One force-fed meal containing labelled (14)C-astaxanthin and (3)H-canthaxanthin or (3)H-zeaxanthin was given to eight mature female rainbow trout. Ninety-six hours after the test meal ingestion, trout were killed and liver, skin, muscle and ovaries were dissected out. Astaxanthin accumulated slightly more in muscle than canthaxanthin but in all tissues astaxanthin and canthaxanthin were very significantly more concentrated than zeaxanthin. (3)H-zeaxanthin metabolites were found only in the liver, whereas (14)C-phoenicoxanthin was the only metabolic pigment from (14)C-astaxanthin detected and was found in all investigated tissues. (3)H-astaxanthin was found in the liver of all trout indicating that (3)H-canthaxanthin and (3)H-zeaxanthin were astaxanthin precursors, and that salmonids probably possess carotenoid oxidative pathways unknown until now. Labelled retinol1 and retinol2 were detected only in the liver and (3)H-zeaxanthin was largely the predominant precursor of these two vitamin A forms.
The effects of feed intake, growth rate and temperature (8 and 12 degrees C) on apparent digestibility coefficients (ADC), blood uptake of individual astaxanthin E/Z isomers and metabolism of astaxanthin (3,3'-dihydroxy-beta,beta-carotene-4,4'-dione) were determined in Atlantic salmon. Accumulation of idoxanthin (3,4,3'-trihydroxy-beta,beta-carotene-4-one) in plasma was used to indicate metabolic transformation of astaxanthin.
The present study investigated the in vivo protective effect of astaxanthin isolated from the Xanthophyllomyces dendrorhous mutant against ethanol-induced gastric mucosal injury in rats. The rats were treated with 80% ethanol for 3 d after pretreatment with two doses of astaxanthin (5 and 25 mg/kg of body weight respectively) for 3 d, while the control rats received only 80% ethanol for 3 days. The oral administration of astaxanthin (5 and 25 mg/kg of body weight) showed significant protection against ethanol-induced gastric lesion and inhibited elevation of the lipid peroxide level in gastric mucosa. In addition, pretreatment with astaxanthin resulted in a significant increase in the activities of radical scavenging enzymes such as superoxide dismutase, catalase, and glutathione peroxidase. A histologic examination clearly indicated that the acute gastric mucosal lesion induced by ethanol nearly disappeared after pretreatment with astaxanthin.
/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
解毒与急救
/SRP:/ 高级治疗:对于昏迷、严重肺水肿或严重呼吸困难的病人,考虑进行口咽或鼻咽气管插管以控制气道。使用气囊面罩装置的正压通气技术可能有益。考虑使用药物治疗肺水肿...。对于严重的支气管痉挛,考虑给予β激动剂,如沙丁胺醇...。监测心率和必要时治疗心律失常...。开始静脉输注5%葡萄糖水(D5W)/SRP: "保持开放",最低流量/。如果出现低血容量的迹象,使用0.9%盐水(NS)或乳酸林格液。对于伴有低血容量迹象的低血压,谨慎给予液体。注意液体过载的迹象...。使用地西泮或劳拉西泮治疗癫痫...。使用丙美卡因氢氯化物协助眼部冲洗...。/Poisons A and B/
/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/
/ALTERNATIVE and IN VITRO TESTS/ Astaxanthin is a carotenoid found in plants and algae; it provides the color of marine seafood such as salmon, lobster, or shrimp. Carotenoids are antioxidants and exhibit other biological functions, including effects on gap junctional communication important for homeostasis, growth control, and development of cells. Cancer cells have an impaired gap junctional intercellular communication. The objective of the present study was to determine the effects of astaxanthin and canthaxanthin on gap junctional intercellular communication in vitro. Primary human skin fibroblasts were exposed to carotenoids from 0.001 to 10 umol/L, and gap junctional communication was measured with a dye transfer assay. After incubation with canthaxanthin for 24 and 72 h, intercellular communication increased, whereas it was strongly diminished by astaxanthin at levels > 0.1 umol/L. Inhibition was reversed when astaxanthin was withdrawn. Western blot analysis showed that after exposure to canthaxanthin, the amount of the gap junction protein connexin43 was increased. Incubation with astaxanthin led to a change in the phosphorylation pattern of connexin43, shifting from higher to lower phosphorylation states. We suggest that astaxanthin affects channel function by changing the phosphorylation pattern of connexin43.
/ALTERNATIVE and IN VITRO TESTS/ Astaxanthin (AST), primarily a carotenoid of marine origin, responsible for the pink coloration of salmon, shrimp and lobster, has received relatively little attention. As with other carotenoids, its highly lipophilic properties complicate delivery to model systems. To overcome this issue we have synthesized a novel tetrasodium diphosphate astaxanthin (pAST) derivative with aqueous dispersibility of 25.21 mg/ml. pAST was delivered to C3H/10T1/2 cells in an aqueous/ethanol solution and compared with non-esterified AST dissolved in tetrahydrofuran. We show pAST to (i) upregulate connexin 43 (Cx43) protein expression; (ii) increase the formation of Cx43 immunoreactive plaques; (iii) upregulate gap junctional intercellular communication (GJIC); and (iv) cause 100% inhibition of methylcholanthrene-induced neoplastic transformation at 10(-6) M. In all these assays, pAST was superior to non-esterified AST itself; in fact, pAST exceeded the potency of all other previously tested carotenoids in this model system. Cleavage of pAST to non-esterified (free) AST and uptake into cells was also verified by HPLC; however, levels of free AST were approximately 100-fold lower than in cells treated with AST itself, suggesting that pAST possesses intrinsic activity. The dual properties of water dispersibility (enabling parenteral administration in vivo) and increased potency should prove extremely useful in the future development of cancer chemopreventive agents. /Tetrasodium diphosphate astaxanthin derivative/
Apparent astaxanthin (3,3'-dihydroxy-beta,beta-carotene-4,4'-dione) digestibility coefficients (ADC) and carotenoid compositions of the muscle, liver, whole kidney and plasma were compared in Atlantic salmon (Salmo salar) and Atlantic halibut (Hippoglossus hippoglossus) fed a diet supplemented with 66 mg astaxanthin kg(-1) dry matter for 112 days. The astaxanthin source consisted of 75% all-E-, 3% 9Z- and 22% 13Z-astaxanthin, of (3R,3'R)-, (3R,3'S; meso)-, and (3S,3'S)-astaxanthin in a 1:2:1 ratio. The ADC of astaxanthin was significantly higher in Atlantic halibut than in Atlantic salmon after 56 and 112 days of feeding (P < 0.05). The ADC of all-E-astaxanthin was significantly higher than ADC of 9Z-astaxanthin (P < 0.05). Considerably more carotenoids were present in all plasma and tissue samples of salmon than in halibut. Retention of astaxanthin in salmon muscle was 3.9% in salmon and 0 in halibut. All-E-astaxanthin accumulated selectively in the muscle of salmon, and in plasma of salmon and halibut compared with diet. 13Z-astaxanthin accumulated selectively in liver and whole kidney of salmon and halibut, when compared with plasma. A reductive pathway for astaxanthin metabolism in halibut similar to that of salmon was shown by the presence of 3',4'-cis and trans glycolic isomers of idoxanthin (3,3',4'-trihydroxy-beta,beta-carotene-4'-one) in plasma, liver and whole kidney. In conclusion, the higher ADC of astaxanthin in halibut than Atlantic salmon may be explained by lower feed intake in halibut, and the lower retention of astaxanthin by a higher capacity to transform astaxanthin metabolically.
The present studies were performed to investigate the metabolism of astaxanthin (Ax) in Atlantic salmon, especially in the liver of salmon. The investigations were undertaken in vivo salmon that were fed a diet containing 60 ppm 15, 15' (14)C-labelled Ax prior to sacrifice. The samples of blood, bile, liver, gastrointestinal tract and contents, muscle, skin, remaining carcass and feces were taken for scintillation counting. The highest radioactivity (71.36%) of (14)C-labelled Ax was found in the gastrointestinal contents and feces, 7.13% in the bile and 10.68% in the samples of liver, muscle, and skin at the end of the experiments. The metabolites of (14)C-labelled Ax were extracted from the bile of the salmon and analyzed using thin-layer chromatography (TLC) and high performance liquid chromatography (HPLC). Predominant (14)C-labelled Ax and its cis-isomers were found and no conjugation of (14)C-labelled Ax was observed. These results indicate that (14)C-labelled Ax was not conjugated into larger colorless compound in Atlantic salmon liver.
Electron uptake by classical electron donators: astaxanthin and carotenoid aldehydes
摘要:
Carotenoids are prime examples for antioxidants: they donate electrons to noxious radicals. Density functional calculations anticipate the possibility of electron uptake by carotenoids. This prediction has been confirmed experimentally: carbonyl carotenoids, including the super-antioxidant astaxanthin, easily take up electrons and react as antireductants. (C) 2012 Elsevier Ltd. All rights reserved.
、 Astaxanthin bis(trimethylsilyl)ether 在
氩 、 虾青素 作用下,
以
甲醇 为溶剂,
反应 4.0h,
以Concentration of the mother liquor yielded about 3 g of solid red residue from which a further 0.4 g of crude astaxanthin的产率得到
参考文献:
名称:
Cyclohexenone derivatives and process for making same
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I
as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
The present invention relates to extracts of
Isochrysis
sp., preferably Tahitian
Isochrysis,
its cosmetic, dermatological and/or therapeutic uses and compositions and cosmetic, dermatological or therapeutic products comprising such an extract of
Isochrysis
sp., preferably Tahitian
Isochrysis.
CAROTENOID DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, OR PHARMACEUTICALLY ACCEPTABLE ESTER OR AMIDE THEREOF
申请人:FUJI CHEMICAL INDUSTRIES CO., LTD.
公开号:US20170081289A1
公开(公告)日:2017-03-23
The object of the present invention is to find a carotenoid compound that is excellent in water solubility.
A carotenoid derivative having a formula (I):
wherein
X represents a carbonyl group or a methylene group, one of R
1
and R
2
represents (a) or (b) and the other represents (a), (b), (c) or a hydrogen atom:
(a): —CO-A-B-D wherein A represents an alkylene group an alkenylene group, etc., B represents a formula of —S(O)
n
— or a formula of —NR
4
CONR
5
— and D represents a hydrogen atom, a carboxy group, etc.,
(b): —CO-E-F wherein E represents an alkylene group or a formula of —NR
3
— wherein R
3
represents (a1) a hydrogen atom, (b1) an alkyl group etc., and F represents a sulfo group and
(c): —CO-G wherein G represents a hydrogen atom, an alkyl group, etc.,
a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester or amide thereof.
POLYMER-CARBOHYDRATE CONJUGATES FOR DRUG DELIVERY TECHNOLOGY
申请人:Wu Nian
公开号:US20150157721A1
公开(公告)日:2015-06-11
The invention comprises compounds, methods of making, and methods of using. The compounds may have a linear or cylic backbone and three or four appended functional groups: one or two lipohilic compounds including sterols or “fat soluble” vitamins, one or two hydrophilic polymer, and one or two carbohydrate. A group of polymer-carbohydrate conjugates having a central backbone and three appended functional groups are disclosed wherein one lipophilic compound is void of both steroid acids. The conjugate may have fatty acids as the primary lipophilic carrier, one hydrophilic polymer, and one carbohydrate. Specific functional groups may be selected for specific applications in formulating pharmaceuticals, cosmetics, nutriceuticals, and the like. Typical coupling reaction of the conjugates may involve one or more or combinations or in series of alkylation including N-alkylation or O-alkylation, etherification, esterification and amidation chemical processes. A variety of linkers between the backbone and functional groups may also be selected to modify the carriers or center backbones for the coupling reactions and optimize performance of the conjugates.
[EN] IMPROVED NANOPARTICLE DELIVERY SYSTEMS<br/>[FR] SYSTÈMES AMÉLIORÉS D'ADMINISTRATION DE NANOPARTICULES
申请人:CELATOR PHARMACEUTICALS INC
公开号:WO2017011685A1
公开(公告)日:2017-01-19
Nanopaiticle compositions described herein comprise combinations of prodrugs of therapeutic agents that achieve enhanced therapeutic effects as compared to those observed when combinations of free forms of these therapeutic agents are administered.