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At least 181 records · Page 10Linked to original sources
PubMed1989

[Diflucortolone-21-valerate Reference Standard (Control 871) of National Institute of Hygienic Sciences].

Diflucortolone-21-valerate was tested for the preparation of "Diflucortolone-21-valerate Reference Standard (Control 871)". Analytical data obtained were as follows: loss on drying, 0.05%; infrared spectrum, 1745, 1727, 1667, 1625, 1611, 1169 cm-1; ultraviolet spectrum, lambda max = 239 nm; absorbance, E1%1cm (239 nm) = 348.8; optical rotation, [alpha]20D: + 100.8 degrees; melting point, 203.2 degrees C; thin-layer chromatography, three contaminants were detected; high-performance liquid chromatography, two contaminants were detected; fluorine, 8.06%. On the basis of those results, this material was authorized as the National Institute of Hygienic Sciences Reference Standard (Control 871).

Chemical Phenomena↗
PubMed1978

[Comparative study on the efficacy of diflucortolone valerate in the psoriasis plaque test (author's transl)].

Diflucortolone valerate was administered to 35 psoriatic patients of both sexes in 0.3% concentration as a W/O emulsion in comparison with various commercially available preparations to study its action in the psoriasis plaque test according to Scholtz and Dumas. The study showed the test substance to be equipotent with the halcinonide, clobetasol-17-propionate and desoximetasone preparations and significantly superior to those containing betamethasone-17,21-dipropionate, betamethasone-17-valerate and fluocinonide.

Adult↗
PubMed1983

Effects of a massive single oral dose of oestradiol valerate in a young woman.

Effects of a massive single oral dose of oestradiol valerate were studied in a young woman. A slight increase in serum triglyceride and phospholipid concentrations was seen soon after the oestrogen administration. A marked rise in the serum cortisol concentration was evidently caused by psychic stress on the patient. The EEG examined on the first day after oestrogen administration showed findings typical of subcortical disturbance. One week later the EEG was normal. The low toxicity and slight side effects of a large overdosage of oestradiol valerate by month are worth noting.

Administration, Oral↗
PubMed1983

Effect of N-trifluoroacetyladriamycin-14-valerate on [3H]thymidine uptake and DNA synthesis of human lymphoma cells.

The effects of N-trifluoroacetyladriamycin-14-valerate on the uptake of [3H]thymidine and its incorporation into DNA of human P3HR-1 lymphoma cells were studied. In the absence of the drug, at 0 degrees C, [3H]thymidine was transported into the cells but not incorporated into DNA, as determined by both the trichloroacetic acid-soluble and -precipitable counts obtained with the cells. At 37 degrees C, [3H]thymidine was readily transported into the cells and incorporated into DNA. In the presence of the drug, both [3H]thymidine uptake (as shown by acid-soluble counts) and the amount of its incorporation into acid-precipitable materials were markedly reduced. However, the uptake of [3H]thymidine at 0 degrees C was found to be equally sensitive to drug inhibition as at 37 degrees C. The incorporation at 37 degrees C of [3H]thymidine into acid-precipitable materials of the cells, which had been prelabeled at 0 degrees C with [3H]thymidine, was found to be insensitive to inhibition by the drug. The in vitro activities of DNA polymerases alpha and beta purified from human P3HR-1 cells were also found not to be susceptible to inhibition. Nuclei purified from cells pretreated with the drug continued to synthesize DNA. The cytofluorograms of the cells treated with the drug indicated that the treated cells accumulated at the G2/M phase, whereas the S phase of the cells was not arrested. These results suggest that N-trifluoroacetyladriamycin-14-valerate inhibits [3H]thymidine uptake but not cellular DNA synthesis in human P3HR-1 lymphoma cells.

Cell Line↗
PubMed1980

[Anti-inflammatory effects of prednisolone 17-valerate 21-acetate, a new topical corticosteroid (author's transl)].

Anti-inflammatory activities of prednisolone 17-valerate 21-acetate(PVA) were studied in rats and guinea pigs and results compared with data on topical steroids, such as betamethasone 17-valerate(BV) and hydrocortisone 17-butyrate(HB). PVA given subcutaneously inhibited dose-dependently carrageenin- and kaolin-induced edema. These anti-inflammatory activities of PVA were the weakest among the steroids tested. A local administration of PVA into the site of inflammation, however, had the same or more potent activities than BV and HB in carrageenin-induced edema and paper disk granuloma. Topical application of PVA ointment in carrageenin-induced edema exhibited an inhibitory effect which was dependent on the concentrations (0.1-1.0%). The anti-inflammatory activity of 0.3% PVA ointment was equivalent to that of 0.12% BV ointment. For the other experimental models, i.e. exuberant granulation, croton oil-induced ear edema, passive cutaneous anaphylaxis and tuberculin-induced delayed type hypersensitivity, the activity of 0.3% PVA ointment was the same or somewhat more potent than 0.12% BV and 0.1% HB ointments. The thymolytic activity of PVA ointment in the exuberant granulation model was similar to the activity seen with HB ointment and weaker than of BV ointment. Thus, the anti-inflammatory activities of PVA were equivalent to or more potent than those of BV and HB, and with topical application, the systemic effect of PVA was weaker than the other steroids examined.

Administration, Topical↗
PubMed1980

[Effect of prednisolone 17-valerate 21-acetate on immunological responses in mice (author's transl)].

The in vivo effects of prednisolone 17-valerate 21-acetate (PVA), an anti-inflammatory glucocorticoid on several immunological responses in mice were investigated in comparison with hydrocortisone 17-butyrate (HB) and betamethasone 17-valerate (BV), when given subcutaneously. PVA reduced the spleen weight, the number of splenic nucleated cells, the formation of hemolytic plaque forming cells (PFC), delayed type footpad reaction and the responsiveness of splenic lymphocytes to concanavalin A. These suppressive effects were almost the same as those seen with HB and weaker than those of BV. However, the responsiveness of splenic cells to lipopolysaccharide and circulating IgM antibody response to sheep red blood cells were suppressed by a smaller dose of PVA than that of HB. PVA had no effect on the responsiveness to phytohemagglutinin-P, whereas HB and BV enhanced the phytohemagglutinin-P responsiveness. The suppressive effect of PVA on the host defense to experimental infection with Escherichia coli was weaker than those of HB and BV. From these results, PVA appears to be similar to other glucocorticoids in that it exerts complicated effects on several immunological responses in mice.

Administration, Topical↗
PubMed1981

[Topical anti-inflammatory activity of dexamethasone 17-valerate (author's transl)].

The anti-inflammatory activity of dexamethasone 17-valerate ointment (DV-17, 0.12%) was investigated by topical application in mice and rats, and the effects compared with those of dexamethasone (DX, 0.12%), betamethasone 17-valerate (BV-17, 0.12%), beclomethasone 17,21-dipropionate (BE, 0.025%) and hydrocortisone 17-butyrate (HC, 0.1%) which were prepared with the same ointment base. DV-17 inhibited markedly the superficial inflammation such as increased vascular permeability induced by intradermal injection of histamine or bradykinin in rats and edema induced by a drop of croton oil into the mouse ear. DV-17 also inhibited significantly rat paw edema induced by carrageenin, yeast, nystatin and mustard. The inhibitory activity of DV-17 on those acute inflammatory responses was similar to that of DX and BV-17. In the inhibitory activity on carrageenin induced paw edema, DV-17 was less potent than that of DX when given orally, however was similar to DX in topical application. DV-17 also inhibited granulation tissue proliferation by subcutaneous paper disk implantation and nontreated foot swelling in adjuvant arthritic rats, but the inhibitory activity of DV-17 on the inflammation of these distant areas was lower than that of DX. On the other hand, systemic effects such as decrease in weight of adrenal or thymus and body weight loss were most evident in the case of DX and lower with DV-17. DV-17 prolonged wound healing and inhibited the delayed-type hypersensitivity induced by picryl chloride. The activity was equivalent to that of DX and BV-17. From the above results, it may be considered that DV-17 possesses potent anti-inflammatory activity, whereas it has fewer side effects and is a useful glucocorticoid for external application.

Administration, Topical↗
PubMedDate not supplied

Possible relevance of N-trifluoroacetyladriamycin (AD 41) in the antitumoral activity of N-trifluoroacetyladriamycin-14-valerate (AD 32) in tumor-bearing mice. I. Pharmacokinetic evidence.

N-Trifluoroacetyladriamycin-14-valerate (AD 32) is an analog of doxorubicin whose chemico-physical characteristics are nontypical compared to the parent compound. Its most interesting feature is the lack of capacity to intercalate with DNA; thus, its mechanism of action as an antitumoral drug is still unknown. The N-trifluoroacetyl bond on the glycoside moiety is very stable and does not easily undergo enzymatic hydrolysis. Conversely, the valerate ester is split very rapidly by tissue and blood hydrolases. In this paper we present a kinetic study on AD 32, and we additionally follow the formation and disappearance of its metabolite, N-trifluoroacetyladriamycin (AD 41). Peak levels, areas under the curve, and beta-half-lives of AD 32 and AD 41 after an iv injection of 80 mg/kg of AD 32 to Lewis lung carcinoma-bearing mice are presented. The results indicated very rapid disappearance of AD 32 from blood and tissues, whereas AD 42 persisted for much longer. Moreover, all of the tissues taken into consideration were able to hydrolyze AD 32 to AD 41, suggesting that this compound plays an important role in the antitumoral activity of AD 32.

Animals↗
PubMed1976

[Multicentre-clinical trial of the novel corticosteroid diflucortolone valerate in the forms of cream, ointment and fatty ointment. Part II: Comparative study with several commercial preparations (author's transl)].

6alpha,9-Difluoro-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadiene-3,20-dione (diflucortolone valerate, Nerisona) in the forms of cream, ointment and fatty ointment was investigated against 5 commercial preparations with beta-methasone-17-valerate, fluocinonide, fluocinolone acetonide, flumetasone pivalate and desoximetasone in 15 simultaneously conducted and multicentre-clinical studies-all on double-blind contralateral studies-involving a total of 1923 patients. The Nerisona preparations proved to be highly effective-particularly in eczematous diseases- and comparable to the above-mentioned commercial preparations. Nerisona ointment was shown to be superior to flumetasone cream. The statistical reliability of such data is discussed.

Administration, Topical↗
PubMed1979

Combination therapy for psoriasis. Psoralens plus long-wave ultraviolet radiation with betamethasone valerate.

In the treatment of psoriatic patients with psoralens plus long-wave ultraviolet radiation (PUVA), clearing of psoriatic lesions was obtained more quickly and with smaller doses of ultraviolet light when topically applied corticosteroid therapy was added. Twelve patients with symmetrical plaque-type psoriasis were given PUVA on one side of the body and PUVA plus betamethasone valerate on the other side in a paired comparison study. Ten of the patients had faster clearing of lesions on the side that was treated with PUVA and betamethasone than on the side treated with PUVA alone. The other two patients had equal clearing on both sides. All patients remained clear of lesions during maintenance with PUVA alone for at least five months after steroid therapy was discontinued. Combination therapy may save the patient time, expense, and unnecessary exposure to radiant energy.

Adult↗
PubMed1979

Physical model evaluation of topical prodrug delivery-simultaneous transport and bioconversion of vidarabine-5'-valerate II: Parameter determinations.

Results of initial studies on methods for determining various model parameters are reported. By employing excised hairless mouse skin in a diffusion cell system, numerous model parameter values were deduced. The stratum corneum permeability was estimated from steadystate fluxes with preparations of heat-separated epidermal membranes. Determinations of dermis diffusivities and enzyme rate constants in situ involved considering the simultaneous transport and the enzyme processes and factoring the diffusivities and enzyme rate constants from the overall kinetics. Dermal diffusivities were on the order of 10-6 cm2/sec for vidarabine and its 5'-valerate ester. The enzyme rate constants were 1.70 x 10-3 sec-1 for the esterase and 8.68 x 10-3 sec-1 for the deaminase.

Animals↗
PubMed1994

Significance of viable skin layers in percutaneous permeation and its implication in mathematical models: theoretical consideration based on parameters for betamethasone 17-valerate.

The role of viable skin layers (viable epidermis and dermis) is examined by the three-layer model using parameter values for betamethasone 17-valerate. The mathematical three-layer diffusion model indicates that the lag time and half-life after vehicle removal in epidermis and split-thickness skin are longer than those in stratum corneum without viable layers, even if drug flux at steady-state is minimally altered. The theoretical values of the lag time and half-life predicted for epidermis and split-thickness-skin samples are compatible with the values observed in another in vitro study. The results predicted by the three-layer model indicate that the simplified model (single-layer or compartment model), which regards the whole skin as one diffusion layer or one compartment, may be warranted because all three skin layers have the same half-life after vehicle removal. The parameters used in the simplified model are estimated from some of the following values directly obtainable in the experiment: flux from skin and amount in the whole skin at steady-state, lag time, and drug concentration or amount maintained to be unchanged in the donor site. However, the simplified model often cannot resolve some discrepancy between the data and model (e.g., the ratio of the half-life to lag time) even if the data may be explained by the three-layer model.

Betamethasone Valerate↗
PubMed2003

Differential-pulse polarography (DPP) determination of betamethasone valerate in dosage form.

The electrochemical reduction of betamethasone valerate (BV) in a pharmaceutical formulation containing neomycin has been carried out in Britton-Robinson buffer (BRB) (0.04 mol L(-1)) by differential-pulse polarography (DPP). BV exhibits a well-defined irreversible reduction peak at -1.03 V/ref. The influence of pH on the reduction of BV was studied in Britton-Robinson buffer (pH range 1.7-10). A method for the analysis of BV in BRB (0.04 mol L(-1)), which allows quantification over the range 3.9x10(-6)-1.1x10(-4) mol L(-1), was proposed and successfully applied to the determination of BV in tablets with mean recovery and relative standard deviation of 100.81% and 0.45%, respectively.

Betamethasone Valerate↗
PubMed2001

Betamethasone valerate foam for treatment of nonscalp psoriasis.

BACKGROUND: Although betamethasone valerate (BMV) foam, 0.12% (Luxiq, Connectics Corporation, Palo Alto, CA) is approved by the Food and Drug Administration for the treatment of corticosteroid-responsive scalp dermatoses, no data are available for its use on nonscalp psoriasis. OBJECTIVE: We evaluated the safety and efficacy of BMV foam in treating psoriatic lesions at nonscalp sites. METHODS: We conducted a randomized, double-blind, placebo-controlled, paired-comparison, split-body study of 40 patients with mild to moderate plaque-type psoriasis. Patients applied BMV foam and placebo foam twice daily for 12 weeks. RESULTS: At the end of the treatment period, 70% of patients had greater than 50% improvement of lesions on their active foam-treated side compared with 24% of patients with similar improvement on their placebo foam-treated side. Adverse effects were limited to temporary stinging, burning, or itching in several patients. Three patients (7.5%) withdrew because of stinging or itching. CONCLUSIONS: The results indicate that BMV foam is effective against nonscalp psoriasis. Twice-daily applications are well tolerated, compliance exceeds 90%, cosmetic characteristics are acceptable, and the medication may reduce the need for multiple prescriptions.

Administration, Topical↗
PubMed1977

Action of 5-(2-thienyl)valeric acid as a biotin antagonist.

5-(2-Thienyl)valeric acid (TVA), a biotin analogue which can be easily prepared through chemical process, inhibited the growth of a biotin synthesizing Rhodotorula glutinis. The growth inhibition was reversed by the addition of biotin. Among biotin intermediates, dethiobiotin and 7,8-diaminopelargonic acid reversed the inhibition by TVA, while 7-keto-8-amino-pelargonic acid and pimelic acid did not. From these results, it was concluded that TVA is a biotin antagonist which probably acts as an inhibitor of biotin biosynthesis.

Biotin↗
PubMed2003

Rat NTE-related esterase is a membrane-associated protein, hydrolyzes phenyl valerate, and interacts with diisopropylfluorophosphate through a serine catalytic machinery.

The serine hydrolases constitute multi-families of proteins that include lipases, esterases, and proteases. These enzymes contain a signature motif GXSXG, in which the serine residue acts as the nucleophile and initiates catalysis. This report describes the characterization of a novel serine hydrolase from rat. This enzyme exhibits a moderate sequence identity with the neuropathy target esterase (NTE), thus is designated NTE-related esterase (NRE). Transfection with the NRE cDNA resulted in marked increases in the hydrolysis of phenyl valerate and reactivity with diisopropylfluorophosphate. Such increases, however, were markedly or completely abolished in mutants that had a substitution (Ala, Cys, Asp, or His) on the serine residue in the GXSXG motif, providing direct evidence that NRE is a serine hydrolase. By Northern blot analyses, three NRE transcripts were detected and they differed markedly in length (approximately 2.6, 4.2, and 5.0 kb). The 4.2-kb transcript was present in all organs analyzed except the testis, in which both 2.6- and 5.0-kb transcripts were detected. The testicular transcripts were completely depleted in rats treated with clofibrate, whereas the levels of NRE mRNA in the liver were markedly increased in rats treated with perfluorodecanoic acid. Both clofibrate and perfluorodecanoic acid are efficacious activators of the peroxisome proliferator activated receptor-alpha (PPAR-alpha). The differential effects on the levels of NRE mRNA suggest that these chemicals regulate the expression of NRE through mechanism(s) rather than the activation of PPAR-alpha.

Amino Acid Sequence↗
PubMed1994

Peroxisome proliferation of hepatocytes in rats by a microbial degradation product of cholic acid, 4-(decahydro-6-methyl-3-oxocyclopenta(f)quinoline-7-yl)valeric acid.

Three-week oral administration of 4-(decahydro-6-methyl-3-oxo-cyclopenta(f)quinoline-7-yl)valeric acid (32-1328) in the diet supplemented at concentrations of 0.1% or 0.3% was associated with hepatomegaly and hypotriglyceridemia in male F344 rats. Electron microscopic examination of the liver revealed a remarkable increase of peroxisomes in hepatocytes both in number and size. Biochemically, there were increased activities of peroxisomal marker enzymes including the heat-labile enoyl-CoA hydratase and catalase while the mitochondrial enoyl-CoA hydratase activity was unchanged after feeding of 32-1328. These findings indicate that 32-1328 can exert peroxisome-proliferating activity to rat liver in a manner similar to typical peroxisome proliferators such as clofibrate or di(2-ethylhexyl)phthalate.

Animals↗