A New Phenolic Glycoside and a New Trans-clerodane Diterpene from Conyza Blinii

Abstract

A new phenolic glycoside, 4-propionyl-2,6-dimethoxyphenyl β-D-glucopyranoside (1) and a new trans-clerodane diterpene named 19-deacetylconyzalactone (2), were isolated from the aerial parts of Conyza blinii.     

Stilbenoids from Stemona japonica

Three new dihydrostilbenes, stilbostemins J–L (1–3), and a new dihydrophenanthrene, stemanthrene F (4), were isolated from the roots of Stemona japonica together with two known bibenzyls, 3,5-dihydroxy-4-methylbibenzyl (5) and 3,5-dihydroxy-2′-methoxy-4-methylbibenzyl (6). Their structures were elucidated by spectroscopic analyses. Compounds 3–6 exhibited strong antibacterial activities against Staphylococcus aureus and Staphylococcus epidermidis.     

Structures of Two New Benzofuran Derivatives from the Bark of Mulberry Tree (Morus Macroura Miq.)

Abstract

Two new benzofuran derivatives, macrourins A (1) and B (2), together with two known stilbene derivatives, were isolated from the barks of Morus macroura Miq. Their structures were elucidated by means of spectroscopic evidence.     

Three New Triterpenoids from Fuscoporia Obliqua

Abstract

Three new lanostane triterpenoids, fuscoporianol A (1), B (2), and C (3) were isolated from the petroleum ether extracts of Fuscoporia obliqua and their structures have been determined on the basis of chemical, spectroscopic methods and X-ray crystallographic analysis as 25-methoxy-21, 22-cyclolanosta-8-ene-3β, 21α-diol (1), 3β, 22α-dihydroxy-lanosta-8, 23E-diene-25-peroxide (2), 3β, 22α, 25-trihydroxy-lanosta-8, 23E-diene (3).     

Five New Norditerpenoid Alkaloids from Aconitum Sinomontanum

Abstract

From the roots of Aconitum sinomontanum, five new norditerpenoid alkaloids, sinomontanitines A (1) and B (2), sinomontanines A (3), B (4) and C (5), were isolated together with the known alkaloids lappaconitine (6) and ranaconitine (7), The structures of the new alkaloids were determined by spectral analysis.     

Do animal models hold value in Autism spectrum disorder (ASD) drug discovery?

ABSTRACT

Introduction: Autism spectrum disorder (ASD) defines impairments in a broad range of behaviors in two domains, social communication and repetitive behaviors and/or restricted interests. Drug discovery is ongoing for ASD, but no drugs have been approved for the core behaviors. Animal models are invaluable for drug discovery, but are limited by the face, construct, and predictive validity for ASD. The genetic construct validity of animal models has provided potential targets including biological events early in development which are indeed challenging to treat pharmacologically.

Areas covered: The focus of this review is on the current models for ASD being used to test potential therapeutics. Drugs reviewed include sulforaphane, propranolol, oxytocin, vasopressin antagonists, arbaclofen, and bumetanide, that have been evaluated on behaviors with face validity for both the core behaviors of ASD, social and repetitive behaviors, and the modifying behaviors including learning and memory.

Expert opinion: Animal models for the core symptoms of ASD have suffered from the same problems hampering research in humans, including lack of a biomarker, heterogeneity of symptom severity, and appropriate endpoints for evaluation. Despite this, the data from animal models has allowed several drugs to move on to clinical testing.     

Patient-reported treatment satisfaction with rivaroxaban in Japanese non-valvular atrial fibrillation patients: an observational study

Objectives: Rivaroxaban has previously been shown to be as efficacious and safe as warfarin for the prevention of stroke in non-valvular atrial fibrillation (NVAF). Therefore, treatment satisfaction becomes an important consideration. Here we examine treatment satisfaction in Japanese NVAF patients who were switched from warfarin to rivaroxaban.

Methods: Patient-reported outcome (PRO) data were collected as part of a prospective, multi-center, post-marketing surveillance (PMS) of a direct oral-anticoagulant, rivaroxaban, in Japan. The Anti-Clot Treatment Scale (ACTS) and the Treatment Satisfaction Questionnaire for Medication version II (TSQM-II) were collected at baseline, month 3, and month 6. Change in scores from baseline to month 3 and month 6 were assessed. Exploratory analyses included change in scores by patient characteristics. Safety and effectiveness of rivaroxaban were also assessed.

Results: ACTS Burdens scores significantly improved at month 3 (54.6?±?6.3) and month 6 (54.5?±?6.5) compared to baseline (51.0?±?7.6) (p?<?.001). ACTS Benefits score remained stable over time (baseline?=?10.1?±?2.8, month 3?=?10.2?±?3.1, month 6?=?10.1?±?3.1). Mean TSQM-II sub-scale scores significantly improved at month 3 and month 6 compared to baseline for all four domains (all p?<?.001).

Conclusions: Findings suggest treatment satisfaction may improve in Japanese NVAF patients after a switch from warfarin to rivaroxaban. Higher treatment satisfaction may translate into improved treatment adherence, which is critical for the long-term prevention of stroke.     

The effects of lutein on cisplatin-induced retinal injury: an experimental study

Aim: Lutein is one of the most common carotenoids defined in human plasma as having potent anti-oxidant effects. We aimed to determine the biochemical and histopathological effects of lutein on cisplatin-induced oxidative retinal injury in rats.

Materials and methods: Twenty-four rats were equally divided into four groups as healthy controls (HC group), only cisplatin (5?mg/kg) administered group (CIS group), Lutein (0.5?mg/kg)?+?cisplatin (5?mg/kg) administered group (LC group), and only Lutein (0.5?mg/kg) (LUT group) administered group. From the blood samples obtained, serum malondialdehyde (MDA), total glutathione (tGSH), interleukin 1 beta (IL-1β), and tumor necrosis factor alpha (TNF-α) levels were investigated. In histopathological analyses, the total retinal thickness, retinal pigment epithelium (RPE), photoreceptor layer (PL), outer nuclear layer (ONL), outer plexiform layer (OPL), inner nuclear layer (INL), inner plexiform layer (IPL), and ganglion cell layer (GCL) were evaluated.

Results: MDA, IL-1β, and TNF-a levels were statistically significantly higher (p?p?Conclusions: Lutein co-administration was highly effective in prevention of cisplatin-induced retinal damage due to the anti-oxidant and anti-inflammatory effects of lutein.     

Chemical Composition and Antinociceptive Properties of Hyeronima alchorneoides. Leaves

Abstract

In the current study, we investigated the analgesic activity of a crude methanol extract and some fractions obtained from Hyeronima alchorneoides Allemao leaves and analyzed its phytochemical profile to determine active principles. All the fractions exhibited analgesic properties using the writhing test in mice, but the hexane fraction was the most active, causing 96.4 ± 1.0% inhibition at 10 mg/kg. Three compounds were isolated and identified based on their spectral data: simiarenol (1), β.-sitosterol (2), and amentoflavone (3). Compound 1, a rare terpene isolated for the first time from the family Euphorbiaceae, presented a calculated ID₅₀ value of 18.87 (14.6–24.4)µmol/kg with the writhing test, being about 8-fold more active than two known analgesic and anti-inflammatory drugs (aspirin and dipyrone). In the formalin test, it was particularly active against the second phase, with inhibition of 59.5 ± 9%, suggesting a peripheral activity. In the capsaicin and glutamate tests, it showed inhibition of 52.3 ± 4 and 52.1 ± 6%, respectively.     

A Graph-Theoretical Approach to the Prediction of Physical Properties of Alkanes Based on the Distance Matrix

A new topological index, the largest eigenvalue of the distance matrix (DI), is presented as a measure of molecular branching. The DI and Balaban's J index are used to predict the densities of a series of alkanes. The statistical correlations obtained are excellent and give a correlation coefficient of 0.961.     

Triterpenoid Saponin from Primula Elatior Subsp. Meyeri

Abstract

A new triterpenoid saponin, protoprimuloside B (2), has been isolated from the roots of Primula elatior subsp. meyeri and its structure deduced as 3β-O-{[α-L-rhamnopyranosyl-(1–2)-β-D-galactopyranosyl-(1–3)]-[β-D-glucopyranosyl-(1–2)]-β-D-glucopyranosyl}-protoprimuloside B by means of spectral data, especially NMR (400 MHz), including ¹H, ¹³C, DEPT, COSY, HMBC, HMQC, NOESY techniques and (+)FAB-MS spectrum.     

Activity of Alkaloid Extract of Carica papaya. Seeds on Reproductive Functions in Male Wistar Rats

ABSTRACT

Activity of the alkaloid extract of Carica papaya. Linn seed on male reproductive physiology was investigated. Male rats were divided into two groups. Each group of 20 male rats was further divided into 4 subgroups of 5 rats. Each rat was treated with C. papaya. seed extract (10, 50, and 150 mg kg^?1day^?1) daily for 3 days for fecundity study, semen analysis, and testis histopathology, respectively. Twenty male rats treated with C. papaya. seed extract (10, 50, and 150 mg kg^?1 day^?1), abstained from sex for 7 days and divided into 4 groups, were mated with fertile female rats: another set of 30 male rats, divided into 4 groups, treated with the seed extract (10, 50, and 150 mg kg^?1 day^?1), respectively, was used for semen analysis and testis histopathology. The results showed that oral administration of C. papaya. seed extract prevented ovum fertilization, reduced sperm cell counts, revealed sperm cell degeneration, and induced testicular cell lesion. These observations led to the conclusion that C. papaya. seed extract oral administration could induce reversible male infertility and therefore could be used for pharmaceutical development of a male contraceptive.     

The effect of nicotine and cytisine on3H-acetylcholine release from cortical slices of guinea-pig brain

Summary Nicotine 1.8×10^–5–1.8×10^–4 mol/l enhanced the spontaneous³H-efflux from guinea-pig cortical slices preloaded with³H-choline and perfused in the presence of hemicholinium (HC-3).The facilitation of tritium outflow was prevented by tetrodotoxin 5×10^–7 mol/l and byd-tubocurarine 4.5×10^–6 mol/l. Nicotine 1.8×10^–6–1.8×10^–4 mol/l, and the agonist cytisine 5×10^–7–5×10^–5 mol/l increased, in a concentration-dependent way,³H-efflux from electrically-stimulated slices (0.2 Hz). The concentration-response curves of both drugs were parallelly shifted to the right byd-tubocurarine 4.5×10^–6 mol/l. The EC₅₀ values (i.e. the concentrations required to cause a 50% increase in the S₂/S₁ ratio) changed for nicotine from 5.58×10^–5 to 4.34×10^–4 and for cytisine from 6.3×10^–6 to 2.75×10^–4 mol/l in the absence and in the presence of the antagonist, respectively.In the range of 0.2–2 Hz the magnitude of the effect of nicotine was inversely related to the rate of stimulation.The response to nicotine was subject to rapidly developing tachyphylaxis; it was resistant to atropine.It is concluded that nicotine and cytisine facilitate³H-efflux from the cholinergic nerve endings of guinea-pig cerebral cortex. This effect involves sodium-dependent mechanisms and is due to an interaction of the drugs with receptors showing affinity ford-tubocurarine.     

Glabcensin Q-U,Five New ent-Kaurane Diterpenoids from Isodon angustifolius Var. Glabrescens

Abstract

Examination of the diterpenoid constituents of the dried leaves of Isodon angustifolius var. glabrescens led to the isolation of five new ent-kaurane diterpenoids, named as glabcensin Q-U (2–6). The structures were elucidated on the basis of spectroscopic evidences.     

A Simple Method for Isolation of Plumbagin from Roots of Plumbago rosea.

Abstract

Plumbagin, the major active compound and a potential biomarker characteristically found to be present in different Plumbaginales, is isolated by an austere and efficient method involving column chromatography. A literature survey suggests that the roots of Plumbago rosea. Linn. are the richest source of plumbagin. Chemically identified as a naphthoquinone, the compound is claimed to sublime at 90°C. This disposition of the compound correlates with the implication of cold maceration employed in isolation methodology for extraction of root powder with acetone. Plumbagin, being hydrophobic and insoluble in water, was precipitated out by addition of water to the acetone extract. The filtered residue was taken in chloroform, and the concentrated chloroform extract, when subjected to column chromatography, yielded plumbagin (1.65%), elution being carried out with n-hexane:ethyl acetate (92:8). The identity of the compound was confirmed by melting point data, UV, IR, and mass spectral data reported in the literature. The purity of the compound was further analyzed by subjecting the compound to HPTLC studies.     

A new sesquiterpene and other terpenoid constituents of Chisocheton penduliflorus

A new aromadendrane sesquiterpene, allo-aromadendrane-10α, 14-diol (3), was isolated from Chisocheton penduliflorus (Meliaceae), along with two known sesquiterpenes: allo-aromadendrane-10β, 14-diol (2) and allo-aromadendrane-10β, 13, 14-triol (7). Six dammarane triterpenoids, including cabraleadiol (1), eichlerialactone (4), cabraleahydroxylactone (5), cabralealactone (6), hollongdione (8) and dammaradienone (9), the coumarins scoparone and scopoletin, and vanillic acid were also isolated from the wood and leaves of this plant. Compounds 1–7 displayed antimycobacterial activity against Mycobacterium tuberculosis. Compounds 1, 4, 5 and 6 were weakly cytotoxic to a breast cancer (BC) cell line; whereas, compound 6 was moderately active against a small-cell lung cancer (NCI-H187) cell line.     

Comparison of Microwave-Assisted Hydrodistillation and Hydrodistillation Methods for the Analysis of Volatile Secondary Metabolites

Abstract

Microwave-assisted hydrodistillation (MWHD) and hydrodistillation (HD) were carried out for the analysis of volatile components in whole and ground fruits of Anethum graveolens. L. (dill seed) and Coriandrum sativum. L. (coriander seed). Fruits were distilled using a microwave oven modified to fit a Clevenger apparatus. The effect of microwave energy on the yield and composition of the essential oil was investigated against the classical hydrodistillation. Essential oils of all samples were analyzed by GC-FID and gas chromatography-mass spectrometry (GC-MS). In the whole dillseed oil, the amounts of cis.-isodihydrocarvone (from 7.5% to 10.9%) and carvone (from 45.7% to 69.3%) were increased by microwave energy while limonene (from 17.7% to 4.7%), myristicin (from 8.7% to 5.7%) and dill apiole (from 14.1% to 6.1%) were decreased. Grinding of the material also increased the amounts of main components except for myristicin and dill apiole. A decrease in the linalool content of the coriander oil (from 80.0% to 75.5%) was observed in the microwave-assisted hydrodistilled ground fruits. Microwave-assisted distillation appeared to increase the amounts of fatty acids, for example, tetradecanoic acid (from 2.8% to 8.8%) and hexadecanoic acid (from 1.9% to 6.0%) in coriander oil.     

A new <Emphasis Type="Italic">Erythrina</Emphasis> alkaloid from <Emphasis Type="Italic">Erythrina herbacea</Emphasis>

A new Erythrina alkaloid, 10-hydroxy-11-oxoerysotrine (1), has been isolated from the flowers of Erythrina herbacea together with five known compounds: erytharbine (2), 10,11-dioxoerysotrine (3), erythrartine (4), erysotramidine (5) and erysotrine-N-oxide (6). The structure of the new compound was elucidated on the basis of its spectral data, including 2-D NMR and mass (MS) spectra. The new compound is a rare C-10 oxygenated Erythrina alkaloid. The antioxidant activities of the isolated compounds 1–6 were evaluated by scavenging with peroxynitrite.     

Aromatic monoterpenoid glycosides from the seeds of Paeonia ostii

Phytochemical investigation into the seeds of Paeonia ostii T. Hong et J. X. Zhang (Paeoniaceae) led to the identification of three new aromatic monoterpenoid glycosides, named paeostisides A–C (1–3), along with one known compound. Their structures were identified by spectroscopic analysis and chemical method.     

A New Sesquiterpene Lactone Glucoside from Ixeris Sonchifolia

Abstract

A new sesquiterpene lactone glucoside, Ixerin Z₁ (1), was isolated from the whole plants of Ixeris sonchifolia (Bge.) Hance, along with 15 known compounds. The structure of 1 was elucidated as 1(10),3,11(13)-guaiatriene-12,6-olide-2- one-3-O-[6′-(p-hydroxyphenylaceryl)]-gluco-pyranoside by spectroscopic methods including 2D-NMR techniques.