厚朴丸对小鼠胃肠活动的影响

目的:观察厚朴丸对小鼠胃排空和小肠推进运动的影响.方法:利用胃复安和阿托品造成小鼠胃排空亢进和胃排空抑制模型,利用新斯的明和肾上腺素造成小鼠小肠推进亢进和小肠推进抑制模型,观察厚朴丸对正常、亢进及抑制状态下小鼠胃肠活动的影响.结果:厚朴丸抑制正常小鼠胃排空和胃复安所致小鼠胃排空加快,能加强阿托品所致小鼠胃排空的抑制作用;对正常小鼠小肠推进和新斯的明所致小鼠小肠推进亢进也有抑制作用,但对肾上腺素所致小鼠小肠推进抑制无明显影响.结论:厚朴丸具有抑制正常和亢进状态的小鼠胃排空和小肠推进的作用,与临床用于止泻相符合.     

厚朴提取物及其有效成分的呼吸系统药理作用研究进展

厚朴药材具有止咳祛痰作用,对气管平滑肌具有收缩和舒张的双向作用。厚朴酚及和厚朴酚是疏水性烯丙基联苯酚类结构的同分异构体,也是厚朴产生呼吸系统药理作用的主要活性成分。厚朴酚及和厚朴酚都具有松弛气管平滑肌作用和平喘作用,都具有肺保护作用和对抗各种病理因子引起的肺损伤作用。厚朴酚及和厚朴酚还具有广谱的抗病毒、抗菌和细胞保护作用,尤其适用于具有基础疾病的各种肺损伤,以期被开发为新药供临床利用。     

苍术及其有效成分消化系统药理作用的研究进展

苍术及其有效成分的消化系统药理作用主要包括抗胃溃疡、促进胃排空、调节胃肠推进运动、抗腹泻、利胆和保肝以及提高消化吸收功能作用。苍术可通过阻断H₂受体抑制胃酸分泌,抑制胃组织炎性因子过度表达产生抗胃溃疡作用。苍术还可通过阻断5-羟色胺受体,提高血清和胃组织的胃泌素、三叶因子水平,增加胃黏膜血流量,促进胃黏膜生长和修复,产生抗溃疡作用。而苍术促进胃排空和胃肠推进运动主要与其抑制中枢促皮质素释放因子的释放和刺激迷走神经以及促进胃肠激素胃泌素、胃动素释放,抑制血管活性肠肽释放和5-羟色胺-3受体,提高胃肠组织Cajal间质细胞数量有关。抗炎作用是苍术抗腹泻的主要机制。     

厚朴提取物、厚朴酚及和厚朴酚的抗氧化和抗衰老药理作用研究进展

厚朴系木兰科植物厚朴Magnolia officinalis或凹叶厚朴M.officinalis Rehd.et Wils.var.biloba的干燥干皮、根皮及枝皮,具有燥湿消痰、下气除满的功效。厚朴提取物、厚朴酚及和厚朴酚都具有抗炎、抗氧化和抗衰老作用,厚朴酚及和厚朴酚是厚朴抗炎、抗氧化和抗衰老的主要活性成分。它们的抗氧化能力是通过对自由基的直接清除作用以及提高机体的抗氧化酶活性间接猝灭自由基表现出来。因此厚朴提取物、厚朴酚及和厚朴酚能防治各种氧化应激性炎性疾病,长期应用可能有防治机体衰老发生发展的作用。综述厚朴提取物、厚朴酚及和厚朴酚的抗氧化和抗衰老药理作用研究进展,以期为抗氧化和抗衰老的新药研发提供依据。     

厚朴酚及和厚朴酚抗抑郁药理作用及机制的研究进展

动物实验证实厚朴酚及和厚朴酚具有防治急慢性抑郁作用,其主要机制是抗氧化和抗炎:通过直接清除自由基以及提高机体的核因子E2相关因子-2抗氧化信号通路和抗氧化酶活性间接清除自由基而抑制活性氧生成;通过阻滞磷脂酰肌醇-3蛋白激酶/蛋白激酶B,细胞外信号调节激酶/丝裂原活化蛋白激酶和把关受体/丝裂原活化蛋白激酶信号通路抑制炎性细胞因子表达和小胶质细胞、星形细胞的激活,保护脑神经。也可增强脑内5-羟色胺能神经功能,提高脑源性神经营养因子表达,促进海马神经再生,产生抗抑郁作用;还可下调抑郁时的下丘脑-垂体-肾上腺轴功能的亢进,改善抑郁样行为。     

厚朴酚及和厚朴酚防治高血糖、高脂血症及其并发症的药理机制研究进展

厚朴酚及和厚朴酚是来自于中药厚朴的同分异构体,具有相同的药理活性。它们都可通过保护胰腺β-细胞,促进胰岛素分泌,提高血中胰岛素水平及细胞对葡萄糖的摄取和利用,从而降低胰岛素抵抗和血糖水平;还能通过抑制脂质合成和促进脂质分解,产生调血脂作用。厚朴酚及和厚朴酚可通过降血糖、调血脂及抗氧化作用,从源头上减少氧化低密度脂蛋白（ox-LDL）和晚期糖基化终末产物（AGEs）的生成,还可通过抗氧化、抗炎及细胞保护作用,保护心血管系统、肾脏、肝脏、胰腺等组织器官对抗高血糖、高脂血症诱导并发症的发生和发展。因此厚朴酚及和厚朴酚有开发成为治疗代谢综合征新药的潜力。     

中药厚朴及其成分厚朴酚与和厚朴酚体外抗各种球菌的药理作用研究进展

中药厚朴不同溶剂的粗提取物具有体外抗各种球菌的药理作用,其中厚朴石油醚和乙醇提取物的抗球菌作用最强.厚朴酚(magnolol)及和厚朴酚(honokiol)是中药厚朴抗球菌的主要活性成分,其中厚朴酚抗球菌作用稍强于和厚朴酚.厚朴酚及和厚朴酚均能抑制金黄色葡萄球菌(以下简称"金葡菌")的自溶酶和α-溶血素、肠毒素-A、肠毒素-B的表达,阻断金葡菌的自溶和抑制其黏附功能及毒力,阻滞球菌诱导宿主细胞的炎性损伤反应.厚朴酚及和厚朴酚均能抑制被膜态金葡菌合成和释放eDNA和PIA,进而抑制生物被膜的形成,降低球菌的自我保护能力,产生抗球菌作用.本文中综述了中药厚朴及其成分厚朴酚及和厚朴酚体外抗各种球菌的药理作用,并对其研究进展做了分析.     

厚朴及其有效成分防治阿尔茨海默病和帕金森病的药理作用及机制研究进展

动物实验证实厚朴及其有效成分（厚朴酚、和厚朴酚等）具有防治阿尔茨海默病和帕金森病的药理作用。它们最主要的作用机制是抗氧化和抗炎作用：通过直接清除自由基和提高机体的核因子红系2-相关因子-2（Nrf2）抗氧化信号通路和抗氧化酶活性间接清除自由基的方式抑制活性氧生成；通过激活去乙酰化酶（SIRT），阻滞磷脂酰肌醇-3激酶（PI3K）/蛋白激酶-B（Akt），细胞外信号调节蛋白激酶（ERK）/丝裂原活化蛋白激酶（MAPK）和Toll样受体-2（TLR2）/MAPK/核因子-κB（NF-κB）信号通路和促进线粒体自噬，抑制炎性细胞因子表达，保护脑神经（包括海马、黑质和纹状体等），表现出防治阿尔茨海默病和帕金森病的作用。     

藿香正气制剂中厚朴不同提取工艺对胃肠活动的影响研究

目的:探讨60%、70%、95%乙醇三种不同溶媒热回流提取的厚朴提取液对缓解小鼠便秘、促进大鼠胃肠道蠕动作用的影响。方法:采用灌胃消旋山莨菪碱造成小鼠便秘模型实验,观察各组小鼠首次排便时间,6 h排便粒数和重量,测定厚朴提取液对缓解小鼠便秘作用;采用腹腔注射左旋精氨酸造成大鼠胃肠运动障碍模型实验,得到各组大鼠胃残留率和肠推进率,测定厚朴提取液对促进大鼠胃排空和小肠推进作用。结果:厚朴提取物组1、2、3号均能有效缓解消旋山莨菪碱模型小鼠的便秘(P0.05或P0.01)和促进左旋精氨酸致胃肠运动障碍模型大鼠胃排空运动和小肠推进运动(P0.01),其中70%乙醇热回流提取组有强于60%乙醇热回流提取组和95%乙醇热回流提取组的趋势。结论:3种厚朴提取液均具有促进胃肠道蠕动、缓解便秘作用,70%乙醇热回流提取组较优。     

芪参益气滴丸通过调控TLR-4/NF-κB信号通路对阿霉素所致小鼠心脏毒性的保护作用

和厚朴酚具有广泛的生物活性,如抗菌、抗病毒、抗肿瘤、抗炎、抗氧化和抗衰老作用,对消化、神经、心血管和呼吸系统等均有明显的药理活性。和厚朴酚是一种疏水性联苯酚类结构化合物,难溶于水,易溶于脂,在胃肠道吸收较差,但分布广泛,50%以上口服剂量的和厚朴酚经胃肠道排出体外,40%以上的和厚朴酚经代谢后排出体外。通过综述和厚朴酚药动学参数,体内过程,总结和厚朴酚的药动学研究进展,为合理用药提供参考。     

厚朴酚的药动学研究进展

厚朴酚具有广泛的生物活性，如抗菌、抗病毒、抗肿瘤、抗炎、抗氧化和抗衰老等，对消化、神经、心血管和呼吸系统等均有明显的药理作用。厚朴酚是一种疏水性联苯酚类结构化合物，难溶于水、易溶于脂，在胃肠道吸收较差，但分布广泛，约50%口服剂量的厚朴酚经胃肠道排出体外，40%以上的厚朴酚经代谢后排出体外。通过综述厚朴酚药动学参数、体内过程，总结厚朴酚的药动学研究进展，为合理用药提供参考。     

Inhibition of smooth muscle contraction by magnolol and honokiol in porcine trachea

Magnolol and honokiol are the two major phenolic constituents of the plant medicine "Houpo" ( Magnolia obovata), which is used in the treatment of chest tightness and asthma. The aim of this study was to investigate the influence of magnolol and honokiol on smooth muscle tone in porcine trachea. Magnolol and honokiol (0.1 - 100 microM) inhibited carbachol- and high K +-induced muscle contractions in a concentration-dependent fashion, but did not affect basal muscle tension. After washout of these pretreatments, carbachol- and high K +-evoked muscle contractions were still abolished, suggesting that the inhibition was irreversible. Magnolol and honokiol also concentration-dependently decreased the Ca 2+-dependent muscle contraction induced by high K + depolarization. Ca 2+ channel antagonists attenuated carbachol-induced muscular response by approximately 30 %, but did not further potentiate the inhibitory actions of magnolol and honokiol on muscle contraction. However, the inhibitory effects of magnolol and honokiol on carbachol-evoked muscular contractile response were partially reversed after removal of Ca 2+ channel antagonist pretreatment. Alternatively, caffeine-elicited muscle contractions were not altered by magnolol, honokiol, and verapamil. In conclusion, the relaxant effects of magnolol and honokiol on porcine tracheal smooth muscle suggest an association with the blockade of Ca 2+ influx through voltage-operated Ca 2+ channels instead of Ca 2+ release from intracellular Ca 2+ stores. The magnolol- and honokiol-induced inhibitions on tracheal smooth muscle contraction may be relevant to the claimed therapeutic effects of the extract from magnolia bark and contribute to their pharmacological effects by acting as anti-asthmatic agents.     

厚朴提取物、厚朴酚及和厚朴酚的抗炎作用及其机制研究进展

厚朴系木兰科植物厚朴Magnolia officinalis或凹叶厚朴M.officinalis var.biloba的干燥干皮、根皮及枝皮,具有燥湿消痰、下气除满的功效。厚朴提取物、厚朴酚及和厚朴酚是厚朴抗炎的主要活性成分,其抗炎机制有：阻滞磷脂酰肌醇-3激酶/蛋白激酶B（PI3K/Akt）、细胞外调节蛋白激酶/丝裂原活化蛋白激酶（ERK/MAPK）和把关受体-2/丝裂原活化蛋白激酶（TLR/MAPK）信号通路,抑制炎性细胞因子表达;还可通过直接抑制诱导型一氧化氮合酶（iNOS）、环氧化酶-2（COX-2）、5-脂氧化酶（5-LO）的酶活性,阻滞炎症介质一氧化氮、前列腺素（PGs）、白三烯（LTs）的合成和释放,以及抑制组织胺释放等,产生广谱的抗炎作用。厚朴提取物、厚朴酚及和厚朴酚的抗氧化活性也是其抗炎作用的主要机制之一。厚朴为常用的非毒性中药,可以把研究重点放在防治慢性的或退行性疾病的微炎症方面。     

The mechanism of honokiol-induced and magnolol-induced inhibition on muscle contraction and Ca2+ mobilization in rat uterus

The effects of honokiol and magnolol extracted from the Magnolia officinalis on muscular contractile responses and intracellular Ca²⁺ mobilization were investigated in the non-pregnant rat uterus. Honokiol and magnolol (1–100 mol/l) were observed to inhibit spontaneous and uterotonic agonists (carbachol, PGF₂, and oxytocin)-, high K⁺-, and Ca²⁺ channel activator (Bay K 8644)-induced uterine contractions in a concentration-dependent manner. The inhibition rate of honokiol on spontaneous contractions appeared to be slower than that of magnolol-induced response. The time periods that were required for honokiol and magnolol, at 100 mol/l, to abolish 50% spontaneous contractions were approximately 6 min. Furthermore, honokiol and magnolol at 10 mol/l also blocked the Ca²⁺-dependent oscillatory contractions. Consistently, the increases in intracellular Ca²⁺ concentrations ([Ca²⁺]_i) induced by PGF₂ and high K⁺ were suppressed by both honokiol and magnolol at 10 mol/l. After washout of these treatments, the rise in [Ca²⁺]_i induced by PGF₂ and high K⁺ was still partially abolished. In conclusion, the inhibitory effects of honokiol and magnolol on uterine contraction may be mediated by blockade of external Ca²⁺ influx, leading to a decrease in [Ca²⁺]_i. Honokiol and magnolol may be considered as putative Ca²⁺ channel blockers and be of potential value in the treatment of gynecological dysfunctions associated with uterine muscular spasm and dysmenorrhea.     

Inhibitory effects of magnolol on distal colon of guinea pig in vitro

The influence of plant product magnolol (0-100 microM) on the contractile activity of isolated colonic muscle strips in guinea pig and related mechanism were investigated. Magnolol did not affect the base tone of colon muscle strips, but it dose-dependently inhibited 40 mM KCl-, 1 microM carbachol (CCh)- and 10 microM serotonin (5-HT)-induced contractions at concentrations higher than 10 microM. And also, magnolol inhibited the 5-HT- or CCh-induced muscle contraction in calcium-free buffer. Furthermore, magnolol inhibited the KCl-induced contraction under the condition of procaine. In addition, inhibition rate of nifedipine plus magnolol on muscle strips was lower than that of nifedipine alone. Moreover, magnolol dose-dependently decreased the velocity of pellet propulsion in the concentration range of 0.1-10 microM, and totally inhibited pellet propulsion at the concentration higher than 30 microM. Thus, it can be concluded that magnolol may 1) block receptor-operated cation channels and the voltage dependent Ca2+ channel, and 2) inhibit calcium release from the sarcolemmal membrane (SR) through blocking InsP3-sensitive and ryanodine-sensitive pathways. This explains, at least partially, that Cortex magnoliae officinalis exerts therapeutic effects on gastrointestinal disease through relaxation of GI tract smooth muscles.     

Magnolol and honokiol account for the anti-spasmodic effect of Magnolia officinalis in isolated guinea pig ileum

Magnolia officinalis is a commonly used traditional Chinese medicine for treating gastrointestinal disorders. HPLC quantification analysis revealed that magnolol and honokiol were the most abundant constituents of M. officinalis extracts, with their contents in the ethanol extract being the highest, the water extract the least and the 50 % ethanol extract in between. In guinea pig isolated ileum, both magnolol and honokiol inhibited contraction to acetylcholine. The herbal extracts also produced inhibitory responses, in an order of decreasing efficacy: ethanol extract > 50 % ethanol extract > water extract. The differences in inhibitory efficacies among the three extracts were similar to the differences in their magnolol and honokiol contents. Further examination demonstrated that two mixtures containing solely magnolol and honokiol at concentrations identical to those determined in the ethanol and water extracts exhibited similar levels of anti-spasmodic effects as their respective extracts while a "blank" ethanol extract free of magnolol and honokiol failed to produce any response. These observations suggest that the magnolol and honokiol contents account for the anti-spasmodic effects of M. officinalis extracts in guinea pig isolated ileum.     

Magnolol and honokiol: inhibitors against mouse passive cutaneous anaphylaxis reaction and scratching behaviors

The antiallergic effects of magnolol and honokiol, isolated from the bark of Magnolia obovata (family Magnoliaceae), were investigated both in vitro and in vivo. Magnolol and honokiol potently inhibited passive cutaneous anaphylaxis reactions in mice induced by IgE-antigen complex as well as compound 48/80-induced scratching behaviors. These constituents exhibited not only potent inhibitory activity on the degranulation of RBL-2H3 cells induced by IgE-antigen complex, with IC(50) values of 45 and 55 muM, respectively, but also inhibited the protein expressions of IL-4 and TNF-alpha. Based on these findings, magnolol and honokiol may improve IgE-induced allergic diseases.