Policosanol extracted from sugarcane wax is a generic term used for total fatty alcohols obtained from esterification of fatty acids. It has been approved as a health functional food by the Ministry of Food and Drug Safety of Korea in 2006. Policosanol is well-known to aid in lowering blood cholesterol level. Recently, several studies have reported the physiological activities of policosanol, such as anti-inflammatory effects, antioxidant effects, and lowering of the incidence of ageing-related diseases, for example, hypertension, stroke, among others. This review describes the physiological activities of policosanol and its applications in the field of health functional foods.
Antioxidants ; Cholesterol ; Esterification ; Fatty Acids ; Fatty Alcohols ; Functional Food ; Hypertension ; Incidence ; Korea ; Saccharum ; Stroke

Gatifloxacin (GFX) is a kind of chiral fluoroquinolones compound due to the methyl group at the C-3 position of the piperazine ring[1]. Although the enantiomers of GFX show similar levels of antimicrobial activity and pharmacokinetics[2], the other biological activities (i.e., toxicity or enantioselective recognition to various receptors in vivo) of GFX enantiomers have not yet been studied. With this in mind, we developed a rapid and cost-effective high performance liquid chromatographic (HPLC) separation procedure for GFX enantiomers with a pre-column esterification strategy. With significant enhancement of drug solubility and optimization for chromatographic conditions, the proposed method was scaled up to preparative HPLC to obtain optical active S-(-)- and R-(+)-GFX. The antibacterial activities of GFX enantiomers after preparative separation were further verified by measuring the Minimum Inhibitory Concentration (MIC) values against Escherichia coli ATCC 25922. In addition, the binding selectivity of GFX enantiomers to protein receptor were evaluated by antibody using enzyme-linked immunosorbent assay (ELISA) for the first time.
Anti-Bacterial Agents ; chemistry ; pharmacology ; Escherichia coli ; drug effects ; Esterification ; Fluoroquinolones ; chemistry ; pharmacology ; Microbial Sensitivity Tests ; Molecular Structure ; Structure-Activity Relationship

Adipose tissue, where various metabolic hormones are secreted, plays a role in metabolizing different substances including androgen. Within fat tissue, enzymes such as aromatase and aldo-keto reductase 1C are responsible for metabolizing testosterone into estrogen and 5-dihydrotestosterone into inactive metabolites. Adipose tissue can also affect the secretion of gonadotropin, which influences the formation of androgen in the testes. At the same time, androgen has an impact on the distribution and proliferation of adipose tissue. The adrenoreceptors for catecholamines, which have been proven to play an essential role in controlling lipolysis, function by being up-regulated by androgens. Furthermore, androgens regulate the activity of lipoprotein lipase, a key enzyme involved in intracellular esterification of adipose tissue.
Adipose Tissue ; Alcohol Oxidoreductases ; Androgens ; Aromatase ; Catecholamines ; Esterification ; Estrogens ; Gonadotropins ; Humans ; Lipolysis ; Lipoprotein Lipase ; Male ; Oxidoreductases ; Testis ; Testosterone

AIM: To synthesize three novel esterified-derivatives of mangiferin and evaluate their hypoglycemic activities. METHODS: Acetic, propionic, and butyric anhydride were reacted with mangiferin, respectively. The hypoglycemic activity of the derivatives was evaluated using a hyperglycemic mouse model induced by streptozotocin (STZ), and the islet cells were checked by biopsy inspection. RESULTS: 7, 2', 3', 4', 6'-penta-acetyl-mangiferin (PAM), 3, 6, 7, 2', 3', 4', 6'-hepta-propionyl-mangiferin (HPM) and 3, 6, 7, 2', 3', 4'-hexa-butyryl-mangiferin (HBM) were synthesized and their structures were identified by MS,(1)H, (13)C NMR, and 2D NMR. These three compounds were reported for the first time. PAM group (0.5, 0.25 mmol·kg(-1)), HPM group (0.5, 0.25 mmol·kg(-1)), and HBM group (0.5, 0.25, 0.125 mmol·kg(-1)) mice showed strong hypoglycemic activity (P < 0.01); mangiferin group (1, 0.5 mmol·kg(-1)), PAM group (0.125 mmol·kg(-1)) and HPM group (0.125 mmol·kg(-1)) showed marginal hypoglycemic activity (P < 0.05); mangiferin group (0.25 mmol·kg(-1)) had the potential for a hypoglycemic effect, although it did not demonstrate that statistically. In histological examination, the islet cells of the PAM, HPM, and HBM groups could recover from the STZ damage; islet cells of the mangiferin group could recover also, but less than the esterified-derivative groups. CONCLUSION Derivatives could repair the damaged islet cells, and had higher lipid-solubility and stronger hypoglycemic activity than mangiferin itself. There existed a structure activity effect, and a solubility effect relationship: the larger esterification moieties, or the higher lipid-solubility, the stronger the hypoglycemic activity (no ester → acetyl → propionyl → butyryl). Esterified derivatives of mangiferin are potential compounds for new anti-diabetes drugs.
Animals ; Diabetes Mellitus, Experimental ; drug therapy ; Esterification ; Humans ; Hypoglycemic Agents ; administration & dosage ; chemical synthesis ; chemistry ; Islets of Langerhans ; drug effects ; Male ; Mice ; Molecular Structure ; Xanthones ; administration & dosage ; chemical synthesis ; chemistry

The asialoglycoprotein receptor (ASGPR) was used to mediate drug carrier for hepatic targeted drug delivery, this article showed the enzyme-catalyzed esterification of galactose and vinyl stearate and a kind of ASGPR ligand-targeted which was used to insert the surface of liposome has been synthesized. The structure of product has been confirmed by TLC, ESI-MS and 1H NMR. The factors of types and quantity of enzyme, organic solvents, molar ratio of substrate, temperature and time of reaction have been studied. Results showed when using acetone as reaction medium, the quantity of Novozym 435 immobilized lipase was 30 mg mL(-1), molar ratio of galactose to vinyl stearate was 1:5, and reacted at 60 degrees C for 12 h, the transformation of vinyl stearate reached more than 70%. This study provides a novel and efficient route to the synthesis of ligand-targeted modifier.
Acetone ; chemistry ; Asialoglycoprotein Receptor ; chemical synthesis ; Catalysis ; Esterification ; Galactose ; chemistry ; Ligands ; Lipase ; chemistry ; Stearates ; chemistry ; Temperature ; Vinyl Compounds ; chemistry

This paper reports the progress of biodiesel production with enzymatic catalysis in Beijing University of Chemical Technology, one of the leaders in biodiesel R & D in China, which includes screening of high-yield lipase production strains, optimization and scale-up of the lipase fermentation process, lipase immobilization, bioreactor development and scale-up, biodiesel separation and purification and the by-product glycerol utilization. Firstly, lipase fermentation was carried out at industrial scale with the 5 m3 stirred tank bioreactor, and the enzyme activity as high as 8 000 IU/mL was achieved by the species Candida sp. 99-125. Then, the lipase was purified and immobilized on textile membranes. Furthermore, biodiesel production was performed in the 5 m3 stirred tank bioreactor with an enzyme dosage as low as 0.42%, and biodiesel that met the German biodiesel standard was produced. And in the meantime, the byproduct glycerol was used for the production of 1,3-propanediol to partly offset the production cost of biodiesel, and 76.1 g/L 1,3-propanediol was obtained in 30 L fermentor with the species Klebsiella pneumoniae.
Biofuels ; Bioreactors ; Biotechnology ; economics ; methods ; Candida ; enzymology ; Catalysis ; China ; Enzymes, Immobilized ; metabolism ; Esterification ; Fermentation ; Lipase ; metabolism ; Plant Oils ; chemistry

Pectin, a polysaccharide extracted from the cell wall of plants, was used as the drug carrier to synthesize the pectin-adriamycin conjugates (P(A)n). The structure of the conjugates was confirmed by UV and IR. The degree of esterification (DE) of the pectin was assessed, and it was found that DE significantly influenced the carboxy group contents, inherent viscosity and galacturonic acid contents of the pectin. The results of drug release test in vitro showed that the conjugate was stable in normal saline, but was gradually enzymolyzed to release the adriamycin in blood plasma and in lymph nodes. The results of lymphatic targeting study of P(A), demonstrated that the modification of DE or drug coupling capacity of pectin significantly influenced the lymphatic targeting characteristics of P (A)n. The adriamycin concentration of lymph nodes was 208 times higher than that of plasma after local injection of the P(A)n, of which the adriamycin content was 27.9% and the pectin was deesterificated 120 minutes by the use of hypothermy alkaline deesterification method.
Animals ; Antibiotics, Antineoplastic ; administration & dosage ; pharmacokinetics ; Doxorubicin ; administration & dosage ; pharmacokinetics ; Drug Carriers ; chemistry ; Esterification ; Lymph Nodes ; metabolism ; Pectins ; administration & dosage ; pharmacokinetics ; Rabbits

OBJECTIVETo prepare colon-targetting tablets of total alkaloids of Sophora alopecuroides and evaluate the effect of pectins of different degree of esterification (DE) on sophoridine release profiles in-vitro.

METHODWet granulation technique was employed to prepare petin-based matrix tablets, then tablets were coated the optimal formulation with Kollicoat MAE 30 DP based on the optimal formulation and analysed their release.

RESULTCoated formulation E could target total alkaloids of S. alopecuroides to colon and various DE of pectin exerted different effects on sophoridine release. The release of low DE pectin-based matrix tablets coating with Kollicoat MAE 30 DP approximatedly fitted zere-order eqution, which was erosion depended.

CONCLUSIONLow DE pectin-based matrix tablet coating with Kollicoat MAE 30 DP can deliver sophoridine to colon, hence improve the effectiveness of sophoridine.

Alkaloids ; chemistry ; Animals ; Chemistry, Pharmaceutical ; Chromatography, High Pressure Liquid ; Colon ; chemistry ; Esterification ; Hydrogen-Ion Concentration ; In Vitro Techniques ; Male ; Pectins ; chemistry ; Quinolizines ; chemistry ; Rats ; Rats, Sprague-Dawley ; Sophora ; chemistry ; Tablets ; chemistry

The method was established study the influence of different herbal combination with Radix Aconiti in the traditional medical formulae on content of the aconite alkaloids, for elucidating the scientific basis of reducing the toxicity of aconite in traditional Chinese medical formulation. The samples for ESI-MS study were prepared by decocting a mixture of Radix Aconiti Lateralis Preparata ( RALP) with Radix Glycyrrhizae Preparata (RGP) , Radix Paeoniae Alba ( RPA) , Rhizoma Zingiberis (RZ) or Radix Et Rhizoma Rhei ( RERR) , separately, and extracting the residue of the above mentioned mixtures after decocting. The diester-diterpenoid alkaloids (DDAs) was lower in the herb couples of RALP-RGP, RALP-RPA, RALP-RZ and RALP-RERR, and lipo-alkaloids was increased in the herb couples of RALP-RGP, RALP-RPA and RALP-RZ. The reason of reducing toxic effect principle is that the components of RGP, RPA and RZ have ester-exchange reactions with DDAs in RALP to produce lipo-alkaloids of low toxicity in the decocting process of the herb couples. The combination of RALP-RERR can reduce the content of DDAs in decoction and residue due to the formation of water insoluble alkaloid compound.
Aconitine ; analogs & derivatives ; analysis ; chemistry ; Aconitum ; chemistry ; Alkaloids ; analysis ; chemistry ; Diterpenes ; analysis ; chemistry ; Drug Combinations ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Esterification ; Ginger ; chemistry ; Glycyrrhiza uralensis ; chemistry ; Hot Temperature ; Paeonia ; chemistry ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Rheum ; chemistry ; Spectrometry, Mass, Electrospray Ionization ; methods

Biodiesel fuel produced with the enzyme-catalyzed esterification and transesterification of high acid value waste oil through ultrasonic assistant was explored. Propyl oleate, biodiesel, converted from high acid value waste oil and 1-proponal catalyzed with immobilized lipases from Candida antarctica and Aspergillus oryzae in conditions of ultrasonic assistant. Commercial immobilized lipase Novozym 435 from C. antarctica was used as biocatalyst catalyzing high acid value waste oil and 1-proponal esterification and transesterification to propyl oleate under the ultrasonic assistant conditions and different conditions such as lipases amounts, initiatory molar ratio of propanol to oil, frequency of ultrasonic and power of ultrasonic were investigated and optimized. It is revealed that the enzymatic activity of Novozym435 is enhanced and, in particular, enzyme-catalyzed transesterification activity is enhanced obviously under the ultrasonic assistant conditions. Low frequency and mild energy ultrasonic is a key factor for enhancing enzymatic activity, emulsifying oil-propanol system and accelerating the speed of produce diffusing in the system. Under the optimal ultrasonic assistant reaction conditions, such as Novozym435 amounts 8% by oil quantity, initiatory molar ratio of propanol to oil 3:1, frequency of ultrasonic 28 KHz, power of ultrasonic 100 W and temperature of water batch 40-45 degrees C, the conversion ratio to propyl oleate reached to 94.86% in 50 mins in comparison with the highest conversion ratio to propyl oleate 84.43% under the conventional mechanical agitation conditions. Furthermore, it is demonstrated that various short chain linear and branched alcohols (C1-C5) show high conversion ratio to fatty acid alkyl esters (biodiesel) under the optimal ultrasonic assistant reaction conditions. On the other hand, ultrasonic energy is propitious to reduce the adsorption of product propyl oleate, by-product glycerol and other emplastics in system on the surface of immobilized lipase Novzym435 and recyclable Novozym435 possess clean appearances, well decentralizations, no agglomeration and easy washing and well operational stability.
Bioelectric Energy Sources ; Catalysis ; Esterification ; Gasoline ; Lipase ; chemistry ; Ultrasonics ; Waste Disposal, Fluid ; methods