Pistagremic acid,a glucosidase inhibitor from Pistacia integerrima

Pistacia integerrima Stewart in traditionally used as folk remedy for various pathological conditions including diabetes. In order to identify the bioactive compound responsible for its folk use in diabetes, a phytochemical and biological study was conducted. Pistagremic acid (PA) was isolated from the dried galls extract of P. integerrima. Strong α-glucosidase inhibitory potential of PA was predicted using its molecular docking simulations against yeast α-glucosidase as a therapeutic target. Significant experimental α-glucosidase inhibitory activity of PA confirmed the computational predictions. PA showed potent enzyme inhibitory activity both against yeast (IC₅₀: 89.12 ± 0.12 μM) and rat intestinal (IC₅₀: 62.47 ± 0.09 μM) α-glucosidases. Interestingly, acarbose was found to be more than 12 times more potent an inhibitor against mammalian (rat intestinal) enzyme (having IC₅₀ value 62.47 ± 0.09 μM), as compared to the microbial (yeast) enzyme (with IC₅₀ value 780.21 μM). Molecular binding mode was explored via molecular docking simulations, which revealed hydrogen bonding interactions between PA and important amino acid residues (Asp60, Arg69 and Asp 70 (3.11 Å)), surrounding the catalytic site of the α-glucosidase. These interactions could be mainly responsible for their role in potent inhibitory activity of PA. PA has a strong potential to be further investigated as a new lead compound for better management of diabetes.     

Antioxidant, icthyotoxicity and brine shrimp lethality tests of Magonia glabrata

The ethanolic extract of the fruit bark from Magonia glabrata yielded shikimic acid, scopoletin, sitosterol glycoside and 2-O-methyl-l-inositol. Antioxidant, icthyotoxicity and brine shrimp lethality activities were observed in this extract. The major constituent, 2-O-methyl-l-inositol, was found to be inactive in two assays but showed moderate activity as a radical scavenger.     

Tyrosinase inhibition constituents from the roots of Morus australis

The phytochemical profiles of Morus australis roots, stems and twigs were firstly compared by HPLC analysis. It was found that Morus australis stem extract mainly contained one known tyrosinase inhibitor, oxyresveratrol, while its root and twig extract might contain some unknown potential tyrosinase inhibitors. The root extract of Morus australis was further investigated in this study. One new compound, austraone A, together with 21 known compounds, was isolated and their structures were identified by interpretation of MS and NMR data. In the tyrosinase inhibitory testing, some of them, such as oxyresveratrol, moracenin D, sanggenon T, and kuwanon O, exhibited stronger tyrosinase inhibitory activities than that of kojic acid. These results suggested the Morus australis root extract as a good source of natural tyrosinase inhibitors with a great potential to be used in foods as anti-browning agents and in cosmetics as skin-whitening agents.     

Evaluation of Pluchea carolinensis extracts as antioxidants by the epinephrine oxidation method

Many methods have been used to evaluate synthetic and natural products as hydroxyl radical scavengers. In this study a spectrophotometric method to evaluate the scavenger activity of the hydroxyl radical produced in Fenton reaction is proposed. The oxidation of l-epinephrine to adrenochrome permitted the detection of the hydroxyl radical by spectrophotometry and its possible scavenging by hydroquinone, a well known antioxidant. The method was used to evaluate the antioxidant activity of Pluchea carolinensis leaves.     

Sorocein I, a new Diels-Alder type adduct from Sorocea ilicifolia

From ethyl acetate extract of the root bark of Sorocea ilicifolia a new ketalized Diels-Alder type adduct, sorocein I (1), was isolated.     

Extraction and characterization of volatile compounds in Maytenus ilicifolia, using high-pressure CO2

This work is focused on the chemical characterization of Maytenus ilicifolia extracts obtained from high-pressure CO2 extraction. The experiments were performed in a laboratory-scale unit, where the effect of particle size (35-200 mesh), CO2 mass flow rate (1-3 g/min), temperature (293-323 K), pressure (100-250 bar), and extraction time was investigated in terms of liquid yield and chemical composition of the extracts. Results show that the particle size and CO2 mass flow rate did not affect the liquid yield, whereas the extraction temperature and solvent density exerted a pronounced effect on both liquid yield and chemical distribution of volatile compounds. The extracts were chemically analyzed with regard to phytol, squalene, vitamin E, stigmasterol, friedelan-3-ol, friedelin, dodecanoic acid and geranyl acetate in a GC/MSD.     

Wireworm damage reduction in potatoes with an attract-and-kill strategy using <Emphasis Type="Italic">Metarhizium brunneum</Emphasis>

Innovative wireworm control strategies are required to implement integrated pest management on the basis of the (EC) No regulation 1107/2009 and Directive 2009/128/EC. Entomopathogenic fungi, such as Metarhizium brunneum (Metschnikoff) Sorokin, are potential biological control agents for wireworm control but do not achieve high control efficacies in the field when applied as a conidia suspension. In a 2-year study, wireworm control with a novel attract-and-kill strategy aimed at enhancing M. brunneum efficacies in organic potato production systems in Lower Saxony, Germany. The approach is based on the attraction of wireworms (Agriotes spp. Eschscholtz) towards an artificial carbon dioxide-emitting source, using baker’s yeast (Saccharomyces cerevisiae Meyen ex Hansen) in combination with M. brunneum conidia for wireworm infection. Both components were encapsulated in alginate as a carrier material and applied in a mixture with two types of beads (one for encapsulated yeast and one for M.brunneum conidia). An application of these beads within the potato rows during potato planting reduced wireworm tuber damage by 37–75% relative to the untreated control and was able to enhance the efficacy of M. brunneum by up to 35% through an attract-and-kill approach compared to beads without a carbon dioxide source only. This strategy offers a high potential to promote biological wireworm control as an alternative to insecticide use by potentially reducing the inoculum compared to an inundate M. brunneum conidia release strategy.     

Lignans from the heartwood of Streblus asper and their inhibiting activities to hepatitis B virus

Three new lignans, erythro-strebluslignanol (1), threo-7'-methoxyl strebluslignanol (2) and erythro-7'-methoxyl strebluslignanol (3), together with twelve known compounds were isolated from the n-butanol and chloroform fractions of the heartwood of Streblus asper. Their structures were elucidated through extensive spectroscopic methods, including MS and 2D NMR experiments (HMQC and HMBC). The stereochemistry at the chiral center was determined using CD spectra, as well as analysis of coupling constants and optical rotation data, respectively. Primary bioassays showed that 6-hydroxyl-7-methoxyl-coumarin (5) and ursolic acid (10) showed anti-HBV activities, with IC(50) values of 29.60 μM and 89.91 μM for HBsAg at no cytotoxicity, and IC(50) values of 46.41 μM and 97.61 μM for HBeAg at no cytotoxicity, respectively.     

Chemical constituents of Anacolosa pervilleana and their antiviral activities

In an effort to identify novel inhibitors of Chikungunya (CHIKV) and Dengue (DENV) virus replication, a systematic study with 820 ethyl acetate extracts of Madagascan plants was performed in a virus-cell-based assay for CHIKV and a DENV NS5 RNA-dependant RNA polymerase (RdRp) assay. The extract obtained from the leaves of Anacolosa pervilleana was selected for its significant activity in both assays. One new (E)-tridec-2-en-4-ynedioic acid named anacolosine (1), together with three known acetylenic acids, the octadeca-9,11,13-triynoic acid (2), (13E)-octadec-13-en-9,11-diynoic acid (3), (13E)-octadec-13-en-11-ynoic acid (4), two terpenoids, lupenone (5) and β-amyrone (6), and one cyanogenic glycoside, (S)-sambunigrin (7) were isolated. Their structures were elucidated by comprehensive analyses of NMR spectroscopy and mass spectrometry data. The inhibitory potency of these compounds was evaluated on CHIKV, DENV RdRp and West-Nile polymerase virus (WNV RdRp). Both terpenoids showed a moderate activity against CHIKV (EC(50) 77 and 86 μM, respectively) and the acetylenic acids produced IC(50) values around 3 μM in the DENV RdRp assay.     

Micropropagation of Leptadenia pyrotechnica (Forsk.) Decne: A Multipurpose Plant of an Arid Environment

Leptadenia pyrotechnica (Forsk.) Decne belongs to the family Asclepiadaceae. It is commonly known as Kheemp in India. L. pyrotechnica is an important component of an arid ecosystem and source of fiber, forage, and medicines. We report here in vitro propagation protocol of L. pyrotechnica. Cotyledonary nodes of in vitro raised seedlings were used as an explant for multiplication of shoots. Shoots were multiplied on Modified Murashige and Skoog's (MMS) medium containing 1.33 μM BAP and additives (50 mg L^?1 ascorbic acid and 25 mg L^?1 each of citric acid, arginine, and adenine). Cultures were maintained at 30 ± 2°C temperature, 50–60 μmol m^?2 s^?1 SFP, 12 hr day^?1 photoperiod, and 60% relative humidity (RH). In vitro multiplied shoots were rooted in vitro on half-strength MS medium containing 2.46 μM IBA and 100 mg L^?1 activated charcoal. Shoots were rooted ex vitro using 2460 μM IBA pretreatment for 15 min. Plantlets were hardened in a greenhouse, and survived on a mixture of sand, garden soil, and organic manure in 3:1:1 ratio in polybags in natural habitats.     

Free radical scavenging activity of three Equisetum species from Fruska gora mountain

The scavenger activities of Equisetum arvense, Equisetum ramosissimum and Equisetum telmateia aboveground parts phosphate buffer (pH 7) extracts were evaluated using three different methods: DPPH assay, ESR and NO radical inhibition assay. Total reducing power was determined by FRAP assay. The E. telmateia extract demonstrated the most relevant scavenger and antioxidant properties. ESR signal of DMPO-OH radical adducts in the presence of E. telmateia phosphate buffer (pH 7) extract was reduced to 98.9% which indicated that E. telmateia could be a useful source of antioxidants with huge scavenger ability.     

Anti-hyperglycemic action of apigenin-6-C-β-fucopyranoside from Averrhoa carambola

A stimulatory effect of apigenin-6-C-β-fucopyranoside (1) on glucose uptake was observed when rat soleus muscle was incubated with 1, 10 and 100μM of this flavonoid glycoside. The presence of specific insulin signaling inhibitors, such as wortmannin, an inhibitor of phosphoinositide 3-kinase (PI3K), RO318220, an inhibitor of protein kinase C (PKC), PD98059, an inhibitor of mitogen-activated protein kinase (MEK), and HNMPA(AM)(3), an insulin receptor tyrosine kinase activity inhibitor showed that apigenin-6-C-β-fucopyranoside triggers different metabolic pathways in skeletal muscle. The oral administration of crude extract, fractions and isolated flavonoids (apigenin-6-C-β-fucopyranoside (1) and apigenin-6-C-(2″-O-α-rhamnopyranosyl)-β-fucopyranoside (2)) from Averrhoa carambola leaves exhibited a potential hypoglycemic activity in hyperglycemic normal rats. Additionally, both flavonoids significantly increased the muscle and liver glycogen content after an acute treatment. The results indicate that A. carambola can be regarded as a potent antihyperglycemic agent with insulin secretagogue and insulin mimetic properties.     

In vitro antifungal activities of longan (Dimocarpus longan Lour.) seed extract

Longan, Dimocarpus longan Lour., contains polyphenolic compounds which exhibit several pharmacological properties. This study aims to evaluate antifungal activities of longan fruit extract in comparison to its active compounds. The results showed that longan seed exhibited antifungal activity against the opportunistic yeasts (Candida species and Cryptococcus neoformans). In contrast, longan pulp and whole fruit did not demonstrate any inhibitory effects. Ellagic acid showed the most potent antifungal activity followed by corilagin and gallic acid, respectively. Ellagic acid inhibited Candida parapsilosis and C. neoformans more effectively than Candida krusei and also some Candida albicans clinical strains. Baidam cultivar possessed higher antifungal activity (MIC=500-4000 μg/ml) as it contained higher contents of ellagic acid and gallic acid than Edor (MIC=1000-8000 μg/ml). For antibacterial activity, only corilagin and gallic acid possessed weak to moderate inhibitory effects against Staphylococcus aureus and Streptococcus mutans, respectively. Longan seed was then applied in the oral care products. Longan effervescent granule (5% extract) significantly reduced adhesion of C. albicans to acrylic strips. Mouthwash containing 0.5% extract exhibited good antifungal activity compared to a commercial product. These findings indicated that longan seed extract and its polyphenolic compounds can be used as an antifungal agent in oral care products for the treatment of opportunistic yeast infection.     

Red pine harvest debris as a potential source of inoculum of Diplodia shoot blight pathogens

A high incidence of Diplodia shoot blight (site means ranging 85-100%) was observed on recently planted red pine (Pinus resinosa) seedlings where mature red pine stands previously had been clearcut. An investigation of the potential of harvest debris as a source of inoculum of Diplodia pathogens then was conducted. Cones, bark, needles, stems from shoots bearing needles, and stems from shoots not bearing needles (both suspended above the soil and in soil contact) were collected from harvest debris left at sites where clearcutting occurred. Conidia were quantified, and their germination rate was assessed, and Diplodia species were identified using PCR. Conidia of Diplodia species were found at all study sites and conidia counts increased from samples collected from 6 to 18 months after harvest. Germinable conidia were obtained from debris collected 6 months to 5 years after harvest. Fewer conidia were obtained from debris collected at intervals of up to 4-5 years after harvest and the percentage of germinable conidia was lower after longer intervals following harvest. More conidia were obtained and a greater percentage germinated from debris collected above the soil than from debris in soil contact. The host substrate also influenced the number of conidia and the percentage that germinated. Planting red pine seedlings next to debris infested with Diplodia pathogens could provide a persistent source of inoculum. Results should prompt further consideration by land managers and researchers of the potential forest health risks, in addition to benefits, that may be associated with harvest debris.     

Pinostrobin from Cajanus cajan (L.) Millsp. inhibits sodium channel-activated depolarization of mouse brain synaptoneurosomes

This investigation focuses on the in vitro neuroactive properties of pinostrobin, a substituted flavanone from Cajanus cajan (L.) Millsp. of the Fabaceae family. We demonstrate that pinostrobin inhibits voltage-gated sodium channels of mammalian brain (IC₅₀ = 23 µM) based on the ability of this substance to suppress the depolarizing effects of the sodium channel-selective activator veratridine in a synaptoneurosomal preparation from mouse brain. The resting membrane potential of synaptoneurosomes was unaffected by pinostrobin. The pharmacological profile of pinostrobin resembles that of depressant drugs that block sodium channels.     

Cytotoxic triterpene saponins from the leaves of Aralia elata

Phytochemical investigation of the leaves of Aralia elata has led to the isolation of four new compounds, 3-O-β-D-glucopyranosyl (1→3)-β-D-glucopyranosyl (1→3)-β-D-glucopyranosyl oleanolic acid (1), 3-O-[β-D-glucopyranosyl (1→3)-β-D-glucopyranosyl (1→3)]-[β-D-glucopyranosyl (1→2)]-β-d-glucopyranosyl hederagenin 28-O-β-D-glucopyranoside (2), 3-O-{[β-D-glucopyranosyl (1→2)]-[β-d-glucopyranosyl (1→3)-β-d-glucopyranosyl (1→3)]-β-D-glucopyranosyl} oleanolic acid 28-O-β-D-glucopyranosyl ester (3) and 3-O-[β-D-glucopyranosyl (1→2)]-[β-D-glucopyranosyl (1→3)]-β-d-glucopyranosyl caulophyllogenin (4) and two known compounds, 3-O-[β-D-glucopyranosyl (1→3)-α-l-arabinopyranosyl]-echinocystic acid (5) and 3-O-α-L-arabinopyranosyl echinocystic acid (6). The structural determination was accomplished with spectroscopic analysis, in particular (13)C-NMR, 2D-NMR and HR-ESI-MS techniques. Compounds 1-6 were tested for their inhibition of the growth of HL60, A549 and DU145 cancer cells. Compound 1 showed significant cytotoxic activity against HL60 and A549 cancer cells with IC(50) values of 6.99μM and 7.93μM respectively. In addition, compounds 5 and 6 showed significant cytotoxic activity against HL60 cancer cells with IC(50) values of 5.75μM and 7.51μM, respectively.     

A new phenolic glycoside from Sorocea ilicifolia stem bark

A new phenolic glycoside, 3,4-dimethoxyphenyl-1-O-beta-d-apiofuranosyl (1-->2)-beta-d-glucopyranoside (1), was isolated from the acetone extract of the Sorocea ilicifolia stem bark, along with the known compounds, 3,4,5-trimethoxyphenyl-1-O-beta-apiofuranosyl (1-->6)-beta-d-glucopyranoside, benzyl-O-beta-d-apiofuranosyl (1-->2)-beta-d-glucopyranoside, sorocein A, mulberrofuran K, kuwanon J, sorocein B, chalcomoracin, and kuwanol E.     

Ganoderic acid Df,a new triterpenoid with aldose reductase inhibitory activity from the fruiting body of Ganoderma lucidum

Ganoderic acid Df, a new lanostane-type triterpenoid, was isolated from the fruiting body of Ganoderma lucidum. Its structure was characterized as 7β, 11β-dihydroxy-3, 15, 23-trioxo-5α-lanosta-8-en-26-oic acid by 1D- and 2D-NMR spectra. This compound exhibited potent human aldose reductase inhibitory activity, with an IC₅₀ of 22.8 μM in vitro. A carboxyl group of this compound's side chain is essential for eliciting inhibitory activity because its methyl ester is much less active.     

Modeling heliotropic tree growth in hardwood tree species—A case study on Maesopsis eminii

There are many impacts during a tree's life that affect bole development. In Maesopsis eminii, a high-potential timber species in Uganda, studies have shown that the occurrence of strongly bent boles is the overwhelming reason that boles fail quality criteria. This observation is incongruous with the tree architecture model of Roux, which describes M. eminii as a tree with a strong apical dominance, meaning that it has a strong genetically based preference for vertical growth of the terminal sprout relative to side branches. As external causes for bent boles could be excluded, we demonstrate in this study the proof of heliotropic growth, i.e. an active bending towards light, for M. eminii beyond the sapling stage. We develop a model used to describe the effects of competition on bole quality using bole form parameters and basic information about the neighbouring trees, and without having to incorporate crown parameters. By means of calculated bole parameters and a mathematical equation to calculate the intensity and direction of competition, we prove the existence of a heliotropic growth reaction. However, we are not able to predict the intensity of this reaction. Finally, general silvicultural recommendations are discussed for tree species with strong heliotropic growth.