nitrendipine to cardiac sarcolemma and found that ethaverine inhibited [3H]nitrendipine binding with a Ki of approximately 8.5 microM. Ethaverine also inhibited the binding of [3H]diltiazem and [3H]verapamil, with Ki values of 1-2 microM. Because ethaverine is structurally related to verapamil, it is likely that ethaverine acts by binding to the verapamil binding sites on the L-type calcium channels to inhibit channel activation and dihydropyridine binding.     

Baclofen, a GABA derivative, inhibits stress-induced prolactin release in the rat

The effect of baclofen, beta-(4-chlorophenyl)GABA, on prolactin secretion was investigated in rats under several experimental conditions. In adult male rats subjected either to immuobilization, ether, swimming or cold stress there was a rapid increase of serum prolactin levels; acute pretreatment with baclofen, 10 mg/kg i.p. inhibited the hormone response to all these stresses. The same blocking effect of the drug was observed in prepubertal male and female rats and in adult gonadectomized animals. In basal conditions, i.e. in undisturbed male rats, baclofen did not change the hormone titers significantly. Taken together our results indicate that baclofen blocks prolactin release when release of the hormone is dynamically stimulated by stress and this effect is relatively independent of the endocrine status of the rat.     

Neurochemical study of mafoprazine, a new phenylpiperazine derivative

Mafoprazine, a phenylpiperazine derivative, was neurochemically investigated in rats to determine its action mechanism. The rank order of affinity of mafoprazine for neuronal receptors was D2 greater than or equal to alpha 1 greater than S2 greater than alpha 2 much greater than D1 greater than beta greater than mACh. The affinity of mafoprazine for D2 receptors (Ki = 10.7 nM) was 2 times higher than that of azaperone, and 6 and 16 times lower than those of chlorpromazine and haloperidol, respectively, whereas the D2 receptor selectivity [D1/D2 (Ki value ratio)] of mafoprazine was 10, 9 and 2 times higher than those of chlorpromazine, azaperone and haloperidol, respectively. The affinity of mafoprazine for alpha 2 receptors in terms of the ratio of the Ki values for D2 and alpha 2 receptors (D2/alpha 2) was 345, 26 and 3 times higher than those of haloperidol, chlorpromazine and azaperone, respectively. Mafoprazine slightly showed the inhibitory effect on dopamine-stimulated adenylate cyclase (IC50 = 52300 nM), and it had almost no affinity for beta and mACh receptors. Mafoprazine significantly increased dopamine metabolites in the corpus striatum and nucleus accumbens, although to lesser extents as compared with azaperone and chlorpromazine. These results suggest that mafoprazine probably manifests its antipsychotic action mainly through D2 receptor blocking activity and alpha-adrenergic activity (alpha 1 receptor blocking activity and alpha 2 receptor stimulating activity).