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PubMed1976

Increased insulin binding by lymphocyte receptors induced by beta-OH butyrate.

The serum concentration of ketones increases in both fasting and diabetic ketoacidosis. Whether ketones alter, independent of changes in pH, in number and affinity of insulin receptors is not known. The binding of insulin 125I by 24 X 10(6)IM-9 lymphocyte cells was examined in both the presence and absence of 8 mM beta-OH butyrate. Studies were conducted at multiple concentrations of insulin. A consistent increase of insulin binding was induced by beta-OH butyrate. The mean maximum increase of insulin binding was 35%, which achieved significance at the 1% level.

Acidosis↗
PubMed1978

Gamma-amino-beta-hydroxy butyric acid stimulates prolactin and growth hormone release in normal women.

The influence of gamma-amino-beta-hydroxy butyric acid (GABOB) treatment on pituitary function has been investigated in this study. Different doses (50 x 100 mg) of GABOB were iv injected into three and six normal women, respectively. PRL and GH plasma levels were measured before and after the injection. The treatment with 150 mg GABOB, performed in another two normal women, was interrupted because of side-effects (loss of consciousness etc.) due to the treatment. The treatment with 50 mg GABOB did not induce significant variations of the two hormones; however, significant increases of PRL (P less than 0.05) and GH (P less than 0.01) plasma levels were observed after injection with 100 mg GABOB. The present data suggest that gamma-amino butyric acid (GABA) itself of GABAergic drugs might play an important role in the control of hypothalamic-pituitary function.

Adolescent↗
PubMed1981

[Pharmacological study on hydrocortisone 17-butyrate 21-propionate (author's transl)].

The topical and systemic anti-inflammatory activities of hydrocortisone 17-butyrate 21-propionate (HBP) were studied. The systemic anti-inflammatory activities of HBP and reference steroids were examined for their effects on dinitrochlorobenzene dermatitis, carrageenin edema, cotton pellet granuloma and adjuvant arthritis in rats and by the delayed allergic edema test in mice. The topical anti-inflammatory activities of these steroids were examined for their effects on croton oil dermatitis, croton oil ear edema, carrageenin edema and cotton pellet granuloma in rats. Furthermore, effects of these steroids on liver glycogen deposition in mice, thymolysis, and decrease of serum corticosterone level in rats were examined. Systemically administered HBP was less potent than betamethasone 17-valerate (BV), but was almost equal to hydrocortisone 17-butyrate (HB) in anti-inflammatory activity, and its effects on liver glycogen deposition, thymolysis, and the decrease of serum corticosterone level. However, the topical anti-inflammatory activity of HBP was more potent than that of BV and HB, although in the same experiment, thymolytic activity of HBP was less potent than that of BV, but was almost equal to HB. The inhibitory effect of HBP on hypotonic induced hemolysis was weaker than that of BV, but was stronger than that of HB in vitro. The affinity of HBP was higher than that of BV and HB to polymorphonuclear leucocytes used as the inflammatory cells in vitro. On the other hand no marked difference was observed in the affinity to erythrocytes used as the non-inflammatory cells in vitro. These results suggest that HBP is a useful drug which has superior topical anti-inflammatory activity, but has a weak systemic effect.

Animals↗
PubMed1985

Characteristics of binding of a new anti-inflammatory glucocorticoid, hydrocortisone 17-butyrate 21-propionate (HBP), to glucocorticoid receptors of rat liver.

Characteristics of the specific binding of hydrocortisone 17-butyrate 21-propionate (HBP) to the cytoplasmic fraction from rat liver were investigated. The inhibition constant (Ki) of HBP for the site of 3H-dexamethasone (3H-DM) binding was approximately equal to the value of DM and significantly smaller than that of hydrocortisone (HC). The maximum number of binding sites (Bmax) and dissociation constant (Kd) for 3H-HBP were also approximately equal to those for 3H-DM. The Scatchard and Hofstee plots analyses of 3H-HC binding indicated that the HC binding sites consisted of three components with different affinity, while that of 3H-DM had only one site with an intermediate affinity. HBP and hydrocortisone 17-butyrate (HB) bound to other binding sites of HC in addition to the site for DM. The IC50 value for synthetic glucocorticoids determined from the inhibition curves of 3H-HC binding in the first phase agreed with the values determined by the displacement study of 3H-DM binding. Furthermore, the first phase of HBP in the inhibition curve of 3H-HC binding disappeared from the curve, and only the second phase remained following the addition of DM. These results indicate that the esterification of C-17 and C-21 OH increases the affinity of the binding site for synthetic glucocorticoid and attenuates the affinity for the other binding sites of HC.

Adrenalectomy↗
PubMed1980

[Studies on toxicity of clobetasone-17-butyrate (II)--chronic toxicity in rats (author's transl)].

Chronic toxicity of clobetasone-17-butyrate, an anti-inflammatory corticosteroid, was investigated in rats. Subcutaneous administration with the drug at dose of 0.003, 0.01 and 0.03 mg/kg/day for three and six months induced no significant changes in the rats. At 0.1 and 0.3 mg/kg/day, however, some dose-dependent symptoms such as suppression of body weight gain, emaciation, regressive changes in adrenals, lymphatic and hematopoietic tissues, decrease in circulating white blood cell and lymphocyte counts, which have been known as toxic effects of synthetic corticosteroids, were induced. The results indicates that the maximum no-toxic dose of clobetasone-17 butyrate was 0.03 mg/kg/day on this experimental condition. In the recovery test for two months no significant differences in the treated rats from controls were found, suggesting that the toxic effects were reversible in the animals treated at 0.3 mg/kg/day and lower than that.

Adrenal Glands↗
PubMed1981

[Studies on toxicity of hydrocortisone 17-butyrate 21-propionate -2. Subacute toxicity in rats by subcutaneous administration (author's transl)].

Subacute toxicity of hydrocortisone 17-butyrate 21-propionate (HBP), a new synthetic corticosteroid, was studied in rats, using betamethasone 17-valerate (BV) and hydrocortisone 17-butyrate (HB) as the reference drugs. HBP was subcutaneously injected to rats at the daily doses of 0.08, 0.4, 2.0, 10 and 50 mg/kg for 30 days. BV and HB were also administered at the daily doses of 0.08, 0.4 and 2.0 mg/kg. The recovery test was performed for 4 weeks after administration of HBP, BV and HB. The suppression of body weight gain by HBP was observed at the doses more than 0.08 mg/kg in male and more than 2.0 mg/kg in female rats. In addition, at the doses more than 0.4 mg/kg of HBP induced the dose-dependent symptoms such as decrease in the number of circulating white blood cells, lymphocyte counts and S-ALP level, increase in total cholesterol, GOT and GPT level of serum, and regressive changes in adrenals, lymphatic and hematopoietic tissues. There were fatal cases in rats given 50 mg/kg of HBP. These changes are considered to be common phenomena to other corticosteroids, and less toxic in female than male rats. Changes of symptoms caused by the administration of HBP 2.0 mg/kg were almost recovered after withdrawal. The toxicities of three corticosteroids were in the order of BV greater than HB greater than or equal to HBP in strength. As the result, maximum non-toxic dose of HBP was estimated to be 0.08 mg/kg in female and lower than that in male rats.

Administration, Topical↗
PubMed1981

[Studies on toxicity of hydrocortisone 17-butyrate 21-propionate -4. Chronic toxicity in rats by subcutaneous administration (author's transl)].

Chronic toxicity of hydrocortisone 17-butyrate 21-propionate (HBP), a new synthetic corticosteroid, was studied in rats. HBP was subcutaneously injected to rats as the daily doses of 0.001, 0.01, 0.01, 1.0 and 3.0 mg/kg for 6 months, and the following recovery test was carried out for 4 weeks. Hydrocortisone 17-butyrate (HB) and betamethasone 17-valerate (BV) were used as the reference drugs at the doses of 0.1, 1.0 and 3.0 mg/kg. The suppression of body weight gain by the administration of HBP was observed at the doses more than 1.0 mg/kg in male and more than 0.1 mg/kg in female, and the dead animals were sent at the highest dose of HB and BV. Mainly at the doses more than 0.1 mg/kg HBP induced the dose-dependent symptoms such as decrease in the number of white blood cells and total protein level in serum, and increase in total cholesterol, GOT and GPT level in serum, and atrophic changes of adrenals, lymphatic tissues, skin and subsexual organs. No usual abnormality was recognized at the doses less than 0.01 mg/kg of HBP. These symptoms were more toxic in male, and the strength of toxicity was in the order of BV greater than HB greater than HBP. Many of these findings have known as common effects of corticosteroids. The changes observed in this study were almost recovered after withdrawal of HBP at the doses less than 0.1 mg/kg. As the result, it was suggested that the maximum non-toxic dose of HBP was 0.001 mg/kg.

Administration, Topical↗
PubMed1981

[Studies of toxicity of hydrocortisone 17-butyrate 21-propionate -5. Chronic toxicity in rats by percutaneous administration (author's transl)].

Chronic toxicity of a new synthetic corticosteroid, hydrocortisone 17-butyrate 21-propionate (HBP), was investigated in rats of both sexes. HBP was percutaneously given to rats with 0.1%, 0.5% cream and ointment at the daily dose level of 150 mg per 100 g body weight for 6 months. For the comparison, the percutaneous toxicity with 0.12% betamethasone 17-valerate (BV) cream and ointment, and 0.1% hydrocortisone 17-butyrate (HB) cream and ointment at the daily dose level of 150 mg per 100 g body weight were studied. Rats receiving HBP showed the dose-dependent changes such as the suppression of body weight gain and food intake, emaciation, decrease in the number of white blood cells and lymphocytes, total protein, increase in the number of red cells, hematocrit, hemoglobin, blood sugar and total cholesterol, regressive changes in adrenal cortex, lymphatic and hematopoietic tissues and skin, and gastric erosion, which have been well known as toxic effects of synthetic corticosteroids. These findings were comparatively high toxic in male, and almost disappeared in rats elapsed recovery time of month after withdrawal of HBP. The toxicities of HBP, BV and HB were qualitatively same. However, the grade of effects of HBP toxicity was similar to that of HB, weaker than of BV.

Administration, Topical↗
PubMed1976

Comparison of desoximetasone and hydrocortisone butyrate in psoriasis.

Thirty psoriatics were treated for 2 weeks on a double-blind controlled basis with desoximetasone (0.25%) and with hydrocortisone butyrate (0.1%). It was a randomised left-right comparative trial. Thirteen out of 27 patients preferred desoximetasone, 3 patients preferred hydrocortisone butyrate. There was also a significantly better effect of desoximetasone as judged by the observer after the second week of treatment.

Administration, Topical↗
PubMed1994

Colostral milk fat percentage and pig performance are enhanced by feeding the leucine metabolite beta-hydroxy-beta-methyl butyrate to sows.

Three trials were conducted to test whether feeding the leucine metabolite beta-hydroxy-beta-methyl butyrate (HMB) would increase fat content of sows' milk and pig weight gain. All sows received a basal diet and were assigned at random to receive either 2 g of CaCO3/d (control) or 2 g of Ca(HMB)2/d (HMB), which was top-dressed to the basal diet. Treatment began 3 to 4 d before farrowing. In Trials 1, 2, and 3 there were 4, 19, and 11 pairs of sows, respectively. In a combined analysis that included all three trials, milk fat at d 1 was increased by 41% (P = .01) and pig weight at d 21 was increased by 7% (P = .01) for sows fed diets containing HMB compared with sows fed control diets. Sows fed HMB lost more backfat (P = .03); however, sows receiving HMB had more (P < .05) backfat depth at farrowing than control sows. At weaning there was no difference in backfat depth between the treatment groups. Sows fed HMB tended to consume less feed (P = .07) than control sows. In Trials 2 and 3, data were collected on the subsequent reproductive cycles of the sows. A combined analysis of the data revealed no differences in sow performance when sows previously fed the diet containing HMB were compared with sows previously fed the control diet. In conclusion, beta-hydroxy-beta-methyl butyrate, when fed to sows at 2 g/d, resulted in an increase in fat percentage of sow's milk and pig performance.(ABSTRACT TRUNCATED AT 250 WORDS)

Adipose Tissue↗
PubMed1982

Anti-oxidative effects of vitamin B2-butyrate on the cardiac mitochondrial disorders induced by adriamycin.

The combined use of CoQ10 with adriamycin has been recommended for reduction of the cardiotoxicity that occurs during cancer chemotherapy. Vitamin B2-butyrate was also investigated in order to determine anti-oxidative effects on adriamycin cardiotoxicity. This vitamin analysis prevented enhanced lipid peroxidation and rectified the respiratory disorders of heart mitochondria induced by adriamycin, however, the deficiency of the CoQ10-pool was not rectified. The combined approach of using CoQ10 for rectifying the deficiency of this component and of using B2-butyrate for reducing lipid peroxidation was indicated for adriamycin cancer chemotherapy.

Animals↗
PubMed1976

The central effect of 5-hydroxytryptamine, gamma-amino-butyric acid and carbachol on thermoregulation in the neonatal guinea pig.

5-Hydroxytryptamine (10 microgram), gamma-amino-butyric acid (20 microgram) and carbachol (1 microgram) were injected through the soft skull into the lateral cerebral ventricle of guinea pigs aged 2 to 12 days, at the slightly subneutral ambient temperature of 30 degrees C. 5-Hydroxytryptamine (5-HT) produced no immediate change in oxygen consumption, whereas colonic temperature fell rapidly. One hour after injecting 5-HT, when colonic temperature had decreased by about 0.5 degrees C, oxygen consumption increased and after a lag of 30--40 min was followed by an increase in colonic temperature. Gamma-amino-butyric acid (GABA) increased oxygen consumption and colonic temperature after a latency of 30--60 min. Carbachol was followed by an immediate decrease in colonic temperature and oxygen consumption. Colonic temperature was below the pre-injection level throughout the five-hour period of observation.

Aminobutyrates↗
PubMedDate not supplied

Anti-inflammatory properties of tixocortol 17-butyrate,21-propionate (JO 1222), a novel, locally acting corticosteroid.

Tixocortol 17-butyrate,21-propionate (JO 1222) is a novel, locally acting, C-21 thioester-linked corticosteroid with significant activity in a number of models of inflammation. In models of acute inflammation, JO 1222 had an ED30 of 3 micrograms in carrageenan-induced oedema, an ED50 of 5 ng in croton oil-induced inflammation, and 4 micrograms and 2 micrograms/pleural cavity in carrageenin-induced pleurisy in the rat and mouse respectively. In a model of subchronic inflammation JO 1222 had an ED50 of 39 micrograms/pellet (cotton pellet-induced granuloma) and an ED50 of 13 ng in oxazolone-induced hypersensitivity. The overall relative potency was found to be beclomethasone DP greater than betamethasone DP = JO 1222 greater than hydrocortisone 17-butyrate,21-propionate greater than hydrocortisone acetate. In contrast to any of the other corticosteroids, including beclomethasone DP, JO 1222 did not have any marked systemic effects in any of the above models following oral or local administration. Furthermore, in contrast to other locally acting corticosteroids such as beclomethasone DP, JO 1222 had little or no effect on the thymus or body weight. These findings suggest that JO 1222 is a novel, potent, locally acting corticosteroid with little or no systemic effects and thus has therapeutical potential in diseases such as asthma, arthritis, ulcerative colitis and rhinitis.

Adrenal Cortex Hormones↗
PubMedDate not supplied

Liquid chromatographic determination of clobetasone-17-butyrate in ointments.

A liquid chromatographic (LC) method has been developed for determination of clobetasone-17-butyrate in ointment using clobetasone propionate as an internal standard. Separation was carried out on a C18 reverse-phase column using water-methanol as a mobile phase. Methylparaben and propylparaben (both sodium salt) used as preservatives did not interfere with separation. Compounds are detected photometrically at 235 nm. Mean assay results for 0.05% commercial ointments were 100.36% (n = 5). Mean recovery of clobetasone-17-butyrate added to commercial ointment was 99.89%.

Administration, Topical↗
PubMed1986

Hydrolysis of hydrocortisone 17-butyrate 21-propionate by cultured human keratinocytes.

Hydrolysis of 17-butyrate 21-propionate (HBP) by human keratinocytes was studied using an in vitro system. In the culture of human keratinocytes 1.308 nmole/ml of hydrocortisone 17-butyrate (de-esterified HBP at the position of 21) was found at 1 h after the addition of 10 nmole/ml HBP. At 6 h most of HBP was de-esterified to become HB17 and a small amount of hydrocortisone 21-propionate (de-esterified HBP at the position of 17) was detected. Hydrocortisone (HC) was not detectable. These results indicate that when HBP is applied on the skin, it is hydrolyzed at the position of 21, and reaches the dermis where it finds the way to get into the systemic circulation. The intracellular concentration of HBP was estimated to be more than 5 times its extracellular concentration and its accumulation was higher than HC. These results were discussed in relation to the potentiation of local antiinflammatory action and the reduction of systemic effects of topical glucocorticoid.

Administration, Topical↗
PubMed1986

Determination of ketone body kinetics using a D-(-)-3-hydroxy[4,4,4-2H3]butyrate tracer.

In studies where D-(-)-3-hydroxy[4,4,4-2H3]butyrate is employed as isotopic tracer in vivo, we have described a selected ion monitoring, gas-liquid chromatography-mass spectrometry micromethod which measures [2H3] tracer enrichment in 3-hydroxybutyrate and acetoacetate from 300-microliters blood samples. For plasma samples in the physiologic range, intra- and interassay precisions for each ketone averaged better than +/- 1% and +/- 2%, respectively. The use of the method was validated by comparing kinetic data obtained with the above tracer with simultaneous flux data obtained with conventional D-(-)-3-hydroxy[3-14C]butyrate tracer in five fasted rats.

3-Hydroxybutyric Acid↗
PubMed1982

[Synthetic inhibitors of serine proteinases. Part 26: Inhibition of trypsin, plasmin and thrombin by amides of N alpha-arylsulfonylated 2-amino-4-(4-amidino-phenyl) butyric acid and 2-amino-5-amidinophenyl valeric acids (author's transl)].

Among the derivatives of the N alpha-arylsulfonylated omega-amidinophenyl-alpha-aminoalkyl carboxylic acids, the primary amides of N alpha-arylsulfonylated 2-amino-4-(4-amidinophenyl) butyric acid proved to be compounds with strong antiplasmin and antitrypsin activity, they exert, however, only slight inhibitory effect on thrombin. So far, no benzamidine derivatives with strong inhibitory effects on plasmin but with weak antithrombin activity have been known. The secondary amides of the N alpha-arylsulfonylated 2-amino-4-(4-amidinophenyl)butyric acid possess slight inhibitory effects, the corresponding derivatives of 2-amino-5-amidinophenyl valeric acids, however, are potent inhibitors of thrombin.

Amidines↗
PubMed1996

A comparison of fluticasone propionate ointment, 0.005%, and hydrocortisone-17-butyrate ointment, 0.1%, in the treatment of psoriasis.

The efficacy and safety of twice-daily topical application of fluticasone propionate ointment, 0.005%, and hydrocortisone-17-butyrate ointment, 0.1%, were compared in 113 adult patients with moderate-to-severe psoriasis in a multicenter, double-blind, randomized, parallel study. The majority of patients had psoriatic involvement of long duration over a large body surface area (mean, 17%). The following efficacy assessments were made at weekly intervals for up to four weeks following initiation of treatment: physician's gross assessment of clinical response of the target lesion; severity of psoriatic signs and symptoms; and patients' assessment of treatment effects. Safety was assessed by monitoring and reporting any adverse events that occurred during the study. Fluticasone propionate ointment, 0.005%, was found to be therapeutically superior to hydrocortisone-17-butyrate ointment, 0.1%, as well as safe and well tolerated. Its onset of action was rapid and no systemic adverse effects occurred. Overall patients experienced progressive improvement with fluticasone propionate ointment, 0.005%.

Administration, Topical↗