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Secondary metabolites from the genus I Metarhizium i yielded several bioactive compounds, such as metarhiziumoids A and B showed glycosidase inhibitory activity [[3]], omalvin A displayed antibacterial activity [[4]], and destruxin A exhibited phytotoxic activity [[5]]. I Metarhizium marquandii i is an endophytic fungus isolated from the Chinese medicinal plant I Sophora tonkinensis i (Leguminosae) I . i In our ongoing search for biologically active compounds from fungi [[6]-[9]], the metabolites of I M. marquandii i were investigated. At the concentration of 100 g/mL, compound B 2 b showed antifungal activity to all five fungi. Graph Compounds B 1-5 b were evaluated for their antifungal activities against five phytopathogenic fungi, I Alternaria alternaria i , I Alternaria cabbage i , I Cochliobolus miyabeanus i , I Colletotrichum capsici i , I Ceratocystis paradoxa i , using a modified version of the 2-fold serial dilutions method [[15]]. [Extracted from the article]

Hedychium flavum Roxb., a medicinal, edible, and ornamental plant, is widely cultivated throughout China, India, and Southeast Asia. The rhizome from this plant has been used for food flavoring and in traditional Chinese medicine to treat diverse diseases, but the detailed constituents and bioactivities are still limited known. Therefore, phytochemical analysis by GC-MS and UHPLC-Q-Orbitrap-MS, and antioxidant, antibacterial, cytotoxic, and enzyme inhibitory activities tests have been conducted in the current study. Based on the GC-MS results, the essential oil (EO) of rhizome was mainly composed of coronarin E (20.3%), β -pinene (16.8%), E -nerolidol (11.8%), and linalool (8.5%). Among them, coronarin E was reported in H. flavum EO firstly. Furthermore, the spectrophotometric indicated rhizome had high total phenolic content (TPC, 50.08–57.42 mg GAEs/g extract) and total flavonoid content (TFC, 12.45–21.83 mg REs/g extract), no matter in water extract (WE) or in 70% ethanol extract (EE). UHPLC-Q-Orbitrap-MS was applied to further characterize composition, and 86 compounds were putatively identified from WE and EE, including 13 phenolic components. For the bioactivities, both WE and EE showed remarkable antioxidant activity by DPPH and ABTS tests, being superior to the positive control (butylated hydroxytoluene, BTH). EO revealed significant antibacterial activity against Staphylococcus aureus , Bacillus subtilis , Pseudomonas aeruginosa , and Proteus vulgaris with DIZ (10.34–24.43 mm), MIC (78.13–312.50 μg/mL), and MBC (156.25–625.00 μg/mL). Moreover, EO exhibited a considerable selectivity to human tumor cell K562 (IC50 = 27.16 μg/mL), and its toxicity was more than 3.5-fold different from that of non-cancerous MRC-5 cell (IC50 = 95.96 μg/mL) and L929 cell (IC50 = 129.91 μg/mL). A series of apoptosis analysis demonstrated that EO induced apoptosis against K562 cells in a dose-dependent manner. In enzyme inhibitory effect assays, WE and EE showed strong α -glucosidase inhibition activity, being superior to the positive control (acarbose). Besides, the EO, WE, and EE didn't show a promising inhibition on tyrosinase (19.30–32.51 mg KAEs/g sample) and exhibited a weak inhibitory effect on cholinesterase. Based on the current results, H. flavum could be considered as a source of bioactive compounds and has high exploitation potential in the cosmetics, food, and pharmaceutical industries. [ABSTRACT FROM AUTHOR]

The essential oil from Curcumae wenyujin (CWEO) has antibacterial activity, but the antibacterial compounds in the CWEO have not been identified. The spectrum-effect relationship between chemical compositions and pharmacological activity is regarded as a potentially useful tool to screen bioactive compounds. The binary chromatographic fingerprint of CWEO was established by gas chromatography/mass spectrometry (GC-MS) and high-performance liquid chromatography/diode-array (HPLC-DAD). A data-level information integration method was used to investigate the chemical characteristics encoded in two chromatographic fingerprints. Additionally, the antibacterial activity against Escherichia coli (E. coli）was determined by the liquid dilution method. The spectrum-effect relationship between the binary chromatographic fingerprint and antibacterial activity was investigated with principal component analysis (PCA) and orthogonal projection to latent structures (OPLS) analysis. Compared with a single data matrix, the combined data matrix allowed more accurate identification of the strong outliers in the PCA. Additionally, the results of OPLS were used to establish a spectrum-effect relationship with a closer correlation than that generated with the single data matrix. The results indicated that germacrone, curdione, and furanodiene were detected in HPLC and GC-MS fingerprints, and may be the main antibacterial components. Abbreviations: CWEO, essential oil from C. wenyujin; MIC, minimum inhibitory concentration; OPLS, orthogonal projection to latent structures. [ABSTRACT FROM AUTHOR]

4-Acylphenols are important chemical feedstocks for the synthesis of various bioactive compounds. 4-Acylphenols derivatives were achieved by electrochemical oxygenation using H 2 O as the sustainable green oxygen source. The strategy also provides expedient access to amination of p -methylphenols with sulfonamides. Detailed mechanistic studies by isotope trace experiments, NMR spectroscopy and cyclic voltammetry studies provided the possible pathways for the indirect electrochemical oxygenation events. [Display omitted] Electrochemical C(sp3) − H oxygenation of phenols derivatives were accomplished using H 2 O as the sole oxygen source. Thus, selectively oxidative 4-cresols to 4-acylphenols derivatives proved viable with the aid of indirect electrolysis, through metal- and external oxidant free environmental-friendly and safe electrocatalytic conditions. Advances of this strategy were proved by its ability to transform various sulfonamides with excellent site and regioselectivity. Detailed mechanistic studies allowed to delineate the exact profile of the generation of the oxygenation events. [ABSTRACT FROM AUTHOR]

Abstract: The advantageous features of a split-and-recombination (SAR) microreactor for organic synthesis of labile bioactive compounds are demonstrated with rapid and efficient cross-coupling reactions of two monophosphate components to form a saccharide–nucleoside diphosphate. With this microreactor possessing the SAR mechanism that dramatically enlarges the material interface to promote the fluidic mixing, 85% conversion of a cross-coupling reaction (GlcNAc monophosphate reacting with UMP-morpholidate) to the diphosphate (acetylated UDP-GlcNAc) was achieved in 10s, which is a small fraction of the two days for 80% conversion with a conventional batch reactor; the duration of reaction is hence decreased 105 fold. Diphosphate from another cross-coupling reaction (GlcNAc monophosphate reacting with phosphoro-p-anisidate) was prepared in 94% yield (HPLC analysis) over a reaction duration 90s with this microreactor; furthermore, 1mg of the resulting compound was obtained in ∼20min. An abbreviated duration and satisfactory output are expected to be realized when several SAR microreactors are applied in parallel. By means of this microreactor technique, a synthesis with burdensome and protracted procedures becomes facile to generate products with great efficiency. [Copyright &y& Elsevier]

Gx-50 is a bioactive compound for the treatment of Alzheimer's disease (AD) found in Sichuan pepper (Zanthoxylum bungeanum). In order to find a stronger anti-AD lead compound, 20 gx-50 (1–20) analogs have been designed and synthesized, and their molecular structures were determined based on nuclear magnetic resonance (NMR) and mass spectrometry (MS) analysis, as well as comparison with literature data. Compounds 1–20 were evaluated for their anti-AD potential by using DPPH radical scavenging assay for considering their anti-oxidant activity, thioflavin T (ThT) fluorescence assay for considering the inhibitory or disaggregate potency of Aβ, and transgenic Drosophila model assay for evaluating their rescue effect on memory loss. Finally, compound 13 was determined as a promising anti-AD candidate. [ABSTRACT FROM AUTHOR]

Plant secondary metabolites (SMs) are not only a useful array of natural products but also an important part of plant defense system against pathogenic attacks and environmental stresses. With remarkable biological activities, plant SMs are increasingly used as medicine ingredients and food additives for therapeutic, aromatic and culinary purposes. Various genetic, ontogenic, morphogenetic and environmental factors can influence the biosynthesis and accumulation of SMs. According to the literature reports, for example, SMs accumulation is strongly dependent on a variety of environmental factors such as light, temperature, soil water, soil fertility and salinity, and for most plants, a change in an individual factor may alter the content of SMs even if other factors remain constant. Here, we review with emphasis how each of single factors to affect the accumulation of plant secondary metabolites, and conduct a comparative analysis of relevant natural products in the stressed and unstressed plants. Expectantly, this documentary review will outline a general picture of environmental factors responsible for fluctuation in plant SMs, provide a practical way to obtain consistent quality and high quantity of bioactive compounds in vegetation, and present some suggestions for future research and development. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance: Paeoniflorin (PF) is the principal bioactive component of Radix Paeoniae alba, which is widely used in Traditional Chinese Medicine for the treatment of neurodegenerative disorders such as Parkinson''s disease (PD). Aim of the study: To evaluate the neuroprotective effects of PF on MPP+- or acid- (pH 5.0) induced injury in cultured PC12 cells and to investigate the activity of autophagy-lysosome pathway (ALP). Amiloride (Ami), a non-selective blocker of acid-sensing ion channels (ASICs), as a positive control drug, since it is neuroprotective in rodent models of PD. Materials and methods: The cell viability was analyzed with MTT assay. The cell injury was assessed by lactate dehydrogenase (LDH) assay. Flow cytometry and Western blot analysis were used to study the apoptotic, calcium influx and autophagic mechanisms. Results: Ami (100μM) and PF (50μM) both protected PC12 cells against MPP+- or acid-induced injury as assessed by MTT assay, lactate dehydrogenase release, and apoptosis rate. The concentrations of cytosolic free Ca2+ were raised after exposure to MPP+ or acidosis, while Ami and PF both reduced the influx of Ca2+. More importantly, we found that the mechanisms of neuroprotective effects of Ami and PF were closely associated with the upregulation of LC3-II protein, which is specifically associated with autophagic vacuole membranes. Furthermore, application of MPP+ or acid induced the overexpression of LAMP2a, which is directly correlated with the activity of the chaperone-mediated autophagy pathway. However, Ami and PF inhibited the overexpression of LAMP2a. Conclusions: Our data provide the first experimental evidence that PF modulates autophagy in models of neuron injury, as well as providing the first indication of a relationship between ASICs and ALP. [Copyright &y& Elsevier]

Abstract: Ergosta-4,6,8(14),22-tetraen-3-one (ergone), isolated from the medicinal fungus Polyporus umbellatus, has been proven to prevent the progression of renal injury and the subsequent renal fibrosis. UPLC Q-TOF/MS was employed to investigate the metabonomic characteristics of adenine-induced chronic renal failure (CRF) and the proactive effects of ergone. The significant difference of the metabolic profiling was observed from ergone-treated group compared with the CRF model group during the 10-day and 20-day study periods by using the principal components analysis (PCA). The significant difference of the ergone-treated group in metabolic profiling was also observed between 10-day and 20-day study periods. The time-dependent tendency in ergone-treated group from day 10 to 20 was obtained, indicating the time-dependent recovery effect of ergone on CRF rats. Some significantly changed metabolites like creatinine, proline, adrenosterone, taurine, creatine, phenylalanine, ornithine, dopamine, kynurenine, kynurenic acid and 3-O-methyldopa have been identified during the 20-day study period. These biochemical changes are related to the disturbance in energy metabolism and amino acid metabolism, which are helpful to further understand the CRF and the therapeutic mechanism of ergone. This work suggests that this metabonomic approach could be used as a potentially powerful tool to investigate the biochemical changes of certain physiopathological conditions, such as metabolic syndrome, as an early diagnostic measure. [Copyright &y& Elsevier]