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Xinzhou Yang et al.
Journal of ethnopharmacology, 171, 161-170 (2015-06-09)
Bitter and cold Chinese medicines have been long used for the treatment for diabetes mellitus (DM) for thousands of years in China. The roots of Sophora flavescens Ait., one of bitter and cold Chinese medicines commonly used to remove lung
Jee Hee Suh et al.
Chemical & pharmaceutical bulletin, 63(8), 573-578 (2015-06-05)
We describe the synthesis and biological evaluation of N-aryl-5-aryloxazol-2-amine derivatives that are able to inhibit 5-lipoxygenase (5-LOX), a key enzyme of leukotriene synthesis, for the treatment of inflammation-related diseases including asthma and rheumatoid arthritis. A novel structural moiety containing oxazole
Kuruva Chandra Sekhar et al.
Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 22, 76-76 (2014-12-30)
Chronic and oral administration of benzylamine improves glucose tolerance. Picolylamine is a selective functional antagonist of the human adenosine A2B receptor. Phosphonic diamide derivatives enhance the cellular permeability and in turn their biological activities. A series of heteroaryl phosphonicdiamide derivatives
Benjamin J Pages et al.
Dalton transactions (Cambridge, England : 2003), 43(41), 15566-15575 (2014-09-10)
Eight platinum(II) complexes with anticancer potential have been synthesised and characterised. These complexes are of the type [Pt(I(L))(A(L))](2+), where I(L) is either dipyrido[3,2-f:2',3'-h]quinoxaline (dpq) or 2,3-dimethyl-dpq (23Me2dpq) and A(L) is one of the R,R or S,S isomers of either 1,2-diaminocyclohexane
Xiu-Mei Li et al.
European journal of medicinal chemistry, 96, 436-444 (2015-04-29)
Hypericum ascyron L. has been used as a traditional medicine for the treatment of wounds, swelling, headache, nausea and abscesses in China for thousands of years. However, modern pharmacological studies are still necessary to provide a scientific basis to substantiate
Hannu Elo et al.
European journal of medicinal chemistry, 92, 750-753 (2015-01-27)
Certain substituted salicylaldehydes are potent antibacterial and antifungal agents and some of them merit consideration as potential chemotherapeutic agents against Candida infections, but their mechanism of action has remained obscure. We report here a distinct correlation between broadening of the
Vincenzo Taresco et al.
The journal of physical chemistry. B, 119(26), 8369-8379 (2015-06-16)
Amphiphilic polyelectrolytes (APEs), exhibiting particular self-association properties in aqueous media, can be used in different industrial applications, including drug delivery systems. Their typical core-shell structure (micelle) depends on the balance of interactions between hydrophobic and ionizable monomer units. In this
Nicola Parisi et al.
International journal of pharmaceutics, 493(1-2), 404-411 (2015-08-04)
Hexamidine diisethionate (HEX D) has been used in the personal care industry and in a number of over-the-counter (OTC) drug products as an antimicrobial agent since the 1950's. Recently, the compound has also been investigated for its beneficial effects on
Pavla Simerska et al.
Drug delivery and translational research, 4(3), 246-255 (2015-03-20)
Peptide-based vaccine delivery can be hampered by rapid peptidase activity and poor inherent immunogenicity. The self-adjuvanting lipid core peptide system (LCP) has been shown to confer improved stability and immunogenicity on peptide epitopes of group A Streptococcus, Chlamydia, hookworm, and
Chi-Yuan Cheng et al.
Biophysical journal, 109(2), 330-339 (2015-07-23)
Dimethyl sulfoxide (DMSO) has been broadly used in biology as a cosolvent, a cryoprotectant, and an enhancer of membrane permeability, leading to the general assumption that DMSO-induced structural changes in cell membranes and their hydration water play important functional roles.
Anja Balk et al.
Pharmaceutical research, 32(6), 2154-2167 (2014-12-24)
A poorly water soluble acidic active pharmaceutical ingredient (API) was transformed into an ionic liquid (IL) aiming at faster and higher oral availability in comparison to a prodrug. API preparations were characterized in solid state by single crystal and powder
Denis A Babkov et al.
Bioorganic & medicinal chemistry, 23(21), 7035-7044 (2015-10-08)
The need for novel therapeutic options to fight herpesvirus infections still persists. Herein we report the design, synthesis and antiviral evaluation of a new family of non-nucleoside antivirals, derived from 1-[ω-(4-bromophenoxy)alkyl]uracil derivatives--previously reported inhibitors of human cytomegalovirus (HCMV). Introduction of
Yan Tan et al.
Biomaterials, 56, 219-228 (2015-05-03)
Serious challenges remain in immunotherapy, such as to effectively deliver antigens and non-invasively monitor biological processes. Therefore, we aim to design a useful nanocarrier for enhancing antigen-specific immune response and performing functional molecular imaging guided immunotherapy. To achieve this goal
Navneet Chandak et al.
Journal of enzyme inhibition and medicinal chemistry, 29(4), 476-484 (2013-06-20)
Synthesis of total eighteen 2-amino-substituted 4-coumarinylthiazoles including sixteen new compounds (3a-o and 5b) bearing the benzenesulfonamide moiety is described in the present report. All the synthesized target compounds were examined for their in vivo anti-inflammatory (AI) activity and in vitro
Aditya Kapil Valiveti et al.
Chemico-biological interactions, 237, 125-132 (2015-06-14)
A series of mono pyridinium oximes linked with arenylacetamides as side chains were synthesized and their in vitro reactivation potential was evaluated against human acetylcholinesterase (hAChE) inhibited by organophosphorus inhibitors (OP) such as sarin, VX and tabun. The reactivation data
Amir Mahboubi et al.
Plant physiology, 168(2), 478-489 (2015-05-02)
Wood of trees is formed from carbon assimilated in the photosynthetic tissues. Determining the temporal dynamics of carbon assimilation, subsequent transport into developing wood, and incorporation to cell walls would further our understanding of wood formation in particular and tree
Jinyun Dong et al.
Bioorganic & medicinal chemistry, 22(24), 6876-6884 (2014-12-04)
Bcr-Abl plays an essential role in the pathogenesis and development of chronic myeloid leukaemia (CML). Inhibition of Bcr-Abl has great potential for therapeutic intervention in CML. In order to obtain novel and potent Bcr-Abl inhibitors, twenty seven 4,6-disubstituted pyrimidines were
Daishun Ling et al.
ACS nano, 8(8), 8027-8039 (2014-08-06)
Hepatocellular carcinoma (HCC) has one of the worst prognoses for survival as it is poorly responsive to both conventional chemotherapy and mechanism-directed therapy. This results from a lack of therapeutic concentration in the tumor tissue coupled with the highly toxic
Lenka Roubalová et al.
Bioorganic & medicinal chemistry, 23(17), 5402-5409 (2015-08-12)
Quercetin 3'-O-sulfate is one of the main metabolites of the natural flavonoid quercetin in humans. This study was designed to prepare quercetin 3'-O-sulfate (1), isoquercitrin 4'-O-sulfate (2) and taxifolin 4'-O-sulfate (3) by the sulfation of quercetin, isoquercitrin (quercetin 3-O-glucoside) and
Chung Ying Chan et al.
Dalton transactions (Cambridge, England : 2003), 44(44), 19126-19140 (2015-10-20)
A series of eight Rhenium(I)-N-heterocyclic carbene (NHC) complexes of the general form [ReCl(CO)3(C^C)] (where C^C is a bis(NHC) bidentate ligand), [ReCl(CO)3(C^C)]2 (where C^C is a bis-bidentate tetra-NHC ligand) and [Re(CO)3(C^N^C)](+)[X](-) (where C^N^C is a bis(NHC)-amine ligand and the counter ion
Rong Zhang et al.
Journal of agricultural and food chemistry, 62(33), 8302-8307 (2014-07-30)
Nonvolatile compounds play important roles in the quality of alcoholic beverages. In our previous work, a type of cyclooctapeptide lichenysin was newly identified in Chinese strong-aroma type liquor. In this work, it was found that lichenysin could selectively affect aroma
Virsinha Reddy et al.
Organic & biomolecular chemistry, 13(12), 3732-3741 (2015-02-18)
An efficient and mild protocol for the direct construction of aryl- and alkyl-substituted isoquinolines has been realized through silver nitrate catalyzed aromatic annulation of o-(1-alkynyl)arylaldehydes and ketones with ammonium acetate. The salient feature of this methodology is that this annulation
Ahmed M Younis et al.
International journal of medicinal mushrooms, 17(6), 579-590 (2015-09-10)
Pleurotus ostreatus is an edible mushroom that also has high medicinal values. In this study, P. ostreatus was tested for its ability to inhibit the growth of fungi and bacteria. The freeze-dried fruiting body, broth from submerged culture, and mycelial
Yingli Yang et al.
Oncology reports, 34(3), 1311-1318 (2015-07-03)
In the present study, 2-pyridinecarboxaldehyde 2-pyridinecarboxylic acid hydrazone (PPAH) was prepared and its antitumor activity was evaluated. The inhibition of proliferation of PPAH against the HepG2 and HCT-116 cell lines was less effective, yet in the presence of copper ions
Phuong Hoang Tran et al.
Molecules (Basel, Switzerland), 20(10), 19605-19619 (2015-10-31)
A fast and green method is developed for regioselective acylation of indoles in the 3-position without the need for protection of the NH position. The method is based on Friedel-Crafts acylation using acid anhydrides. The method has been optimized, and
Qi Wang et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 983-984, 39-46 (2015-01-24)
Coumarins are an important group of bioactive constituents in licorice (Glycyrrhiza uralensis), a worldwide popular herbal medicine. This study aims to elucidate the metabolism of two major licorice coumarins, glycyrin and glycyrol in rats. After oral administration of 40mg/kg glycyrin
Ting-Ting You et al.
Bioresource technology, 199, 271-274 (2015-09-14)
Acid enhanced ionic liquid (IL) 1-n-butyl-3-methylimidazolium chloride ([C4 mim]Cl) pretreatment has shown great potential for boosting the yield of sugars from biomass cost-effectively and environmental-friendly. Pretreatment with shorter processing time will promote the commercial viability. In this work, pretreatment of
Xuejiao Liu et al.
Journal of drug targeting, 23(5), 417-426 (2015-02-07)
Hypericin is a necrosis avid agent useful for nuclear imaging and tumor therapy. Protohypericin, with a similar structure to hypericin except poorer planarity, is the precursor of hypericin. In this study, we aimed to investigate the impact of this structural
Zongwang Ma et al.
Applied biochemistry and biotechnology, 177(7), 1520-1529 (2015-09-17)
Bacillus mojavensis B0621A was isolated from the mantle of a pearl oyster Pinctada martensii collected from South China Sea. Semi-purified surfactins (225 mg L(-1)) were obtained by acid precipitation and vacuum flash chromatography. The component of the semi-purified surfactins was preliminarily analyzed
Kun-Ming Jiang et al.
Medicinal chemistry (Shariqah (United Arab Emirates)), 11(5), 453-461 (2014-12-30)
A new series of (E)-N,2,3-triarylacrylamide derivatives were designed and synthesized as potent anticancer agents. Cytotoxicity of the 26 target compounds was evaluated in vitro against six cancer cell lines (HCT116, A549, MDA-MB-468, HepG2, SKNMC and SK-OV-3) by Sulforhodamine B colorimetric
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