A New Coumarin from the Stems of Pterocarpus indicus.

The chemical investigation of the crude ethyl acetate extract from Pterocarpus indicus stems led to isolation of a new coumarin, indicusane (1), together with eleven known compounds (2-12). To the best of our knowledge, all isolated coumarins (1-12) are reported for the first time from this plant. Their structures were identified on the basic of spectroscopic data (NMR, MS and ECD) as well as a chemical reaction (Mosher's method).

Extracted Anaxagorea luzonensis A. Gray Restored Impairment of Endothelium-Dependent Vasorelaxation Induced by Homocysteine Thiolactone in Rat Aortic Rings.

Objective: To investigate the beneficial effects of Anaxagorea luzonensis (AL) extract on homocysteine thiolactone (HTL)-induced impairment of endothelium-dependent relaxation in rat aortic rings. The mechanisms involved in the effects of AL on endothelial dysfunctions by HTL are also examined.

Material And Method: Aortic rings from male Wistar rats were co-incubated for 90 minutes with L-arginine (3 mM), a precursor of nitric oxide (NO); superoxide dismutase (SOD, 200 U/mL), a scavenger of superoxide anion; indomethacin (10 µM), a cyclooxygenase (COX) inhibitor; SC560 (10 µM), a COX-1 inhibitor; NS398 (10 µM), a COX-2 inhibitor; or SQ29548 (1 µM), a thromboxane A₂ receptor antagonist in the presence of HTL (1 mM).

Furoquinoline Alkaloids from the Leaves of Evodia lepta as Potential Cholinesterase Inhibitors and their Molecular Docking.

Nine furoquinoline alkaloids (1-9) were isolated from the leaves of Evodia lepta based on bioassay-guided fractionation and chromatographic techniques. All isolates were evaluated for their cholinesterase (ChEs) inhibitory activities, in which kokusaginine (7) and melineurine (5) exhibited the highest activity toward AChE and BChE, respectively. Lineweaver-Burk plots indicated that 5 and 7 were mixed mode inhibitors of both ChE enzymes.

Phosphodiesterase inhibitory activity of the flavonoids and xanthones from Anaxagorea luzonensis.

Five flavonoids, one isoflavone and five xanthones were isolated from Anaxagorea luzonensis. Of these eleven isolated compounds, 1,3,5-trihydroxy-4-prenylxanthone (3) was a relatively potent inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 3.0 μM.

Novel cucurbitane triterpenoids and anti-cholinesterase activities of constituents from Momordica charantia L.

The C-19 epimers of 5beta,19-epoxycucurbita-6,23(E),25(26)-triene-3f,19-diol (1) and 5/,19-epoxy-25-methoxycucurbita-6,23-diene-3beta,19-diol (2) along with (19R,23E)-5beta,19-epoxy-19-methoxycucurbita-6,23,25-trien-3beta-ol (3), (23E)-5beta,19-epoxycucurbita-6,23-diene-3beta,25-diol (4), ligballinol (5), charantin (6) and momordicoside K(7) were isolated from the green fruits of Momordica charantia. The (S)-epimers of 1 and 2 are the first reports in nature. The acetyl- and butyryl-cholinesterase inhibitory activities of the isolated compounds were evaluated, and 5 showed the highest activity of these compounds against butyrylcholinesterase (IC50 = 32.

A 5,7-dimethoxyflavone/hydroxypropyl-β-cyclodextrin inclusion complex with anti-butyrylcholinesterase activity.

This study aimed to improve the water solubility of 5,7-dimethoxyflavone (5,7-DMF) isolated from Kaempferia parviflora by complexation with 2-hydroxypropyl-β-cyclodextrin (HPβ-CD). The phase solubility profile of 5,7-DMF in the presence of HPβ-CD was classified as AL-type and indicated a 1:1 mole ratio. Differential scanning colorimetry, X-ray diffraction, NMR and SEM analyses supported the formation of a 5,7-DMF/HPβ-CD inclusion complex involving the A ring of 5,7-DMF inside the HPβ-CD cavity.

New furoquinoline alkaloids from the leaves of Evodia lepta.

Three new furoquinoline alkaloids, leptanoines A-C (1-3) along with three known compounds (4-6) were isolated from the leaves of Evodia lepta. Their structures were identified by interpretation of their spectroscopic data as well as comparison with those reported in the literature. In addition, all isolated compounds were evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities.

Potent and selective butyrylcholinesterase inhibitors from Ficus foveolata.

Four stilbenes (1-4), one inseparable mixture of two alkyl diferulates (5a, 5b), one alkyl ferulate (6) and four flavonoids (7-10) were isolated from Ficus foveolata Wall. Except for quercetin (10), the other ten constituents were isolated from F. foveolata for the first time.

Kaempferia parviflora, a plant used in traditional medicine to enhance sexual performance contains large amounts of low affinity PDE5 inhibitors.

Aim Of The Study: A number of medicinal plants are used in traditional medicine to treat erectile dysfunction. Since cyclic nucleotide PDEs inhibitors underlie several current treatments for this condition, we sought to show whether these plants might contain substantial amounts of PDE5 inhibitors.

Materials And Methods: Forty one plant extracts and eight 7-methoxyflavones from Kaempferia parviflora Wall.

Acetyl- and butyryl-cholinesterase inhibitory activities of mansorins and mansonones.

Cholinesterase (ChE) inhibitory activities of three coumarins (mansorins A-C) and five naphthoquinones (mansonone C, E, G and H) were evaluated to determine the relationships between the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory effects and the core structures of these compounds. Among the tested compounds, mansonone E exhibited the highest ChE inhibitory activities, with IC₅₀ values in the low micromolar levels. In addition to revealing the ChE inhibitory activities of naphthoquinones for the first time, the results also revealed structure-activity relationship information that could be useful for further modification.

The ethanolic extract of Kaempferia parviflora reduces ischaemic injury in rat isolated hearts.

Aims Of The Study: The ethanolic extract of Kaempferia parviflora (KPE) has been reported to contain a range of flavonoids and to enhance endothelial synthesis of NO. We investigated the vascular relaxant, antioxidant and cardioprotective activities of KPE.

Materials And Methods: Vascular function was assessed in rat aortic rings and superoxide generation determined using lucigenin enhanced chemiluminescence.

Effects of Kaempferia parviflora Wall. Ex Baker on endothelial dysfunction in streptozotocin-induced diabetic rats.

Aim Of The Study: The aim of the present study was to investigate an ethanolic extract of Kaempferia parviflora (KPE) reduces oxidative stress and preserves endothelial function in aortae from diabetic rats.

Materials And Methods: Diabetes was induced in Sprague-Dawley rats by streptozotocin (STZ) treatment (55 mg/kg i.v.

Possible mechanisms of vasorelaxation for 5,7-dimethoxyflavone from Kaempferia parviflora in the rat aorta.

The present study investigated the vascular effects of 5,7-dimethoxyflavone (DMF), isolated from the rhizomes of Kaempferia parviflora (KP), on rat isolated aortic rings and its possible mechanisms. DMF (1-100 μM) caused concentration-dependent relaxations in aortic rings precontracted with methoxamine. This effect was significantly reduced by removal of the endothelium, and after pretreatment with N(G)-nitro-L-arginine methyl ester (L-NAME, 300 μM), indomethacin (10 μM) and 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one (ODQ, 10 μM), but not 9-(tetrahydro-2-furanyl)-9H-purine-6-amine (SQ22536, 100 μM).

Anticholinesterase activity of 7-methoxyflavones isolated from Kaempferia parviflora.

The rhizome of Kaempferia parviflora or kra-chai-dum (in Thai) is used traditionally as a folk medicine. The preliminary cholinesterase inhibitory screening of this plant extract exhibited significant acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Thirteen known methoxyflavones (1-13) were isolated and their structures were completely elucidated based on NMR analysis and compared with literature reports.

3,5,7-Trimeth-oxy-2-(4-methoxy-phen-yl)-4H-1-benzopyran-4-one.

In the title compound, C(19)H(18)O(6), also known as 3,4',5,7-tetra-methoxy-flavone, the dihedral angle between the benzopyran-4-one group and the attached benzene ring is 11.23 (8)°. An intra-molecular C-H⋯O hydrogen bond generates an S(6) ring motif.

5,7-Dimeth-oxy-2-(4-methoxy-phen-yl)-4H-1-benzopyran-4-one methanol solvate monohydrate.

In the title compound (alternatively called 4',5,7-trimethoxy-flavone methanol solvate hydrate), C(18)H(16)O(5)·CH(3)OH·H(2)O, the flavone mol-ecule is almost planar, the inter-planar angle between the planes of the benzopyran-4-one group and the attached benzene ring being 4.69 (9)°. In the crystal, the flavone mol-ecule makes inter-molecular C-H⋯O hydrogen bonds to adjacent inversion-related flavone mol-ecules, generating R(2) (2)(8) and R(2) (2)(14) rings and an infinite ribbon.