(+) 9-Demethoxyporothramycin B 3a and (+) porothramycin B 3b were synthesized from (S) pyroglutamic acid through a versatile and efficient route.

The first total synthesis of (+)-porothramycin B (1b is described. Our synthetic pathway can be readily applied to the synthesis of other members of the pyrrolo[1,4]benzodiazepine antibiotics.

Proteolysis during the storage of UHT milk is associated with major technological problems, particularly bitter off-flavors and age gelation limiting the shelf life of milk. In this study, untargeted peptide profiling by MALDI-TOF-MS identified peptides that were formed by proteolysis and reflec...

Two series of 1,4-dihydropyridines related to tiamdipine, 2-(2-aminoethylthio)methyl-3-carboethoxy-5-carbomethoxy-6-methyl-4-(3-nitrophenyl)-1, 4-dihydropyridine, have been evaluated for their pharmacologic and radioligand binding properties in smooth and cardiac muscle. In the tiamdipine series...

The pharmacologic and radioligand binding properties of 5-nitro analogs of the 1,4-dihydropyridine Ca2+ channel antagonist, tiamdipine (2-(2-aminoethylthio)methyl-3-carboethoxy-5-carbomethoxy-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine) and its N-formyl derivative have been measured in rat ta...

This study investigated the effects of heating skim milk with soluble calcium salts, calcium chloride, calcium lactate, calcium gluconate and calcium lactobionate, on the physico-chemical and rheological properties of milk. Regardless of the type of salt added, the amount of casein in milk serum...

Prebiotic compounds may be consumed during storage by the foodstuff’s own microflora, so that new processes to protect these bioactive compounds before they are released in the gastrointestinal tract need to be developed. With this aim, lyophilized calcium lactobionate microparticles were desig...

A novel organic compound containing antipyrine and thiadiazole moieties, N-(5-{[antipyrinyl-hydrazono]-cyanomethyl}-[1,3,4]thiadiazol-2-yl)-benzamide (ACTB) has been synthesized. The thermal properties, alternating current electrical conductivity (σAC) and electrical modulus of ACTB have been r...

A one-step synthesis of 5-alkoxypyrrole-3-phosphonates is presented starting from suitable α-cyanomethyl-β-ketophosphonates. The key step in the synthesis involves a one-pot addition and heteroannulation sequence. The zinc perchlorate-catalyzed addition of alcohols to the nitrile carbon of α-...

Details of structure–activity relationships (SAR) for P2 moiety of a P1 2-cyanopyrrolidine dipeptidyl peptidase IV (DPP-IV) inhibitor 4a including stereochemistry are presented. Based on this information, a series of P1 (N-alkyl)aminoacetonitrile analogs 9–20 possessing optimal P2 structure we...

6,7-Dihydroxy-N-cyanomethyl-1,2,3,4-tetrahydroisoquin oline, a cyanomethyl derivative of dopamine formed from cigarette smoke, was found to inhibit the activity of tryptophan hydroxylase. The inhibition was non-competitive to the substrate l-tryptophan (the Ki value 7.25 ± 0.81 μM), but not to...

A convenient and mild synthetic method of synthesizing benzofuran from various 2-(cyanomethyl)phenyl carbonyl compounds under reduced oxygen conditions is reported. Nine C-2 substituted benzofurans were synthesized at 52–89%.

Sagittatoside B, a rare secondary flavonol glycoside in Epimedii Folium, has much better in vivo bioactivities than its original glycoside epimedin B. Its preparation methods, such as acidic hydrolysis, are of low efficiency, and byproducts are generated. The objective of this study was to estab...

Epimedin C is an important component of Epimedium with many beneficial functions to human health. In this study, the feasibility of the extraction of epimedin C from fresh leaves of Epimedium using ultrasonic probe system was demonstrated. The high extraction yield of epimedin C was obtained und...

An ultrasonic-assisted extraction (UAE) procedure of epimedin A, epimedin B, epimedin C and icariin from Herba Epimedii was developed. The effects of ethanol concentration, ratio of liquid to solid, UAE time, extraction temperature and number of extraction cycles on the extraction yields of the ...

ObjectiveTo evaluate the anti-osteoporosis effect of the mixtures of epimedin C and icariin monomers with invariant molarity on zebrafish osteoporosis model.

In this study, a α-l-rhamnosidase gene from Bacteroides thetaiotaomicron VPI-5482 was cloned and expressed in Escherichia coli. The specific activity of rhamnosidase was 0.57 U/mg in LB medium with 0.1 mM Isopropyl β-d-Thiogalactoside (IPTG) induction at 28 °C for 8 h. The protein was purifie...

In this work, near infrared (NIR) spectroscopy was used in combination with chemometrics to determine the epimedin A, epimedin B, epimedin C, icariin, and moisture contents of Herba Epimedii. The variable selection method genetic algorithm (GA) and regression tool support vector machine (SVM) we...

Herba Epimedii is a traditional Chinese herbal medicine that contains a mixture of bioactive flavonoid glycosides. Among them, icariin has the most outstanding bioactive functions, while epimedin C exhibits substantial toxicity. A recombinant α-L-rhamnosidase (synAnRhaE) from Aspergillus nidula...

A series of four closely related 1,2,4-triazole-3-thione (1-4) compounds was obtained by heterocyclization of thiosemicarbazides under basic catalytic conditions. The crystal structures of the 4-alkyl-5-(substituted-phenyl)-2H-1,2,4-triazole-3(4H)-thione derivatives [4-alkyl = 4-ethyl-5-phenyl (...