Terpenoids with quinoid structures are found as natural products. This includes steroidal quinones, quinones with a secosteroid structure and meroterpenoid quinones. Importantly, catechol estrogens as endogenous metab...Terpenoids with quinoid structures are found as natural products. This includes steroidal quinones, quinones with a secosteroid structure and meroterpenoid quinones. Importantly, catechol estrogens as endogenous metabolites of estradiol and estrone are precursors of reactive quinones and semiquinones, which are thought to contribute to estrogen-induced carcinogenesis. On the other hand, a number of quinones that include substituted naphthoquinones and anthraquinones are highly cytotoxic and have been used in cancer treatment. This makes the structures interesting synthetic targets. The following is a review of important natural and synthetic terpenoid and steroid quinone hybrids.展开更多
Background:Strength-trained athletes using anabolic androgenic steroids(AAS)have left ventricular(LV)hypertrophy and myocardial fibrosis that can lead to sudden cardiac death.A similar feature was described in athlete...Background:Strength-trained athletes using anabolic androgenic steroids(AAS)have left ventricular(LV)hypertrophy and myocardial fibrosis that can lead to sudden cardiac death.A similar feature was described in athletes with hypertrophic cardiomyopathy(HCM),which complicates the diagnosis for clinicians.In this context,we aimed to compare the LV function of the 2 populations by measuring global and regional strain and myocardial work using speckle-tracking imaging.Methods:Twenty-four strength-trained asymptomatic athletes using AAS(AAS-Athletes),22 athletes diagnosed with HCM(HCM-Athletes),and 20 healthy control athletes(Ctrl-Athletes)underwent a resting echocardiography to assess LV function.We evaluated LV global and regional strains and myocardial work,with an evaluation of the constructive work(CW),wasted work,and work efficiency(WE).Results:Compared to Ctrl-Athletes,both AAS-Athletes and HCM-Athletes had a thicker interventricular septum,with maj ored values in HCM-Athletes.LV strain was reduced in AAS-Athletes and even more in HCM-Athletes.Consequently,global WE was significantly diminished in both AAS and HCM-Athletes(93%±2%in Ctrl-Athletes,90%±4%in AAS-Athletes,and 90%±5%in HCM-Athletes(mean±SD);p<0.05).Constructive work and WE regional analysis showed specific alterations,with the basal septal segments preferentially affected in AAS-Athletes,and both septal and apical segments affected in HCM-Athletes.Conclusion:The regional evaluation of myocardial work reported specific alterations of the major LV hypertrophy induced by the regular use of AAS compared to the LV hypertrophy due to HCM.This finding could help clinicians to differentiate between these 2 forms of pathological hypertrophy.展开更多
Eosinophilic esophagitis(EoE)is an emerging chronic local immune-mediated disease of the esophagus.Beside proton pump inhibitors and food-restrictiondiets swallowed topical corticosteroids(STC)can be offered as a firs...Eosinophilic esophagitis(EoE)is an emerging chronic local immune-mediated disease of the esophagus.Beside proton pump inhibitors and food-restrictiondiets swallowed topical corticosteroids(STC)can be offered as a first line therapy according to current guidelines.This review describes the background and practical management of STCs in EoE.So far,mainly asthma inhalers containing either budesonide or fluticasone have been administered to the esophagus by swallowing these medications“off label”.Recently esophagus-targeted formulations of topical steroids have been developed showing clinicopathological response rates up to 85%-an orodispersible tablet of budesonide has been approved as the first“in label”medication for EoE in Europe in June 2018.Whereas it was shown that disease remission induction of EoE by STCs is highly effective,there is still a lack of data regarding long-term and maintenance therapy.However,current studies on STC maintenance therapy add some movement into the game.展开更多
Non-traumatic osteonecrosis is a cause of joint pain and deformity, not uncommonly caused by corticosteroid use. Despite this, corticosteroid induced osteonecrosis is poorly represented in the literature. We performed...Non-traumatic osteonecrosis is a cause of joint pain and deformity, not uncommonly caused by corticosteroid use. Despite this, corticosteroid induced osteonecrosis is poorly represented in the literature. We performed a detailed review of corticosteroid induced osteonecrosis, including aetiology, prevention, screening, clinical presentation, investigations, staging systems and treatment. We present this in the context of a patient at our institution who developed bilateral hip, shoulder and knee osteonecrosis following high dose corticosteroid therapy for dermatomyositis.展开更多
Diabetic macular edema(DME)is a common cause of visual impairment in diabetic patients.It is caused by an increase in the permeability of the perifoveal capillaries and a disruption of the blood retinal-barrier.The pa...Diabetic macular edema(DME)is a common cause of visual impairment in diabetic patients.It is caused by an increase in the permeability of the perifoveal capillaries and a disruption of the blood retinal-barrier.The pathogenesis of DME is multifactorial.Several therapeutic modalities have been proposed for the treatment of DME.Corticosteroid treatments have emerged as an alternative therapy for persistent DME or refractory to conventional laser photocoagulation and other modalities,due to anti-inflammatory,anti-vascular endothelial growth factor and anti-proliferative effects.Many studies have demonstrated the beneficial therapeutic effect of corticosteroids with improvement to both retinal thickness and visual acuity in short-term on the treatment of DME.Peribulbar and intravitreal injections have been used to deliver steroids for DME with frequent injections due to the chronic and recurrent nature of the disease.Steroid-related side effects include elevated intraocular pressure,cataract,and injection related complications such as endophthalmitis,vitreous hemorrhage,and retinal detachment particularly with intravitreal steroid injections.In order to reduce the risks,complications and frequent dosing of intravitreal steroids,intravitreal implants have been developed recently to provide sustained release of corticosteroids and reduce repeated intravitreal injections for the management of DME.展开更多
Objective:To determine the chemical profile and steroids composition of the medicinally important plant Aerva lanata(A.lanata) L.Methods:Preliminary phytochemicul screening was done by the method as Harborne described...Objective:To determine the chemical profile and steroids composition of the medicinally important plant Aerva lanata(A.lanata) L.Methods:Preliminary phytochemicul screening was done by the method as Harborne described.HPTLC studies were canied out as Harborne and Wagner et al described.The Ethyl acetate-ethanol-water(8:2:1.2) was employed as mobile phase for glycosides.Results:The desired aim was achieved using Chloroform-acetone(8:2) as the mobile phase.The methanolic extract of stem,leaves,root,flower and seeds of A.lanata showed the presence of 30 different types of steroids with 30 different Rf values from 0.04 to 0.97. Maximum number(11) of steroids has been observed in leaves followed by root(10).Conclusions: HPTLC profile of steroids has been chosen here to reveal the diversity existing in A.lanata.Such finger printing is useful in differentiating the species from the adulterant and act as biochemical markers for this medicinally important plant in the pharma industry and plant systematic studies.展开更多
BACKGROUND: Alcoholic hepatitis (AH) is a necrotizing inflammatory process caused by alcoholic liver injury. It carries a significant short-term mortality. The management of AH is challenging. Although corticosteroids...BACKGROUND: Alcoholic hepatitis (AH) is a necrotizing inflammatory process caused by alcoholic liver injury. It carries a significant short-term mortality. The management of AH is challenging. Although corticosteroids have been demonstrated to exert anti-inflammatory and antifibrotic effects, their efficacy for the treatment of AH remains debatable. DATA SOURCES: A literature search was performed of MEDLINE, ScienceDirect, SpringerLink and Wiley InterScience using the key words "alcoholic hepatitis", "alcoholic liver disease", and "corticosteroids". The available data reported in the relevant literature were analyzed. RESULTS: More than 17 controlled trials and at least 13 meta-analyses have reported the efficacy of corticosteroids in the treatment of AH in the past 40 years. Many were poorly designed and used different inclusion/exclusion criteria, making it difficult to reach a consensus. In this review, we summarized all the controversial data in the past decade and analyzed the potential causes for the varying therapeutic effects of corticosteroids in AH. The focus of the controversy has changed from "whether steroids are beneficial or harmful for AH patients" to "how to accurately identify responders to steroids early and rationalize corticosteroid treatment". An early response to glucocorticoids, as determined by calculating the Lille score after 7 days of treatment, has been shown to be a clinically useful indicator. Moreover, down-regulation of steroid sensitivity, risk of infection, and a rational therapeutic strategy of corticosteroids in AH patients are all crucial for therapeutic effect.CONCLUSIONS: An early and accurate determination of steroid sensitivity is important. Besides, we need to overcome the down-regulation of steroid sensitivity, reduce the infection risk and rationalize the therapeutic strategy of corticosteroids. A fresh perspective is needed on the use of corticosteroids in AH patients.展开更多
Two new steroids,3a,17a,19,20-tetrahydroxy-4a-methylpregn-8-ene(1)and 3a,12a,17a,20-tetrahydroxy-4amethylpregn-8-ene(2)and three new sesquiterpenoids,12-hydroxy-a-cadinol(3),3a,12-dihydroxy-d-cadinol(4),and 3a,6a-dih...Two new steroids,3a,17a,19,20-tetrahydroxy-4a-methylpregn-8-ene(1)and 3a,12a,17a,20-tetrahydroxy-4amethylpregn-8-ene(2)and three new sesquiterpenoids,12-hydroxy-a-cadinol(3),3a,12-dihydroxy-d-cadinol(4),and 3a,6a-dihydroxyspiroax-4-ene(5),have been isolated from cultures of the fungus Phellinus igniarius.Their structures were characterized based on extensive spectroscopic data.In preliminary in vitro assays,compounds 3 and 4 exhibited the vascular-activities against phenylephrine-induced vasoconstriction with the relaxing rates of 11.0%and 7.0%at 3910-4 M,respectively.展开更多
Natural steroids have been showing notable cytotoxic activities, which are quite interesting lead compounds for the development of anticancer drug including estramustine and prednimustine. Considering that these semi-...Natural steroids have been showing notable cytotoxic activities, which are quite interesting lead compounds for the development of anticancer drug including estramustine and prednimustine. Considering that these semi-synthetic molecules are nitrogen mustard functionalized steroidal derivatives, the present review is focused on the methodologies of introducing nitrogen atom or nitrogen-containing heterocycles on A^D rings or side chains of steroids, and analysis of the structure-activity relationship(SAR) for these man-made cytotoxic steroids.展开更多
Maxillofacial space infection (MSI) is one of the most common conditions encountered in oral and maxillofacial surgery clinics. Early recognition and proper management of MSI could prevent a life-threatening event. Ob...Maxillofacial space infection (MSI) is one of the most common conditions encountered in oral and maxillofacial surgery clinics. Early recognition and proper management of MSI could prevent a life-threatening event. Objectives: To report a series of MSI managed with antibiotics, surgical intervention and exogenous steroids as an adjunct, highlighting functional improvement following steroid administration. Methods: A retrospective cohort study was carried out from December 2013 to September 2016, involving 30 patients (n = 30, 22 males, 8 females) diagnosed with MSI. All patients were initially managed with intravenous empirical antibiotics, analgesics and removal of potential source of infection. A course of 3 doses of IV Dexamethasone 8 mg at an interval of 8 hours was started during the first day of hospital admission. Results: This series reports 30 patients presenting with MSI, who received prompt antibiotics and 3 doses of steroids as inpatients. Significant clinical improvement was noted in the form of amelioration of pain, rapid reduction in edema, and improved trismus, shortening hospital stay to an average of 3.5 days, and omission of surgical intervention in 50% of our cases. No adverse effects or drug reaction was noted. Conclusion: In conclusion, the value of synergistic use of corticosteroids with antibiotics in management of MSI is significant. Despite these promising findings, there is scarce evidence in the literature to fully support the use of corticosteroids in abscess management. The role of corticosteroids in treatment of MSI should be explored further.展开更多
Objective:The aim of this study was to determine the expression of Hoxa 10 in endometrium during the menstrual cycle and their response to sex steroids and HB-EGF.Methods:Forty endometrial samples from regularly cycli...Objective:The aim of this study was to determine the expression of Hoxa 10 in endometrium during the menstrual cycle and their response to sex steroids and HB-EGF.Methods:Forty endometrial samples from regularly cycling women were studied.The endometrial epithelial(EEC)and stromal(ESC)cells isolated by collagenase Ⅰ digestion and mechanical dissociation was cultured from every sample.The endometrial stromal cells(ESC)were incubated with 17-beta estradiol(10-8mol/L),medroxyprogesterone acetate(MPA)(10-6mol/L),RU486(10-8mol/L)or HB-EGF(10ng/ml)for 48 hours respectively.The expression of Hoxa10 mRNA was demonstrated by reverse transcription-polymerase chain reaction(RT-PCR).Result:Hoxa10 showed a regulated cycle phase-dependent expression pattern in stromal cells and epithelial cells.Hoxa10 expression dramatically increased during the midsecretory phase of the menstrual cycle,at the time of implantation.The expression of Hoxa10 in cultured endometrial stromal cells was stimulated by estrogen,progesterone and HB-EGF.Conclusion:The cycle phase-specific expression of Hoxa10 and up-regulated by sex steroids and HB-EGF suggests a tight regulation and establishing conditions necessary for implantation.展开更多
Four steroids, 5α,8α-epidioxy-(24ξ)-ergosta-6,22-dien-3β-ol (1), β-sitosterol (2), β-sitostenone (3), and stigmastenone (4), along with 10 known compounds were isolated from the whole plants of Leucaena leucocep...Four steroids, 5α,8α-epidioxy-(24ξ)-ergosta-6,22-dien-3β-ol (1), β-sitosterol (2), β-sitostenone (3), and stigmastenone (4), along with 10 known compounds were isolated from the whole plants of Leucaena leucocephala (Leguminosae). 1, Lupeol (5), 1,3-dipalmitoyl-2-oleoylglycerol (6), methylparabene (8) and isovanillic acid (9) were found for the first time from the species. The structure of these compounds were characterized and identified by spectra analyses.展开更多
11β-Hydroxy-androst-4-en-3,17-dione（1a）,androst-4,9（11）-dien-3,17-dione-（2a）,androst-4-en-3,11,17-trione（3a）,11α-methoxy-androst-4-en-3,17-dione（4a）and 11β-metboxy-androst-4-en-3,17-dione（Sa）were select...11β-Hydroxy-androst-4-en-3,17-dione（1a）,androst-4,9（11）-dien-3,17-dione-（2a）,androst-4-en-3,11,17-trione（3a）,11α-methoxy-androst-4-en-3,17-dione（4a）and 11β-metboxy-androst-4-en-3,17-dione（Sa）were selectively reduced tothe corresponding 17β-OH derivatives in one step without the protection of 3-oxo（and 11-oxo,in the case of 3a）group with the yields ranging from 65% to79%.In these reactions,the ditute NaBH<sub>4</sub>（or KBH<sub>4</sub>）solution in methanol wasadded dropwise to the 3,17-dioxo-steroids solution in methanol-benzene-pyridine,while the reaction mixtures were well stirred at -5～5℃.Acid（such as gtacialacetic acid）was added to quench the reactions.The resulted testosteronederivatives（1b～5b）were purified by flash chromatography.This method appties to the reduction of other 3,17-dioxo-steroids such as△<sup>1</sup>-3-one,△<sup>1.4</sup>-3-one,△<sup>4.6</sup>-3-one,△<sup>1.4.6</sup>-3-one containing compounds.展开更多
Trimethylchlorosilane was used as a stereoselective reagent to determine the e or aorientation of 3-hydroxyl group of some steroids by chemical ionization mass spectrometry.
A new GC/MS method for detection and identification of 19 anabolic steroids in humanurine is presented.The procedure involves adsorption and isolation on a macroporous XAD-2resin,enzymatic hydrolysis,alkaline extracti...A new GC/MS method for detection and identification of 19 anabolic steroids in humanurine is presented.The procedure involves adsorption and isolation on a macroporous XAD-2resin,enzymatic hydrolysis,alkaline extraction,derivatization,GC separation and MS detec-tion.Gas chromatographic-mass spectrometric data illustrate artifacts arising from enzymatichydrolysis of steroid glucuronides and the structural characterization of their metabolites.Using this method,metabolic studies of these steroids in human urine were made after theiringestion by normal and healthy male volunteers.This method was proven to be suitable forlarge-scale routine analysis of anabolic steroids and was used successfully in passing thedoping control test held by the Medical Commission of the International Olympic Committee.展开更多
Objective: To assess the outcomes of hearing and vertigo in patients with Meniere’s disease who were treated with intratympanic methylprednisolone. Study Design: Retrospective study. Setting: Tertiary referral hospit...Objective: To assess the outcomes of hearing and vertigo in patients with Meniere’s disease who were treated with intratympanic methylprednisolone. Study Design: Retrospective study. Setting: Tertiary referral hospital. Methods: In our study with 151 patients [191 ears] were diagnosed as Menieres as per 1995 AAO-HNS guidelines. As an office based procedure these patients were treated with intratympanic methyl prednisolone. Results: There was a 98.6% improvement in the vertigo control rate, a 73.82% improvement in hearing and 29.31% had a definitive improvement in tinnitus. Conclusion: We conclude from our study that intratympanic steroid injection significantly controls vertigo, tinnitus and improves hearing in Meniere’s disease with minimal complications. Hence, it can be tried as a first line treatment for patients with Meniere’s disease.展开更多
AIM: To systematically review the literature to assess the efficacy of corticosteroids in treating postparotidectomy facial nerve palsy(FNP). METHODS: We searched the Cochrane library, EMBASE and MEDLINE(from inceptio...AIM: To systematically review the literature to assess the efficacy of corticosteroids in treating postparotidectomy facial nerve palsy(FNP). METHODS: We searched the Cochrane library, EMBASE and MEDLINE(from inception to 2014) for studies assessing the use of corticosteroids in post-parotidectomy FNP. Studies were assessed for inclusion and quality. Data was extracted from included studies. RESULTS: Two randomised controlled trials met the inclusion criteria. One study assessed the use of dexamethasone and the other prednisolone. None of the studies demonstrated a significant difference in the outcome of FNP post-parotidectomy with the use of corticosteroids vs no therapy. The majority of FNP postparotidectomy is transient. Preoperative factors(size of tumour and malignancy), intraoperative factors(extent of parotidectomy and integrity of facial nerve at the end of the operation) are important in determining prognosis of FNP if it does occur.CONCLUSION: Corticosteroids do not appear to improve FNP prognosis post-parotidectomy. Further studies assessing patients by cohort and with long term followup are required to increase scientific evidence.展开更多
Skin is not only a target organ for various sex steroids and hormones, but also an endocrine organ, which produces sex steroids. It has been suggested by Nikolakis et al. that impairment in skin steroidogenesis may re...Skin is not only a target organ for various sex steroids and hormones, but also an endocrine organ, which produces sex steroids. It has been suggested by Nikolakis et al. that impairment in skin steroidogenesis may result in inflammatory or autoimmune or other skin disorders. Melanoma is one such skin disease or disorder, which is believed to be caused by UV rays. But, epidemiological, clinical, in-vivo and in-vitro studies suggested the involvement of steroids in the regulation of melanoma growth. However, these studies either did not identify the steroid involved or did not relate to the protective function of the steroid in menstruating females in melanoma, as reported by the clinical studies. In this context, our studies with mouse and human melanoma cell lines showed that female sex steroid progesterone not only inhibited melanoma cell growth, but also affected adhesion and migration functions. In addition, our studies also showed that the effect of progesterone was not a toxic or spurious, but a specific effect on melanoma cells. Hence, our in-vitro studies along with previous other studies subscribed to the idea proposed earlier by Slominski et al. that modulation of local steroids could be a new therapeutic approach for treatment of skin disease or disorder, melanoma.展开更多
Corticosteroids are the most widely used class of anti-inflammatory medications in the pharmaceutical industry. There are several pharmaceutical dosage forms available using different corticosteroids. Topical steroids...Corticosteroids are the most widely used class of anti-inflammatory medications in the pharmaceutical industry. There are several pharmaceutical dosage forms available using different corticosteroids. Topical steroids of varying potencies are available in creams, ointments, solutions and other vehicles. Chemical instability and drug degradation are the key quality concerns for these topical dosage forms. Nature of the dosage forms, excipient quality, product composition, and process optimization are some of the common factors which affect the stability of corticosteroids. This article describes drug degradation behavior of three different corticosteroids in different topical dosage forms. Drug degradation patterns of Hydrocortisone, Clobetasol propionate and Desonide formulations observed in stability studies of respective finished drug products under ICH recommended storage conditions were investigated. HPLC, UPLC-MS/MS methods were developed for the separation and characterization of impurities. The structural elucidation of the unknown impurities observed for these steroids and mechanistic consideration of potential degradation pathways has been discussed. Detailed discussion on the analytical methodologies is included as well.展开更多
A battery of sex steroids were used to check their effect on mouse melanoma (B16F10) cell growth in-vitro. Progesterone and its synthetic receptor antagonist RU-486 showed maximum inhibition on in-vitro melanoma cell ...A battery of sex steroids were used to check their effect on mouse melanoma (B16F10) cell growth in-vitro. Progesterone and its synthetic receptor antagonist RU-486 showed maximum inhibition on in-vitro melanoma cell growth [1]. Further research work showed that the inhibition by progesterone was not a toxic, spurious or non-specific effect on mouse melanoma cell growth and the inhibition by progesterone was not mediated through progesterone receptor.展开更多
文摘Terpenoids with quinoid structures are found as natural products. This includes steroidal quinones, quinones with a secosteroid structure and meroterpenoid quinones. Importantly, catechol estrogens as endogenous metabolites of estradiol and estrone are precursors of reactive quinones and semiquinones, which are thought to contribute to estrogen-induced carcinogenesis. On the other hand, a number of quinones that include substituted naphthoquinones and anthraquinones are highly cytotoxic and have been used in cancer treatment. This makes the structures interesting synthetic targets. The following is a review of important natural and synthetic terpenoid and steroid quinone hybrids.
基金supported by YAKHA Sport,Franceby the Platform 3A,funded by the European Regional Development Fund+3 种基金the French Ministry of Research,Higher Education and Innovationthe Provence-Alpes-Côte-d'Azur regionthe Departmental Council of Vauclusethe Urban Community of Avignon。
文摘Background:Strength-trained athletes using anabolic androgenic steroids(AAS)have left ventricular(LV)hypertrophy and myocardial fibrosis that can lead to sudden cardiac death.A similar feature was described in athletes with hypertrophic cardiomyopathy(HCM),which complicates the diagnosis for clinicians.In this context,we aimed to compare the LV function of the 2 populations by measuring global and regional strain and myocardial work using speckle-tracking imaging.Methods:Twenty-four strength-trained asymptomatic athletes using AAS(AAS-Athletes),22 athletes diagnosed with HCM(HCM-Athletes),and 20 healthy control athletes(Ctrl-Athletes)underwent a resting echocardiography to assess LV function.We evaluated LV global and regional strains and myocardial work,with an evaluation of the constructive work(CW),wasted work,and work efficiency(WE).Results:Compared to Ctrl-Athletes,both AAS-Athletes and HCM-Athletes had a thicker interventricular septum,with maj ored values in HCM-Athletes.LV strain was reduced in AAS-Athletes and even more in HCM-Athletes.Consequently,global WE was significantly diminished in both AAS and HCM-Athletes(93%±2%in Ctrl-Athletes,90%±4%in AAS-Athletes,and 90%±5%in HCM-Athletes(mean±SD);p<0.05).Constructive work and WE regional analysis showed specific alterations,with the basal septal segments preferentially affected in AAS-Athletes,and both septal and apical segments affected in HCM-Athletes.Conclusion:The regional evaluation of myocardial work reported specific alterations of the major LV hypertrophy induced by the regular use of AAS compared to the LV hypertrophy due to HCM.This finding could help clinicians to differentiate between these 2 forms of pathological hypertrophy.
文摘Eosinophilic esophagitis(EoE)is an emerging chronic local immune-mediated disease of the esophagus.Beside proton pump inhibitors and food-restrictiondiets swallowed topical corticosteroids(STC)can be offered as a first line therapy according to current guidelines.This review describes the background and practical management of STCs in EoE.So far,mainly asthma inhalers containing either budesonide or fluticasone have been administered to the esophagus by swallowing these medications“off label”.Recently esophagus-targeted formulations of topical steroids have been developed showing clinicopathological response rates up to 85%-an orodispersible tablet of budesonide has been approved as the first“in label”medication for EoE in Europe in June 2018.Whereas it was shown that disease remission induction of EoE by STCs is highly effective,there is still a lack of data regarding long-term and maintenance therapy.However,current studies on STC maintenance therapy add some movement into the game.
文摘Non-traumatic osteonecrosis is a cause of joint pain and deformity, not uncommonly caused by corticosteroid use. Despite this, corticosteroid induced osteonecrosis is poorly represented in the literature. We performed a detailed review of corticosteroid induced osteonecrosis, including aetiology, prevention, screening, clinical presentation, investigations, staging systems and treatment. We present this in the context of a patient at our institution who developed bilateral hip, shoulder and knee osteonecrosis following high dose corticosteroid therapy for dermatomyositis.
文摘Diabetic macular edema(DME)is a common cause of visual impairment in diabetic patients.It is caused by an increase in the permeability of the perifoveal capillaries and a disruption of the blood retinal-barrier.The pathogenesis of DME is multifactorial.Several therapeutic modalities have been proposed for the treatment of DME.Corticosteroid treatments have emerged as an alternative therapy for persistent DME or refractory to conventional laser photocoagulation and other modalities,due to anti-inflammatory,anti-vascular endothelial growth factor and anti-proliferative effects.Many studies have demonstrated the beneficial therapeutic effect of corticosteroids with improvement to both retinal thickness and visual acuity in short-term on the treatment of DME.Peribulbar and intravitreal injections have been used to deliver steroids for DME with frequent injections due to the chronic and recurrent nature of the disease.Steroid-related side effects include elevated intraocular pressure,cataract,and injection related complications such as endophthalmitis,vitreous hemorrhage,and retinal detachment particularly with intravitreal steroid injections.In order to reduce the risks,complications and frequent dosing of intravitreal steroids,intravitreal implants have been developed recently to provide sustained release of corticosteroids and reduce repeated intravitreal injections for the management of DME.
文摘Objective:To determine the chemical profile and steroids composition of the medicinally important plant Aerva lanata(A.lanata) L.Methods:Preliminary phytochemicul screening was done by the method as Harborne described.HPTLC studies were canied out as Harborne and Wagner et al described.The Ethyl acetate-ethanol-water(8:2:1.2) was employed as mobile phase for glycosides.Results:The desired aim was achieved using Chloroform-acetone(8:2) as the mobile phase.The methanolic extract of stem,leaves,root,flower and seeds of A.lanata showed the presence of 30 different types of steroids with 30 different Rf values from 0.04 to 0.97. Maximum number(11) of steroids has been observed in leaves followed by root(10).Conclusions: HPTLC profile of steroids has been chosen here to reveal the diversity existing in A.lanata.Such finger printing is useful in differentiating the species from the adulterant and act as biochemical markers for this medicinally important plant in the pharma industry and plant systematic studies.
基金supported by a grant from the General Project Foundation of the Education Department of Liaoning Province (2009A809)
文摘BACKGROUND: Alcoholic hepatitis (AH) is a necrotizing inflammatory process caused by alcoholic liver injury. It carries a significant short-term mortality. The management of AH is challenging. Although corticosteroids have been demonstrated to exert anti-inflammatory and antifibrotic effects, their efficacy for the treatment of AH remains debatable. DATA SOURCES: A literature search was performed of MEDLINE, ScienceDirect, SpringerLink and Wiley InterScience using the key words "alcoholic hepatitis", "alcoholic liver disease", and "corticosteroids". The available data reported in the relevant literature were analyzed. RESULTS: More than 17 controlled trials and at least 13 meta-analyses have reported the efficacy of corticosteroids in the treatment of AH in the past 40 years. Many were poorly designed and used different inclusion/exclusion criteria, making it difficult to reach a consensus. In this review, we summarized all the controversial data in the past decade and analyzed the potential causes for the varying therapeutic effects of corticosteroids in AH. The focus of the controversy has changed from "whether steroids are beneficial or harmful for AH patients" to "how to accurately identify responders to steroids early and rationalize corticosteroid treatment". An early response to glucocorticoids, as determined by calculating the Lille score after 7 days of treatment, has been shown to be a clinically useful indicator. Moreover, down-regulation of steroid sensitivity, risk of infection, and a rational therapeutic strategy of corticosteroids in AH patients are all crucial for therapeutic effect.CONCLUSIONS: An early and accurate determination of steroid sensitivity is important. Besides, we need to overcome the down-regulation of steroid sensitivity, reduce the infection risk and rationalize the therapeutic strategy of corticosteroids. A fresh perspective is needed on the use of corticosteroids in AH patients.
基金the National Natural Sciences Foundation of China(U1132607,81102346)Natural Sciences Foundation of Yunnan Province(2011FB099).
文摘Two new steroids,3a,17a,19,20-tetrahydroxy-4a-methylpregn-8-ene(1)and 3a,12a,17a,20-tetrahydroxy-4amethylpregn-8-ene(2)and three new sesquiterpenoids,12-hydroxy-a-cadinol(3),3a,12-dihydroxy-d-cadinol(4),and 3a,6a-dihydroxyspiroax-4-ene(5),have been isolated from cultures of the fungus Phellinus igniarius.Their structures were characterized based on extensive spectroscopic data.In preliminary in vitro assays,compounds 3 and 4 exhibited the vascular-activities against phenylephrine-induced vasoconstriction with the relaxing rates of 11.0%and 7.0%at 3910-4 M,respectively.
基金Financial support from the National Natural Science Foundation of China(No.21272136)Youth Talent Development Foundation of China Three Gorges University
文摘Natural steroids have been showing notable cytotoxic activities, which are quite interesting lead compounds for the development of anticancer drug including estramustine and prednimustine. Considering that these semi-synthetic molecules are nitrogen mustard functionalized steroidal derivatives, the present review is focused on the methodologies of introducing nitrogen atom or nitrogen-containing heterocycles on A^D rings or side chains of steroids, and analysis of the structure-activity relationship(SAR) for these man-made cytotoxic steroids.
文摘Maxillofacial space infection (MSI) is one of the most common conditions encountered in oral and maxillofacial surgery clinics. Early recognition and proper management of MSI could prevent a life-threatening event. Objectives: To report a series of MSI managed with antibiotics, surgical intervention and exogenous steroids as an adjunct, highlighting functional improvement following steroid administration. Methods: A retrospective cohort study was carried out from December 2013 to September 2016, involving 30 patients (n = 30, 22 males, 8 females) diagnosed with MSI. All patients were initially managed with intravenous empirical antibiotics, analgesics and removal of potential source of infection. A course of 3 doses of IV Dexamethasone 8 mg at an interval of 8 hours was started during the first day of hospital admission. Results: This series reports 30 patients presenting with MSI, who received prompt antibiotics and 3 doses of steroids as inpatients. Significant clinical improvement was noted in the form of amelioration of pain, rapid reduction in edema, and improved trismus, shortening hospital stay to an average of 3.5 days, and omission of surgical intervention in 50% of our cases. No adverse effects or drug reaction was noted. Conclusion: In conclusion, the value of synergistic use of corticosteroids with antibiotics in management of MSI is significant. Despite these promising findings, there is scarce evidence in the literature to fully support the use of corticosteroids in abscess management. The role of corticosteroids in treatment of MSI should be explored further.
文摘Objective:The aim of this study was to determine the expression of Hoxa 10 in endometrium during the menstrual cycle and their response to sex steroids and HB-EGF.Methods:Forty endometrial samples from regularly cycling women were studied.The endometrial epithelial(EEC)and stromal(ESC)cells isolated by collagenase Ⅰ digestion and mechanical dissociation was cultured from every sample.The endometrial stromal cells(ESC)were incubated with 17-beta estradiol(10-8mol/L),medroxyprogesterone acetate(MPA)(10-6mol/L),RU486(10-8mol/L)or HB-EGF(10ng/ml)for 48 hours respectively.The expression of Hoxa10 mRNA was demonstrated by reverse transcription-polymerase chain reaction(RT-PCR).Result:Hoxa10 showed a regulated cycle phase-dependent expression pattern in stromal cells and epithelial cells.Hoxa10 expression dramatically increased during the midsecretory phase of the menstrual cycle,at the time of implantation.The expression of Hoxa10 in cultured endometrial stromal cells was stimulated by estrogen,progesterone and HB-EGF.Conclusion:The cycle phase-specific expression of Hoxa10 and up-regulated by sex steroids and HB-EGF suggests a tight regulation and establishing conditions necessary for implantation.
文摘Four steroids, 5α,8α-epidioxy-(24ξ)-ergosta-6,22-dien-3β-ol (1), β-sitosterol (2), β-sitostenone (3), and stigmastenone (4), along with 10 known compounds were isolated from the whole plants of Leucaena leucocephala (Leguminosae). 1, Lupeol (5), 1,3-dipalmitoyl-2-oleoylglycerol (6), methylparabene (8) and isovanillic acid (9) were found for the first time from the species. The structure of these compounds were characterized and identified by spectra analyses.
文摘11β-Hydroxy-androst-4-en-3,17-dione（1a）,androst-4,9（11）-dien-3,17-dione-（2a）,androst-4-en-3,11,17-trione（3a）,11α-methoxy-androst-4-en-3,17-dione（4a）and 11β-metboxy-androst-4-en-3,17-dione（Sa）were selectively reduced tothe corresponding 17β-OH derivatives in one step without the protection of 3-oxo（and 11-oxo,in the case of 3a）group with the yields ranging from 65% to79%.In these reactions,the ditute NaBH<sub>4</sub>（or KBH<sub>4</sub>）solution in methanol wasadded dropwise to the 3,17-dioxo-steroids solution in methanol-benzene-pyridine,while the reaction mixtures were well stirred at -5～5℃.Acid（such as gtacialacetic acid）was added to quench the reactions.The resulted testosteronederivatives（1b～5b）were purified by flash chromatography.This method appties to the reduction of other 3,17-dioxo-steroids such as△<sup>1</sup>-3-one,△<sup>1.4</sup>-3-one,△<sup>4.6</sup>-3-one,△<sup>1.4.6</sup>-3-one containing compounds.
文摘Trimethylchlorosilane was used as a stereoselective reagent to determine the e or aorientation of 3-hydroxyl group of some steroids by chemical ionization mass spectrometry.
文摘A new GC/MS method for detection and identification of 19 anabolic steroids in humanurine is presented.The procedure involves adsorption and isolation on a macroporous XAD-2resin,enzymatic hydrolysis,alkaline extraction,derivatization,GC separation and MS detec-tion.Gas chromatographic-mass spectrometric data illustrate artifacts arising from enzymatichydrolysis of steroid glucuronides and the structural characterization of their metabolites.Using this method,metabolic studies of these steroids in human urine were made after theiringestion by normal and healthy male volunteers.This method was proven to be suitable forlarge-scale routine analysis of anabolic steroids and was used successfully in passing thedoping control test held by the Medical Commission of the International Olympic Committee.
文摘Objective: To assess the outcomes of hearing and vertigo in patients with Meniere’s disease who were treated with intratympanic methylprednisolone. Study Design: Retrospective study. Setting: Tertiary referral hospital. Methods: In our study with 151 patients [191 ears] were diagnosed as Menieres as per 1995 AAO-HNS guidelines. As an office based procedure these patients were treated with intratympanic methyl prednisolone. Results: There was a 98.6% improvement in the vertigo control rate, a 73.82% improvement in hearing and 29.31% had a definitive improvement in tinnitus. Conclusion: We conclude from our study that intratympanic steroid injection significantly controls vertigo, tinnitus and improves hearing in Meniere’s disease with minimal complications. Hence, it can be tried as a first line treatment for patients with Meniere’s disease.
文摘AIM: To systematically review the literature to assess the efficacy of corticosteroids in treating postparotidectomy facial nerve palsy(FNP). METHODS: We searched the Cochrane library, EMBASE and MEDLINE(from inception to 2014) for studies assessing the use of corticosteroids in post-parotidectomy FNP. Studies were assessed for inclusion and quality. Data was extracted from included studies. RESULTS: Two randomised controlled trials met the inclusion criteria. One study assessed the use of dexamethasone and the other prednisolone. None of the studies demonstrated a significant difference in the outcome of FNP post-parotidectomy with the use of corticosteroids vs no therapy. The majority of FNP postparotidectomy is transient. Preoperative factors(size of tumour and malignancy), intraoperative factors(extent of parotidectomy and integrity of facial nerve at the end of the operation) are important in determining prognosis of FNP if it does occur.CONCLUSION: Corticosteroids do not appear to improve FNP prognosis post-parotidectomy. Further studies assessing patients by cohort and with long term followup are required to increase scientific evidence.
文摘Skin is not only a target organ for various sex steroids and hormones, but also an endocrine organ, which produces sex steroids. It has been suggested by Nikolakis et al. that impairment in skin steroidogenesis may result in inflammatory or autoimmune or other skin disorders. Melanoma is one such skin disease or disorder, which is believed to be caused by UV rays. But, epidemiological, clinical, in-vivo and in-vitro studies suggested the involvement of steroids in the regulation of melanoma growth. However, these studies either did not identify the steroid involved or did not relate to the protective function of the steroid in menstruating females in melanoma, as reported by the clinical studies. In this context, our studies with mouse and human melanoma cell lines showed that female sex steroid progesterone not only inhibited melanoma cell growth, but also affected adhesion and migration functions. In addition, our studies also showed that the effect of progesterone was not a toxic or spurious, but a specific effect on melanoma cells. Hence, our in-vitro studies along with previous other studies subscribed to the idea proposed earlier by Slominski et al. that modulation of local steroids could be a new therapeutic approach for treatment of skin disease or disorder, melanoma.
文摘Corticosteroids are the most widely used class of anti-inflammatory medications in the pharmaceutical industry. There are several pharmaceutical dosage forms available using different corticosteroids. Topical steroids of varying potencies are available in creams, ointments, solutions and other vehicles. Chemical instability and drug degradation are the key quality concerns for these topical dosage forms. Nature of the dosage forms, excipient quality, product composition, and process optimization are some of the common factors which affect the stability of corticosteroids. This article describes drug degradation behavior of three different corticosteroids in different topical dosage forms. Drug degradation patterns of Hydrocortisone, Clobetasol propionate and Desonide formulations observed in stability studies of respective finished drug products under ICH recommended storage conditions were investigated. HPLC, UPLC-MS/MS methods were developed for the separation and characterization of impurities. The structural elucidation of the unknown impurities observed for these steroids and mechanistic consideration of potential degradation pathways has been discussed. Detailed discussion on the analytical methodologies is included as well.
文摘A battery of sex steroids were used to check their effect on mouse melanoma (B16F10) cell growth in-vitro. Progesterone and its synthetic receptor antagonist RU-486 showed maximum inhibition on in-vitro melanoma cell growth [1]. Further research work showed that the inhibition by progesterone was not a toxic, spurious or non-specific effect on mouse melanoma cell growth and the inhibition by progesterone was not mediated through progesterone receptor.
