Two New Phloroglucinol Glycosides from Lysidice rhodostega Hance

Two new phloroglucinol glycosides, lysidiciside A (1) and lysidiciside B (2), were isolated from the roots of Lysidice rhodostega Hance. Their structures were determined as 1-[(3-methylbutyryl)phloroglucinol]-β-D- glucopyranoside (1), 1- [(3-methylbutyryl)phloro- glucinol]-β-D-glucopyranosyl-5-O-β-D-glucopyranoside (2) on the basis of chemical and spectral analysis .

Separation and Purification of Total Phloroglucinols in Dryopteris crassirhizoma with DM-130 Macroporous Adsorption Resin

To improve the purity of the total phloroglucinols from Dryopteris crassirhizoma extracts, the separation and purification conditions of the total phloroglucinols from Dryopteris crassirhizoma were studied with DM-130 macroporous adsorption resin in this study. Adsorption rate, elution rate and purity of the total phloroglucinols were used as indexes to investigate the adsorption and desorption capacity of the total phloroglucinols with DM-130 macroporous adsorption resin. Through the study, the optimum sample concentration of the total phloroglucinols and maximum sample volume were 1.5 mg·mL^-1 and 7 BV （210 mL）, respectively. The optimum desorption conditions were achieved by using 80% ethanol as desorption solvent at elution flow rate of 1.0 mL·min^-1. The result showed DM-130 macroporous adsorption resin performed effective adsorption and desorption. After purification, the purity of the total phloroglucinols increased by 11.5-fold.

Structurally Diverse Polymethylated Phloroglucinol Meroterpenoids from Baeckea frutescens

Phytochemical investigation of the MeOH extract of twigs and leaves of Baeckea frutescens led to the isolation of seven new polymethylated phloroglucinol meroterpenoids(PPMs),named baeckfrutones M-S(1-7).Their structures and absolute configurations were determined by spectroscopic analyses,chiral-phase HPLC analysis,and electronic circular dichroism(ECD)calculations.PPM 1 is a novel meroterpenoid possessing a 6/6/5/3 tetracyclic skeleton in PPMs,whereas 3 and 4 are the first hydroxytasmanone type phloroglucinol-monoterpene hybrids.(+)-2 and 7 displayed potent antiinflammatory activity with IC50 values of 20.86±0.60 and 36.21±1.18 lL,respectively.

Phloroglucinol, a nutraceutical for IR-induced cardiac damage in diabetic rats

Background:Myocardial injury due to ischemia‐reperfusion(IR)is aggravated in diabetes which is associated with oxidative stress.Alleviating oxidative stress via use of antioxidants has been shown to be effective at minimizing myocardial cell death and improving cardiac function.The aim of the present study was to evaluate the cardioprotective effect of phloroglucinol against myocardial reperfusion injury(MRI)in diabetic rats.Methods:Diabetes was induced in female rats with streptozotocin(50 mg/kg).The diabetic rats were orally treated with phloroglucinol(100 and 200 mg/kg daily for 28 days).After treatment the hearts were isolated and mounted on a Langendorff apparatus.The hearts were subjected to 15 minutes of IR to induce myocardial damage.Cardiac functions including heart rate(HR),resting and developed tension,and rate of change of contraction(+dP/dtmax)were recorded.Cardiac injury biomarkers lactate dehydrogenase(LDH)and creatine kinase(CK‐MB)were measured in the heart perfusate.Levels of the antioxidant enzymes reduced glutathione(GSH)and malondialdehyde(MDA)were measured.Hematoxylin and eosin(H&E)staining was also performed.Results:After IR injury,a decrease in HR and+dP/dtmax in hearts from diabetic rat was seen compared to healthy rat hearts,which was reversed by phloroglucinol treatment.Myocardial infarct size,measured by H&E staining,was increased in diabetic rats compared to healthy rats and an increase in the activity of LDH and CK‐MB in the heart perfusate in diabetic rats was decreased by phloroglucinol treatment.An increase in MDA levels and a decrease in levels of antioxidant enzymes were observed in diabetic rats,which was reversed with phloroglucinol treatment.Conclusion:Phloroglucinol treatment has potential therapeutic promise in the treatment of MRI in diabetes.

New Phloroglucinol Glycosides from Hypericum japonicum

Two new phloroglucinol glycosides, 2,6-dihydroxy-3,5-dimethyl-1-isobutyrylbenzene-4-O-beta-D-glucoside and 2,6-dihydroxy-3,5-dimethyl-1-(2-methylbutyryl) benzene-4-O-beta-D-glucoside were isolated from Hypericum japonicum. Their structures were determined by spectroscopic and chemical methods.

Potential of phloroglucinol to improve erectile dysfunction associated with streptozotocin-induced diabetes in rats

Objective: Diabetes is a common metabolic disease with several complications in its patients. Often, people living with diabetes develop erectile dysfunction (ED). The primary aim of this work was to investigate the effect of phloroglucinol in diabetes-induced ED in rats. Methods: Male Wistar rats were given 52 mg/kg of streptozotocin, by intraperitoneal injection, to induce diabetes and ED. Subsequently, animals were grouped into three groups: group 1, diabetic control;group 2, low-dose phloroglucinol (150 mg/kg body weight);and group 3, high-dose phloroglucinol (250 mg/kg body weight). A group of six normal rats served as a normal control. The rats were treated with phloroglucinol for six weeks and then were assessed for treatment effects. Sexual behavior, glycosylated hemoglobin Ale (HbAlc) values, serum testosterone, serum nitric oxide (NO), blood pressure and sperm count were measured after the end of treatment. Results: After a 6-week treatment period, the high dose of phloroglucinol significantly decreased HbAlc values in diabetic rats. Rats treated with phloroglucinol had increased serum testosterone, NO and sperm count. Animals treated with 250 mg/kg phloroglucinol performed similar to normal rats in the sexual behavioral study, suggesting the reversal of complications of ED. Conversely, a decrease in the blood pressure in treated groups was observed. Conclusion: The results highlight the protective effect of phloroglucinol in diabetes-induced ED in rats warranting further studies.

Euphoractone,a cytotoxic meroterpenoid with an unusual entabietane-phloroglucinol skeleton,from Euphorbia fischeriana Steud.

A novel meroterpenoid,euphoractone(1),was isolated from the extracts of the roots of Euphorbia fischeriana Steud.Its structure was determined by spectroscopic methods and X-ray crystallography.1 possesses an unusual ent-abietane-phloroglucinol skeleton.The plausible biosynthetic pathway for 1 was proposed.1 showed inhibitory activities against human lung cancer H23 and H460 cells with the IC_(50)values of 21.07±3.54 and 20.91±4.07 μmol/L.

间苯三酚联合缩宫素在单胎足月初产妇阴道试产中应用效果

目的:探究间苯三酚联合缩宫素在单胎足月初产妇阴道试产中的应用效果。方法:采用随机数字表法将2021年1月-2023年1月在本院接受阴道试产且阴道试产期间出现第一产程异常的197例初产妇分为单一组(98例)和联合组(99例),分别予缩宫素及间苯三酚联合缩宫素治疗,比较两组用药后产程进展情况、宫颈水肿发生率、用药后宫缩强度及母婴结局。结果:联合组用药至进入活跃期时间(77.3±35.5min)、活跃期时间(100.3±51.3min)、用药至宫口开全时间(55.4±25.7min)均短于单一组(117.6±51.5min、155.3±71.3min、85.4±43.2min),宫颈水肿比例(2.0%)低于单一组(9.2%),宫缩强度为强比例(76.8%)高于单一组(63.3%),自然分娩率(95.0%)高于单一组(84.7%),产时(150.4±55.4ml)及产后6h(250.5±38.3ml)出血量均低于单一组(200.5±44.3ml、291.4±40.6ml)(均P<0.05);两组产钳助产比例、胎位异常、巨大儿、头盆不称比例无差异(P>0.05),胎儿宫内窘迫比例联合组(0)低于单一组(7.1%)(P<0.05);两组新生儿出生后1min、5minApgar评分及新生儿体重均无差异(P>0.05)。结论:苯三酚联合缩宫素用于阴道试产第一产程异常初产妇,可有效促进产程进展,提升自然分娩率,降低产时及产后出血量。

缩宫素联合间苯三酚在低宫颈评分足月胎膜早破产妇分娩中的应用

目的:观察缩宫素联合间苯三酚在低宫颈评分足月胎膜早破(PROM)产妇分娩中的应用。方法:回顾性选取2020年9月—2022年4月海宁市人民医院妇产科收治的160例低宫颈评分足月PROM产妇的临床资料。根据不同治疗方法将其分为对照组、观察1组、观察2组、观察3组,各40例。对照组单纯使用缩宫素,观察组使用缩宫素联合间苯三酚,观察1组于出现规律宫缩时静脉缓慢推注间苯三酚注射液80 mg;观察2组在宫口开大2~3 cm时静脉缓慢推注间苯三酚注射液80 mg;观察3组在进入活跃期、宫口开大≥5 cm时静脉缓慢推注间苯三酚注射液80 mg。比较四组分娩方式、宫口扩张速度、宫口开全时间、产后出血情况、产后并发症及新生儿不良事件。结果:观察2组、观察3组阴道分娩率高于对照组,差异有统计学意义(P<0.05)。观察2组的宫口扩张速度大于对照组与观察1组,宫口开全时间短于对照组与观察1组,差异有统计学意义(P<0.05)。观察1组、观察2组的产后2 h出血量少于对照组与观察3组,差异有统计学意义(P<0.05)。四组产后尿潴留、产褥感染、新生儿不良事件发生率比较,差异无统计学意义(P>0.05)。结论:缩宫素联合间苯三酚在低宫颈评分足月PROM产妇分娩中的应用效果优于单纯使用缩宫素,在宫口开大2~3 cm时静脉缓慢推注间苯三酚80 mg的效果最优,可获得较高的阴道分娩率,且可加快宫口扩张速度、缩短宫口开全时间,减少产后出血量,且不增加产后尿潴留、产褥感染、新生儿不良事件的发生率,有效性与安全性兼具。

间苯三酚(phloroglucinol for injection)静脉滴注联合坦索罗辛口服辅助ESWL治疗泌尿系结石的临床研究

目的 :探讨间苯三酚静脉滴注联合坦索罗辛口服辅助体外冲击波碎石(ESWL)治疗泌尿系结石的临床疗效。方法 :以结石直径<0.6cm并行体外冲击波碎石(ESWL)后24h内的上尿路结石患者150例为研究对象,随机分为A组、B组及C组。所有患者给予常规治疗。A组给予间苯三酚注射液40mg溶于5%葡萄糖250ml注射液中静脉滴注,1次/日;B组给予坦索罗辛0.2mg,口服,1次/日;C组给予坦索罗辛联合间苯三酚注射液,其中坦索罗辛用法用量与B相同;间苯三酚注射液用法用量与A相同。治疗2周后比较3组患者的结石排出率、结石清除率、;平均结石排出时间、石街形成率、肾绞痛发作次数、镇痛药使用人次及治疗期间而不良反应发生情况。结果 :组间比较:治疗2周后,3组的结石排出率、结石清除率、平均结石清除时间、石街形成率、肾绞痛发作率及镇痛药使用率之间具有明显区别,差异具有统计学意义,3组之间的不良反应发生率比较无显著性差异。组内两两比较:C组的结石排出率及结石清除率显著高于另外两组,平均结石排出时间、肾绞痛发作率及镇痛药使用率显著低于另外两组,差异均具有统计学意义;C组的石街形成率显著低于A组,B组的平均结石排出时间明显短于A组。结论:间苯三酚静脉滴注联合坦索罗辛口服辅助ESWL可增加结石排出率,缩短结石排出时间,降低肾绞痛发作率及镇痛药使用率且药物不良反应发生率与单用坦索罗辛或间苯三酚无明显区别,是一种安全有效的上尿路结石治疗方案。

Phloroglucinol Protects the Urinary Bladder Via Inhibition of Oxidative Stress and Inflammation in a Rat Model of Cyclophosphamide-induced Interstitial Cystitis

Background： Phloroglucinol plays an important role in oxidative stress and inflammatory responses. The effects of phloroglucinol have been proven in various disease models. The aim of the present study was to investigate the efficacy and possible mechanisms of phloroglucinol in the treatment of interstitial cystitis （IC）. Methods： Thirty-two female Sprague-Dawley （SD） rats were used in this study. IC was induced by intraperitoneal injection of cyclophosphamide （CYP）. Rats were randomly allocated to one of four groups （n = 8 per group）： A control group, which was injected with saline （75 mg/kg; i.p.） instead of CYP on days 1, 4, and 7; a chronic IC group, which was injected with CYP （75 mg/kg; i.p.） on days l, 4, and 7; a high-dose （30 mg/kg） phloroglucinol-treated group; and a low-dose （15 mg/kg） phloroglucinol-treated group. On day 8, the rats in each group underwent cystometrography （CMG）, and the bladders were examined for evidence of oxidative stress and inflammation. Statistical analysis was performed by analysis of variance （ANOVA） followed by least square difference multiple comparison po.s＇t-hoc test. Results： Histological evaluation showed that bladder inflammation in CYP-treated rats was suppressed by phloroglucinol. CMG revealed that the CYP treatment induced overactive bladder in rats that was reversed by phloroglucinol. Up-regulated tumor necrosis factor-or and interleukin-6 expression in the CYP-treated rats were also suppressed in the phloroglucinol treated rats. CYP treatment significantly increased myeloperoxidase activity as well as the decreased activities ofcatalase of the bladder, which was reversed by treatment with phloroglucinol. Conclusions： The application of phloroglucinol suppressed oxidative stress, inflammation, and overactivity in the bladder. This may provide a new treatment strategy for IC.

元宝草中一个新的间苯三酚及其乙酰胆碱酯酶抑制活性研究

目的研究元宝草化学成分及其乙酰胆碱酯酶抑制活性。方法元宝草二氯甲烷部位采用硅胶柱色谱、Sephedex LH-20、MCI和半制备HPLC等进行化分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。采用Ellman法测定其乙酰胆碱酯酶抑制活性。结果从中分离得到8个化合物,分别鉴定为元宝草素A(1)、hyperbeanin A(2)、hyperpatulol I(3)、hyperhenone I(4)、hypercohone G(5)、hyperbeanol G(6)、hyperlagarin A(7)、hyperascyrone D(8)。化合物抑制乙酰胆碱酯酶IC 50值均在1.16~5.15μmol/L之间。结论化合物1为间苯三酚类新化合物。所有化合物均具有一定程度的乙酰胆碱酯酶抑制活性,是阿尔茨海默病治疗药物的潜在活性先导化合物。

天然间苯三酚类成分抗菌活性研究进展

抗菌药物的广泛使用甚至滥用使得细菌的耐药性日趋严重,耐药菌感染已成为威胁全球公共健康的重大问题。间苯三酚类成分广泛分布于陆地植物及海洋生物中,该类成分结构新颖、生物活性多样,其中不乏抗菌活性显著的新颖化合物,具有良好的开发前景。具有抗菌活性的天然间苯三酚类成分主要分布在桃金娘科及藤黄科植物中,该类成分对金黄色葡萄球菌及其耐药菌株、枯草芽孢杆菌、肠球菌等革兰阳性菌具有良好的抗菌效果。对近30年来报道的230个间苯三酚类成分的抗菌活性研究进行综述,以期为该类成分进一步研究和开发提供参考。

宫腔镜术前宫颈软化的临床研究

目的比较宫腔镜术前应用间苯三酚注射液、米索前列醇、一次性宫颈扩张用模具软化宫颈的效果及不良反应。方法选择2020年7月至2022年12月在该院进行宫腔镜手术的150例患者为研究对象,按照随机数字表法分为间苯三酚组(A组)、米索前列醇组(B组)、一次性宫颈扩张用模具组(C组),每组50例。比较3组患者宫颈软化效果、扩宫时间、术中漏水率及不良反应发生率。结果3组患者宫颈软化有效率比较,差异均有统计学意义(P=0.023),A组宫颈软化有效率明显高于B组(P=0.012),C组宫颈软化有效率虽高于B组,但差异无统计学意义(P=0.053)。3组患者扩宫时间比较,差异有统计学意义(P=0.018),A组和C组扩宫时间均短于B组,差异有统计学意义(P=0.008、0.031),A组和C组扩宫时间比较,差异无统计学意义(P=0.600)。3组患者术中漏水率比较,差异无统计学意义(P=0.108)。3组患者不良反应发生率比较,差异有统计学意义(P<0.001)。B组不良反应发生率最高,均明显高于A组与C组(P<0.001、0.011)。结论3种宫颈扩张方法各有利弊,宫腔镜术前需结合手术时间、漏水率、医疗成本、不良反应等综合考虑,选择软化宫颈的方式。

间苯三酚与山莨菪碱在急诊肾绞痛患者中的应用效果比较

目的探讨间苯三酚与山莨菪碱在急诊肾绞痛患者中的应用效果比较。方法选取2022年3月至2023年9月华中科技大学协和深圳医院急诊收治的86例肾绞痛患者作为研究对象,按随机数字表法将其分为对照组(43例)和观察组(43例)。对照组采用双氯芬酸钠缓释片+山莨菪碱治疗,研究组采用双氯芬酸钠缓释片+间苯三酚治疗。比较两组临床疗效、疼痛程度[视觉模拟评分法(VAS)评分]、疼痛缓解时间、镇痛起效时间、不良反应发生率、24 h复发率。结果研究组总有效率高于对照组,差异有统计学意义(P<0.05);研究组治疗后VAS评分低于对照组,差异有统计学意义(P<0.05);研究组疼痛缓解时间、镇痛起效时间均短于对照组,差异有统计学意义(P<0.05);研究组不良反应总发生率低于对照组,差异有统计学意义(P<0.05);研究组24 h复发率低于对照组,差异有统计学意义(P<0.05)。结论间苯三酚作为一种新型解痉止痛药,与山莨菪碱相比起效快,解痉止痛效果显著,且副作用较小,安全性更高,具有临床应用价值。

间苯三酚对比地西泮对初产妇分娩效果的临床研究

目的对比分析产程潜伏期间应用间苯三酚(PG)和地西泮(DZP)对初产妇分娩效果的影响。方法回顾性分析2022年1月至2023年12月于杭州市妇产科医院分娩产妇的临床资料。根据产程潜伏期用药方案,分为PG组(PG 80 mg,静脉推注)和DZP组(DZP 10 mg,静脉推注)。比较两组宫颈成熟程度、产程时间、分娩情况(宫口扩张度、产后24 h出血量、分娩方式和宫口全开时间)、新生儿Apgar评分和妊娠相关不良结局。结果研究共纳入162例患者,PG组83例,DZP组79例。PG组宫颈总成熟率显著高于DZP组(P<0.05);第一、第二、第三和总产程时间均短于DZP组(P<0.05)。PG组宫颈扩张度显著大于DZP组(P<0.05),产后24 h出血量和宫口全开时间显著小于DZP组(P<0.05),经阴道分娩率高于DZP组(P<0.05)。两组新生儿1 min、5 min Apgar评分、产妇不良结局发生率和新生儿不良结局发生率差异均无统计学意义(P>0.05)。结论与DZP比较,在潜伏期应用PG可提高宫颈成熟度,加快产程进展,提高经阴道分娩率。

间苯三酚注射液联合热敏灸治疗胃脘痛临床疗效观察

目的探讨间苯三酚注射液联合热敏灸治疗胃脘痛的临床疗效。方法选取2021年1月至2023年8月九江市中医医院收治的52例胃脘痛患者作为研究对象,采用随机数字表法将其分为对照组和观察组,每组各26例。对照组采用间苯三酚注射液治疗,观察组加用热敏灸治疗。比较两组临床疗效、疼痛强度、疼痛持续时间和不良反应。结果观察组治疗总有效率高于对照组,差异有统计学意义(P<0.05);两组治疗后疼痛强度评分低于治疗前,差异有统计学意义(P<0.05);观察组治疗后疼痛强度评分低于对照组,差异有统计学意义(P<0.05);观察组疼痛持续时间短于对照组,差异有统计学意义(P<0.05);两组疼痛强度评分时间、组间、交互作用比较,差异有统计学意义,差异有统计学意义(P<0.05)。两组未见明显不良反应。结论间苯三酚注射液联合热敏灸治疗胃脘痛可迅速、有效减轻患者疼痛程度,减少疼痛持续时间,且安全有效,值得推广。

间苯三酚联合双氯芬酸钠栓在孕早期人工流产中的应用效果

目的探讨间苯三酚联合双氯芬酸钠栓在孕早期人工流产中的应用效果。方法将2022年1月—2023年12月我院妇产科行孕早期人工流产176例孕妇进行研究。分组方法选择随机数字表法,分成两组,各88例。对照组:双氯芬酸钠栓辅助干预。观察组:间苯三酚联合双氯芬酸钠栓辅助干预。观察对比两组手术时间、术中出血量、镇痛效果、Kolcaba舒适状况量表评分、扩宫效果(宫口松弛度)、并发症发生情况。结果与对照组比较,观察组手术时间较短,术中出血量较少(P<0.05);观察组镇痛VAS评分、并发症发生率相比对照组较低(P<0.05);观察组术后Kolcaba舒适状况量表评分、扩宫效果(宫口松弛度)总有效率相比对照组较高(P<0.05)。结论间苯三酚联合双氯芬酸钠栓在孕早期人工流产中应用能够缩短孕妇的手术时间,减少术中出血量,镇痛效果明显,舒适度较高,且宫颈软化效果较好,孕妇术后人工流产综合征等并发症发生率较低。

间苯三酚与阿托西班在先兆早产治疗中的临床效果对比分析

目的比较分析间苯三酚与阿托西班治疗先兆早产的临床效果。方法筛选2021年1月至2023年3月上饶市妇幼保健院住院的82例先兆早产孕妇作为研究对象,随机数字表法分A组和B组,各41例。在常规治疗的基础上,A组采用间苯三酚治疗;B组采用阿托西班治疗。比较A、B两组患者用药后的药物起效时间,延长妊娠时间,临床效果,保胎成功率,性激素水平(孕酮、雌三醇),新生儿状态(体质量、头围、身长、Apgar评分)及用药不良反应。结果治疗后,A组患者的药物起效时间较B组相比更快,差异有统计学意义(P<0.05);A组延长妊娠时间较B组更短,差异有统计学意义(P<0.05);A组用药后的临床有效率与B组的临床有效率相比较低,差异有统计学意义(P<0.05);A组保胎成功率与B组相比较低,差异有统计学意义(P<0.05);A组用药后孕酮较B组低,雌三醇较B组高,差异有统计学意义(P<0.05);A组新生儿的体质量、头围、身长、Apgar评分与B组新生儿相比略低,但差异无统计学意义(P>0.05)。比较两组用药后不良反应发生率,A组略低于B组,但差异无统计学意义(P>0.05)。结论在治疗先兆早产时,阿托西班的药物起效时间相较于间苯三酚稍慢,但妊娠延长时间相较于间苯三酚更长,且阿托西班治疗先兆早产后的临床有效率、保胎成功率及改善患者性激素水平的作用与间苯三酚相比更好,故针对治疗先兆早产的患者应优先选用阿托西班。