女贞子及其活性成分抗疲劳作用的研究进展

女贞子及其活性成分红景天苷具有提高运动耐力和抗疲劳作用。它们主要是通过抗氧化应激作用对抗疲劳引起的组织器官中的抗氧化酶、抗氧化物质水平下降,保护细胞膜免遭自由基攻击,从而对抗疲劳引起的骨骼肌、心、肝、肾、脑等重要组织器官的损伤,并维护它们的生理功能。女贞子的另一类活性成分齐墩果酸和熊果酸也具有抗氧化应激和保护骨骼肌、心、肝、肾、肺、脑作用。女贞子、红景天苷、齐墩果酸和熊果酸都能提高一氧化氮合酶的活性,促进NO合成和释放,具有保护血管内膜,松弛血管,改善血液循环作用,以及调控脂糖代谢,提高运动时的能量供应,可延缓疲劳产生和加快疲劳恢复。女贞子、红景天苷、齐墩果酸和熊果酸的促进骨、肌肉生长,增强机体特异性和非特异性免疫功能作用,是抗疲劳的基础性作用。综述女贞子及其活性成分红景天苷提高运动耐力和抗疲劳作用的文献,对其研究进展作了分析。     

女贞子及其有效成分的保肝作用研究进展

女贞子具有保肝的药理作用,已经证实齐墩果酸、红景天苷、女贞子多糖等化合物是其保肝的有效成分。女贞子提取物及其有效成分能对抗多种化学性肝损伤、对抗免疫性或缺血再灌注性肝损伤以及抗肝纤维化,其中齐墩果酸的保肝作用被研究得最为广泛而深入;抗氧化应激、抗炎、抑制肝星状细胞增殖和活化、促进其凋亡以及肝细胞再生可能是它们共同的保肝机制。综述了女贞子粗提物、女贞子多糖和红景天苷保肝作用的研究进展。     

女贞子药材及其制剂中齐墩果酸的含量测定方法研究综述

女贞子中主要成分有齐墩果酸(Oleanalicacid)、女贞子苷(Nuzhenide)、齐墩果苷、4-羟基β-苯乙基β-D葡萄糖苷、熊果酸等。齐墩果酸为其有效成分之一。含齐墩果酸的中药材较多,如连翘、槲寄生、凌霄花、车前草、青叶胆、黄花败酱、东方沙枣、冬凌草、藏茵陈等以及牛膝和五加科属植物根中所含的苷及其苷元也为齐墩果酸。     

HPLC法同时测定屏风扶正颗粒女贞子中齐墩果酸与熊果酸的含量

目的建立可以同时测定屏风扶正颗粒女贞子中齐墩果酸与熊果酸的方法。方法采用高效液相色谱法,色谱柱（ODSC18柱,250 mm×4.6 mm,5μm）;流动相：甲醇-水（90∶10,100 ml加0.08 ml冰醋酸）;流速：0.8 ml.min^-1;检测波长：220nm。结果齐墩果酸进样量在0.3125-10μg,熊果酸进样量在0.15625-5μg线性良好。齐墩果酸与熊果酸回归方程为Y奇墩果酸=342240C-189.93（r=0.9999）与Y熊果酸=300732C＋9.8905（r=0.9999）。精密度试验结果：齐墩果酸与熊果酸的RSD分别为0.36%与0.82%。齐墩果酸与熊果酸的平均加样回收率分别为100.6%（RSD=1.10%）与97.5%（RSD=0.41%）。结论方法简便、准确、专属性强,为屏风扶正颗粒女贞子中齐墩果酸与熊果酸含量测定提供了一个参考方法。     

女贞子及其有效成分药理作用与皮肤科临床应用的进展

女贞子是中医皮肤科常用的中药,其成分中齐墩果酸及其同分异构体熊果酸、红景天苷及其苷元酪醇是女贞子皮肤药理的有效成分,不仅具有保肝、抗糖尿病、抗动脉粥样硬化、心血管保护、神经保护及抗微生物等药理作用.综述女贞子及其有效成分的药理作用和皮肤科临床抗皮肤炎症、变态反应,以及抗皮肤肿瘤、促进毛发生长和黑色素合成的药理作用的文献,并对其研究进展作一分析.     

熊果酸和齐墩果酸抗肝脂肪变和纤维化作用研究进展

熊果酸和齐墩果酸的抗氧化作用能对抗各种原因引起的氧化应激所致的肝组织脂质过氧化反应、炎性损伤、脂肪变和纤维化。熊果酸和齐墩果酸通过阻断两面神激酶2-信号传导及转录激活因子3（JAK2-STAT₃）信号转导,抑制还原型烟酰胺腺嘌呤二核苷酸磷酸氧化酶（NOX）活化,阻止静息态肝星状细胞活化、增殖,促进活化态肝星状细胞凋亡,从而减少胶原生成、增加细胞外基质降解,产生防治肝纤维化的作用。熊果酸和齐墩果酸诱导肝脏去毒酶和外排转运体表达,降低胆汁淤积动物血清胆汁酸、胆红素水平和肝脏胆汁酸水平,减轻胆汁淤积性肝损伤和纤维化;还可通过降血脂作用抑制肝外脂质在肝脏沉积、抑制肝脏脂质生物合成和促进脂质代谢,阻滞肝脂肪变的发生和发展。     

女贞子中齐墩果酸和熊果酸的含量测定

目的 对女贞子中的齐墩果酸和熊果酸进行含量测定,为女贞子药材的质量评价提供科学依据.方法 采用反相高效液相色谱(RP-HPLC)法,同时测定女贞子药材中齐墩果酸与熊果酸的含量.流动相为0.5%冰醋酸-乙腈(10:90),检测波长为210nm,流速为0.8 ml/min;理论塔板数按齐墩果酸计算应＞5000,按熊果酸计算应＞4000.结果 11批次的测试样品巾齐墩果酸的含量范围在6.39-13.40 mg/g,熊果酸的含量范嗣在1.68～3.77 mg/g.结论 经过系统的方法学考察,所建立的测定方法具有操作简便、稳定、专属、可重复的特点,可用于女贞子药材及含女贞子的复方制剂的质量控制.     

女贞子抗炎、抗肿瘤和免疫调节作用的研究进展

女贞子是一味著名的补益类中药,《神农本草经》记载其具有补中、安五脏、养精神、除百疾等功效。现代医学认为炎症或免疫功能异常是包括肿瘤在内的许多疾病的病理、生理过程。女贞子具有抗非特异性炎症、抗变态反应性炎症、抗肿瘤及免疫调节作用,红景天苷、酪醇、羟基酪醇、齐墩果酸、熊果酸和多糖是其主要活性成分,因此其具有极高的医药保健价值,经深度研究后可开发为抗炎、抗肿瘤新药。     

熊果酸和齐墩果酸对心脏保护作用的研究进展

熊果酸和齐墩果酸通过抗氧化作用,抑制心脏脂质过氧化反应,提高心脏组织的抗氧化酶活性和非酶抗氧化物质水平,阻滞心肌细胞凋亡,产生心脏保护作用。熊果酸和齐墩果酸还可通过激活ATP敏感性钾通道并促进心房利钠肽合成和分泌,产生心脏保护作用。熊果酸和齐墩果酸也可通过抑制血管紧张素Ⅱ诱导心肌成纤维细胞增殖、转化生长因子-β_1表达、胶原合成和分泌,阻滞心肌纤维化形成。熊果酸和齐墩果酸的以上作用被认为是它们对抗异丙肾上腺素、乙醇、高血糖、高血压缺血、缺血再灌注引起心脏损伤的主要机制。熊果酸和齐墩果酸还具有免疫调节作用,能抑制T细胞核因子-κB核易位和T细胞活化,因此能防治实验性自身免疫性心肌炎和抑制机体对心脏移植物的排异反应。综述熊果酸和齐墩果酸对心脏保护作用的文献,并对其研究进展作了分析。     

甘草及甘草酸类成分抗病毒性肺炎的药理作用研究进展

甘草及甘草酸类成分有抗冠状病毒、流感病毒、呼吸道合胞病毒和人巨细胞病毒等呼吸道病毒的作用,其机制可能与抑制病毒的蛋白合成,导致病毒复制受阻;改善免疫调控,上调一氧化氮表达,抑制血小板聚集,抑制炎症反应,保护宿主有关。甘草及甘草酸类成分有止咳祛痰、平喘及肺保护和抗肺纤维化作用,其机制可能是通过上调过氧化物酶体增殖激活受体-γ（PPARγ）、血管紧张素转化酶2（ACE2）和IκB-α的表达,阻滞ERK/NF-κB信号通路,又能与高迁移率属蛋白B1（HMGB1）结合直接抑制HMGB1的化学趋化和促有丝分裂的活性,抑制炎性细胞因子表达、杯状细胞增生和黏蛋白过表达,以及上调水通道蛋白表达,减轻炎症反应;通过阻滞TLR-4/MyD88/NF-κB信号通路保护肺上皮细胞;通过阻滞IL-17/TGFβ1/Smad信号通路,抑制胶原合成和成纤维细胞增生,减轻肺纤维化形成;也可通过上调Smad7的表达,抑制气道重塑,改善肺功能。     

Synthesis and evaluation of 2,6-piperidinedione derivatives as potentially novel compounds with analgesic and other CNS activities

New 2,6-piperidinediones 2_a–g and 4_a–d were prepared by initial condensation of aromatic aldehydes or cycloalkanones with cyanoacetamide to give α-cyanocinnamides l_a–g or cycloalkylidenes 3_a,b which underwent Michae1 addition with ethyl cyanoacetate or diethylmalonate. Compounds 4_a–d were alkylated by various alkyl halides to produce the N-alkylated 2,6-piperidinedione derivatives 5_a–m. Some new selected compounds 2_a–c,f, 4_a–d & 5_e,h,j were pharmacologically evaluated for potential anticonvulsant, sedative and analgesic activities. These compounds exhibited significant anticonvulsant and analgesic effects after a single I.P. administration 100 mg/kg b.wt. . On the other hand all the investigated compounds induced hypnotic activity and prolonged the phenobarbital sodium- induced sleep as compared with the control group and the most potent compound was found to be 2_f.     

Metabolism and hepatotoxicity of N,N-dimethylformamide,N-hydroxymethyl-N-methylformamide,and N-methylformamide in the rat

The metabolism and hepatotoxicity ofN,N-dimethylformamide (DMF) and two of its metabolites,N-hydroxymethyl-N-methylformamide (HMMF) andN-methylformamide (NMF) were evaluated over a 4-day period in rats. DMF toxicity was dose dependent and delayed toxicity after the administration of a high DMF dose (13.7 mmol/kg) in comparison to a lower dose (4.1 mmol/kg) was observed. Treatment of rats with 13.7 mmol/kg DMF, HMMF, or NMF showed i) that DMF is more toxic than HMMF or NMR, and ii) that hepatotoxicity occurs later for DMF than for HMMF or NMF. Analysis of serum and urine samples demonstrated that DMF is first metabolized to HMMF, which is then partially converted to NMF. After HMMF administration, NMF was found both in serum and in urine. The time course of DMF and HMMF toxicity in relation to NMF formation fitted the hypothesis that the hepatotoxicity of DMF and HMMF is mediated via NMF. The degree of hepatotoxicity after HMMF and NMF treatment is similar. However, the degree of DMF hepatotoxicity is much higher than in the case of NMF or HMMF. The role of NMF as an obligatory intermediate in DMF and HMMF hepatotoxicity is discussed.     

Tricalysiolide G and tricalysiols A and B: rearranged ent-kaurane-type and ent-kaurane-type diterpenoids from the leaves of Tricalysia dubia (Lindl.) Ohwi

Three rearranged ent-kaurane diterpenes with the cafestol-type framework have been isolated from the leaves of Tricalysia dubia. Two were found to be known diterpenoids, tricalysiolides B and C. Tricalysiolide B was isolated as colorless prisms in this experiment and its three-dimensional structure was determined by X-ray crystallography. The remaining diterpenoid was a new compound and was named tricalysiolide G. Two new ent-kaurane-type diterpenoids, given the trivial names tricalysiol A and tricalysiol B, were also isolated. The structures of the new compounds were elucidated from spectroscopic evidence.     

去壁灵芝孢子粉片的含量测定与免疫调节及心脏保护功能研究

目的 研究并评价“仙芝3号”去壁灵芝孢子粉片的免疫调节和心脏保护作用。方法 首先运用UPLC-Q-TOFMS和比色法分析“仙芝3号”去壁灵芝孢子粉片的主要化学成分,考察其对斑马鱼巨噬细胞减少症模型、斑马鱼心衰模型、H2O2诱导的心肌及内皮细胞氧化应激模型、脂多糖诱导的小胶质细胞炎症模型的影响,通过巨噬细胞形成能力、巨噬细胞吞噬能力、抗神经炎症能力、心脏收缩舒张改善能力、抗心肌及内皮细胞氧化应激损伤能力等多个指标评估其免疫调节及心脏保护作用。结果 “仙芝3号”去壁灵芝孢子粉片可以提高巨噬细胞形成及吞噬能力,改善心脏收缩舒张功能,减少神经炎症并缓解心肌及内皮细胞因氧化应激而造成的损伤,从而起到免疫调节和心脏保护作用。结论 “仙芝3号”去壁灵芝孢子粉片有望用于免疫功能调节及心脏功能保护。     

Prevalence and characterization of the mechanisms of macrolide, lincosamide and streptogramin resistance in viridans group streptococci

The presence of erm genes conferring constitutive and inducible resistance, as well as that of the mefA gene conferring only constitutive resistance, was investigated using PCR in 70 erythromycin resistant (MIC≥1 mg/l) strains of viridans group streptococci (VGS) (18 Streptococcus mitis biotype 1, 16 S. mitis biotype 2, 15 S. oralis, 12 S. salivarius and nine S. sanguis) isolated from the oropharynx of healthy Greek children. All of the 56 isolates belonging to resistance phenotype M harbored the mefA gene. All of the 14 isolates constitutively resistant to macrolides and lincosamides (phenotype CR) harbored the ermB gene. Co-presence of both genes was not observed, whereas class A erm gene (previously known as ermTR) was not detected. Our results are consistent with a possible role of VGS as a reservoir of resistance genes now prevalent in pathogenic species of streptococci.     

Terbinafine susceptibility patterns for onychomycosis-causative dermatophytes and Scopulariopsis brevicaulis

The in vitro antifungal activity of terbinafine against 521 clinical isolates of seven species of dermatophytes, including four onychomycosis-causative species, as well as five Scopulariopsis brevicaulis isolates was determined by a modified Clinical and Laboratory Standards Institute microdilution method. Results showed a high antifungal activity of terbinafine against all dermatophyte isolates (geometric minimal inhibitory concentration (MIC)=0.026 microg/mL; concentration inhibiting 50% of mycological growth (MIC50)=0.03 microg/mL; and concentration inhibiting 90% of mycological growth (MIC90)=0.06 microg/mL). The geometric mean MICs against onychomycosis-causative dermatophyte species was lower (0.024 microg/mL) than the global MIC. However, the in vitro activity of terbinafine against S. brevicaulis was considerably lower (geometric mean MIC=1.38 microg/mL) in comparison with dermatophytes. The antifungal activity of itraconazole was lower than that of terbinafine against these fungi. These data confirm the high in vitro antifungal activity of terbinafine against dermatophytes, under standardised conditions.     

Bioaccessibility of Hg, Cd and As in cooked black scabbard fish and edible crab

Regular consumption of seafood has been widely recommended by authorities. Yet, some species accumulate high levels of contaminants like Hg, Cd and As. In addition, the risks associated to the consumption of such seafood may increase if consumers use cooking practices that enhance the concentration of contaminants and their bioaccessibility. In this study, the bioaccessibility of Hg, Cd and As was assessed with in vitro human digestion of raw and cooked black scabbard fish (Hg; steamed, fried and grilled) and edible crab (Cd and As; steamed and boiled) tissues. Additionally, the toxicological hazards associated with the consumption of these products were also discussed. Generally, Hg, Cd and As bioacessibility increased throughout the digestion process. Cadmium and As revealed high bioaccessibility rates in raw and cooked samples (up to 100%), whereas lower bioaccessible fractions of Hg was observed (up to 40%). Furthermore, this study pointed out the importance of food matrix, elemental chemical properties and cooking practices in the bioaccessibility of Hg, Cd and As. The toxicological hazards revealed that edible crab brown meat (Cd) and grilled black scabbard fish (MeHg) consumption in children should be moderated. In contrast, edible crab muscle (Cd) and fried or steamed black scabbard fish (MeHg) should be consumed to minimize exposure. The use of bioaccessible contaminant data strongly reduced the toxicological risks of MeHg, whereas less risk reduction occurred with Cd and inorganic As.     

Investigation of the prevalence of tetQ, tetX and tetX1 genes in Bacteroides strains with elevated tigecycline minimum inhibitory concentrations

In this study, the antibiotic susceptibilities to tigecycline and tetracycline of 35 selected Bacteroides fragilis group strains were determined by Etest, and the presence of tetQ, tetX, tetX1 and ermF genes was investigated by polymerase chain reaction (PCR). tetQ was detected in all 12 B. fragilis group isolates (100%) exhibiting elevated tigecycline minimum inhibitory concentrations (MICs) (≥8 μg/mL) as well as the 8 strains (100%) with a tigecycline MIC of 4 μg/mL, whilst tetX and tetX1 were present in 15% and 75% of these strains, respectively. All of these strains were fully resistant to tetracycline (MIC ≥ 16 μg/mL). On the other hand, amongst the group of strains with tigecycline MICs < 4 μg/mL (15 isolates), tetQ, tetX and tetX1 were found less frequently (73.3%, 13.3% and 46.7%, respectively). All but two strains harbouring the tetQ gene in this group were non-susceptible to tetracycline, with a MIC > 4 μg/mL. These data suggest that in most cases tigecycline overcomes the tetracycline resistance mechanisms frequently observed in Bacteroides strains. However, the presence of tetX and tetX1 genes in some of the strains exhibiting elevated MICs for tigecycline draws attention to the possible development and spread of resistance to this antibiotic agent amongst Bacteroides strains. The common occurrence of ermF, tetX, tetX1 and tetQ genes together predicted the presence of the CTnDOT-like Bacteroides conjugative transposon in this collection of Bacteroides strains.     

Photodegradation and phototoxicity of thioridazine and chlorpromazine evaluated with chemical analysis and aquatic organisms

The photochemical behaviour of chlorpromazine (CPZ) and thioridazine (THR) incubated under VIS light and a UV-A lamp was investigated with a high-performance liquid chromatography photodiode array detector (HPLC-PAD) and two bioassays. VIS light caused the decrease of CPZ and THR to 25% and 34% of the initial level, respectively, while UV-A degraded the drugs almost totally. CPZ and THR were very toxic to the protozoan Spirostomum ambiguum (Spirotox) and anostracan crustacean Thamnocephalus platyurus (Thamnotoxkit F^TM) with 24-h LC50 values of around 0.5 mg l⁻¹. In spite of the drastic decrease of the concentration of the drugs, the irradiated samples were toxic to the protozoan, especially when a sublethal end-point was taken into consideration. Contrary to the protozoan the crustacean was not sensitive to the products of photodegradation. Mass spectrometry analysis showed the presence of dimers and trimers of the CPZ and mono-, di-, and tri-oxygenated derivatives of THR. The presented data give a strong indication of the importance of the investigation of the environmental fate of drugs, especially those known to be phototoxic.     

Authentication of Stephania tetrandra S. Moore (Fang Ji) and differentiation of its common adulterants using microscopy and HPLC analysis

Stephania tetrandra S. Moore (Hang Fang Ji) is used in traditional Chinese medicine as a diuretic, an antiphlogistic, and an antirheumatic. The name “fang ji” is applied to at least four different genera of plants, including Aristolochia fangchi Y. C. Wu ex L. D. Chow and S. M. Hwang, Cocculus orbiculatus (L.) DC., Stephania tetrandra S. Moore, and Sinomenium acutum Rehder and E. H. Wilson. Due to similarity in the use of their common names, Stephania tetrandra S. Moore is often confused with Aristolochia fangchi Y. C. Wu ex L. D. Chow and S. M. Hwang, which has potentially dangerous consequences. To aid rapid and easy differentiation between the roots of these four species, so as to avoid possible contamination, detailed macroscopic and microscopic observations were made using stereo-and light-microscopy. The powdered samples were further analyzed using HPLC.