藏药塔勒两种基源植物的生药鉴定

目的 对藏药塔勒的两种原植物隐蕊杜鹃和蓝紫杜鹃进行组织、粉末鉴定.方法 对两种原植物进行形态描述,茎、叶横切片显微观察,叶和花的粉末鉴定,对比两种植物.结果 隐蕊杜鹃和蓝紫杜鹃原植物有显著差别;两种植物叶和茎的横切面较相似,但各自的叶脉维管束、茎环髓带和中柱鞘纤维、髓射线等有明显差别;各自粉末有特征表现.结论 对藏药塔...     

杜鹃素的体内代谢

本文报告一项从生物样品中测定杜鹃素含量的简便、灵敏的分光光度法,并利用这个方法进行了一些杜鹃素体内代谢的研究。 大鼠口服杜鹃素后约有30％的药物随粪排出,其余的药物在6～12小时内被吸收。口服后,药物在胃内有少量破坏。口服杜鹃素200mg/kg后1小时,能从肝脏测得少量药物,脂肪、脑、血液仅含痕迹量。静脉注射后药物在各组织中的分布以肺最高,然后脑、肝、肾、脾、心、脂肪等依次递降,血液最少。口服后5天尿中排出的未变药物仅占剂量的1.6％,大部分药物在体内被迅速转化,肝脏是转化杜鹃素的主要器官。从给药大鼠尿中分离到结晶杜鹃素及另外4个代谢产物,其中之一可能是杜鹃素的葡萄糖醛酸结合物。     

杜鹃素对映体的分离及其在中药材中的含量测定

目的 建立杜鹃素对映体分离的HPLC方法,并应用于满山红和照山白药材中的对映体含量测定。方法 用HPLC对杜鹃素对映体进行拆分,优化手性柱种类、流动相比例、流速和柱温的色谱条件。对手性热力学拆分进行探讨,计算杜鹃素对映体在色谱柱分离的焓变、熵变、焓变差值和熵变差值等热力学参数。并在最佳分离条件测定了满山红和照山白2种药材中2个对映体的含量。结果 确定了杜鹃素的2个对映体的最佳分离条件：色谱柱为Chiralcel OJ-RH(4.6 mm×150 mm,5μm),乙腈-水(40∶60)为流动相等度洗脱,流速为0.5 mL·min^–1,柱温为25℃,检测波长为295 nm。在最佳分离条件下,杜鹃素对映体的分离度达到1.5,表明杜鹃素的2个对映体能够完全分离。当柱温为20～35℃时,分离因子随着温度的升高呈降低趋势,2个对映体的lnα与1/T呈良好的线性关系,手性拆分过程受焓的控制。将所建立的杜鹃素对映体分离方法应用于中药材满山红、照山白中的杜鹃素对映体含量测定,杜鹃素的2个对映体线性范围分别为0.718～57.44μg·mL^–1和1.28～102...     

杜鹃素的体内代谢

本文报告一项从生物样品中测定杜鹃素含量的简便、灵敏的分光光度法,并利用这个方法进行了一些杜鹃素体内代谢的研究。大鼠口服杜鹃素后约有30%的药物随粪排出,其余的药物在6～12小时内被吸收。口服后,药物在胃内有少量破坏。口服杜鹃素200mg/kg后1小时,能从肝脏测得少量药物,脂肪、脑、血液仅含痕迹量。静脉注射后药物在各组织中的分布以肺最高,然后脑、肝、肾、脾、心、脂肪等依次递降,血液最少。口服后5天尿中排出的未变药物仅占剂量的1.6%,大部分药物在体内被迅速转化,肝脏是转化杜鹃素的主要器官。从给药大鼠尿中分离到结晶杜鹃素及另外4个代谢产物,其中之一可能是杜鹃素的葡萄糖醛酸结合物。     

山慈菇的本草考证及现代研究进展

目的:为临床合理选用山慈菇品种、进一步开发利用野生中药材资源提供参考。方法:以"山慈菇""杜鹃兰""丽江山慈菇""老鸦瓣""Cremastra appendicutata""Iphigenia indica""Tulipa edulis"等为关键词,组合查询自建库起至2020年1月在中国知网、维普网、万方数据库、中国植物志和Pub Med等数据库中发表的相关文献。在查阅历代本草、医药典籍的基础上对山慈菇的基原、性味归经及功效进行本草考证,并对其化学成分和药理作用的现代研究进行概述。结果与结论:本草典籍中记载的山慈菇主要包括杜鹃兰、丽江山慈菇、老鸦瓣等植物。其中,杜鹃兰Cremastra appendicutata(D.Don)Makino为临床常用品,丽江山慈菇Iphigenia indica Kunth与老鸦瓣Tulipa edulis(Miq.)Baker主要为地方习用品或伪品。3种中药植物均有轻微毒性,不可混用。此外,杜鹃兰、丽江山慈菇和老鸦瓣的功效主要为清热、散结、止痛,临床适用于疮痈肿痛、瘰疬痰核。三者在现代研究方面各有特点、不尽相同。现有关于杜鹃兰的研究较为完整,其化学成分...     

慢性气管炎药物紫花杜鹃甲素及杜鹃素的全合成

在攻克老年性慢性气管炎的群众运动中,全国各地发现许多杜鹃花属植物对气管炎有较好的疗效。如广东的紫花杜鹃、红花杜鹃、华丽杜鹃,东北的兴安杜鹃(满山红),经过反复临床验证,疗效显著。为提取分离这些中草药的有效成分,北京、黑龙江、广东及其他地区的医药工作者做了大量的工作。从紫花杜鹃中分离出紫花杜鹃甲素,药理试验有止咳作用,并经中国医学科学院药物研究所鉴定,其结构为5,7-二羟基-6,8-二甲基-4′-甲氧基双氢黄酮,即     

杜鹃花属植物的化学成分及药理研究进展

目的:对中药杜鹃花属植物的化学成分和药理活性作用进行综述.方法:查阅近30年的相关文献.结果:杜鹃属植物主要合有黄酮类、二萜类等有效成分.药理研究证明其在祛痰、止咳平喘、心血管系统、神经系统、抗炎镇痛、免疫、杀虫等方面具有药理活性.结论:杜鹃属植物在我国分布较广,对其进行进一步的化学和药理学研究具有重要的意义.     

黄杜鹃提取物对几种害虫的生物活性及其作用机理的初步研究

本文对黄杜鹃花提取物进行了生物活性研究。同时报道了黄杜鹃花提取物对粘虫、小菜蛾的拒食和胃毒活性试验以及对菜青虫的盆栽防治试验。并对黄杜鹃提取物较纯组份FC—22的作用机理进行了初步研究。结果发现,黄杜鹃氯仿、苯及二氯甲烷抽提物都有较高的活性。害虫取食黄杜鹃活性物质后会迅速出现兴奋、痉挛、呕吐等症状。FC—22是目前我们分离出活性最高的组份。150ppmFC—22对五龄粘虫幼虫的拒食率达93％。FC—22对三龄粘虫的LC_(50)为209ppm。对小菜蛾抗性及敏感两个品系的比较试验表明,抗杀灭菊酯的小菜蛾对黄杜鹃花二氯甲烷提取物没有表现出抗性。黄杜鹃提取物对菜青虫的盆栽防治效果较好,残效较长,在施药初期黄杜鹃提取物对菜白蝶有明显的产卵忌避作用,对孵化后的菜青虫一岭幼虫有较强的毒杀作用,但无杀卵作用。另外,对粘虫呼吸作用及多功能氧化酶测定结果表明,黄杜鹃提取物FC—22对粘虫幼虫的呼吸作用有一定影响,对粘虫的多功能氧化酶活性有诱导作用。     

黄花假杜鹃提取物用于治疗四氯化碳引起的肝损伤

从黄花假杜鹃 Barleria prionitis Linn.中得到一环烯醚萜糖苷类生物活性部位,该部位含假杜鹃素1.6%～6.2%、乙酰假杜鹃素0.015%～0.38%、山栀子苷(shanzhiside)     

山慈菇的真伪鉴别

山慈菇为兰科植物杜鹃兰Cremastra Variabilis(BL.)Nakai、独蒜兰Pleione bulbocodioides(Franch.)Rolfe的假球茎.杜鹃兰主要分布于黄河流域至西南、华南等地;独蒜兰又名冰球子,主要分布于西南地区.山慈菇的主要功效为清热解毒、消肿散结.     

In Vitro Anthelmintic Effects of Medicinal Plants Used in Czech Republic

The ethanol extracts of 16 Czech medicinal plants, namely, Allium sativum L. (Alliaceae), Artemisia absinthium L. (Asteraceae), Artemisia vulgaris L. (Asteraceae), Carum carvi L. (Apiaceae), Consolida regalis Gray (Ranunculaceae), Cucurbita pepo L. (Cucurbitaceae), Daucus carota L. (Apiaceae), Dryopteris filix-mas (L.) Schott (Dryopteridaceae), Erigeron canadensis L. (Asteraceae), Hedera helix L. (Araliaceae), Inula helenium L. (Asteraceae), Juglans regia L. (Juglandaceae), Satureja hortensis L. (Lamiaceae), Tanacetum vulgare L. (Asteraceae), Thymus vulgaris L. (Lamiaceae), and Valeriana officinalis L. (Valerianaceae), have been tested for their potential in vitro anthelmintic effect against eggs Ascaris suum and infectious larvae Trichostrongylus colubriformis. The extracts of A. sativum, A. absinthium, C. carvi, D. carota, and J. regia possessed the strongest anthelmintic effect on the embryonating eggs at all concentrations tested (62.5, 125, 250, 500, 1000, 2000 μg/mL). The best results, showing a higher effect against the infective third-stage larvae in comparison with synthetic anthelmintic Zentel (albendazole), have been obtained for A. sativum, A. absinthium, C. carvi, C. regalis, I. helenium, J. regia, S. hortensis, and V. officinalis.     

Comparative in vitro activity of -ofloxacin and FK037 to other agents against 10,040 fresh clinical isolates

Fresh clinical isolates collected from November 1, 1992 through November 1, 1993, were tested by agar dilution against 26 different antimicrobial agents including FK037 and -ofloxacin. Among the 10 040 organisms tested were Staphylococcus aureus (n = 1222), methicillin-resistant Staphylococcus aureus (MRSA, n = 455), Staphylococcus epidermidis (n = 533), Staphylococcus hominis (n = 90), Staphylococcus hemolyticus (n = 89), Streptococcus pneumoniae (n = 144), Escherichia coli (n = 2326), Klebsiella pneumoniae (n = 745), Enterobacter cloacae (n = 258), Proteus mirabilis (n = 445), Pseudomonas aeruginosa (n = 998), and Stenotrophomonas (Xanthomonas) maltophilia (n = 102). Both -ofloxacin and FK037 inhibited 98% of S. aureus strains at 4 μg/ml. FK037 was at least 4 times more effective than the third generation cephalosporins against MRSA, inhibiting 79% of the strains at 16 μg/ml. While the potency of these agents looks promising, their clinical utility will depend in part upon the maximal dosage that can be safely administered.     

刺人参挥发油成分及其抗真菌活性的研究

Oplopanax elatus (Ci Ren Shen, in Chinese), a perennial bush with thorn, wildly grows in Chang Bai Mountain area, northeast China. The essential oil of its root, rhizome and stem was extracted by steam distillation with yields of 0.8～1.2%. By means of GC/MS/DS, 31 chemical constituents were identified as follows: n-hexanal (0.22%), heptaldehydc (0.17%), α-pinene (1.30%), β-pentyl furan(0.27%), n-octanal(2.07%), limonene(0.31%), ocimene(1.62%), δ-3-carene(0.19%), perillen(1.33%), 2,6-dimethyl heptalene(1.07%), borneol(1.27%), α-dodecenal(7.14%), α-copaene(0.54%), tetradcanal(1.17%), iaocaryophyllene (0.58%), β-farnesene(0.92%), α-caryophyllene(0.82%), γ-muurolene(0.73%), longifolene(1.67%), 3, 7, 11-trimethyl-2, 6, 10-dodinene(8.64%), γ-cadinene(2.79%), δ-cadinene(5.03%), nerolidol(14.93%), gualol(4.20%), torreyol(10.0%), cedrol(4.24%), bulnesol(7.79%) and farnesol(1.16%).The antimycotic activities of Ci Ren Shen cssential oil was determined in vitro by serial dilutions on solid nutrient medium. Fungistatic results were visible on 5 species, Microporum gypseum, M. lanosun, Trichophyton gypseum, T. purpureatum and Epidermophyton floccosum. The MIC is 0.0625%.     

The risk of dermatological toxicities of combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma patients: a systematic review and meta-analysis

Background: This meta-analysis was conducted to assess the risk of dermatological toxicities of combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma patients.

Methods: We considered relevant prospective randomized phase I, II, and III trials of melanoma patients on the combined BRAF and MEK inhibition versus BRAF inhibition, describing events of rash, photosensitivity reaction (PR), hyperkeratosis (HK), alopecia, cutaneous squamous-cell carcinom(cSCC), skin papilloma(SP), pruritus, and hand-foot syndrome(HFS), as eligible for inclusion.

Results: Eight trials comprising 3163 patients were included in the meta-analysis. The relative risks(RRs) of developing all-grade rash with combined BRAF and MEK inhibition versus BRAF inhibition was 1.59 (95%CI, 1.35–1.86, p?p?=?0.002), SP 0.09(95%CI, 0.04–0.24, p?p?p?p?p?p?=?0.21), HK 0.18(95%CI, 0.06–0.53, p?=?0.002), SP 0.14(95%CI, 0.02–1.16, p?=?0.07), alopecia 0.72(95%CI, 0.14–3.62, p?=?0.69), cSCC 0.23(95%CI, 0.17–0.33, p?<?0.00001), HFS 0.40(95%CI, 0.08–2.06, p?=?0.27), and PR 0.14(95%CI, 0.04–0.51, p?=?0.003), respectly.

Conclusion: Our analysis of data has demonstrated that combined BRAF and MEK inhibitor-based treatment is associated with an increased risk of all-grade rash and a decreased risk of all-grade and high-grade HK, SP, alopecia, cSCC, HFS, and PR compared with single BRAF inhibitor alone in melanoma patients. Appropriate prevention and management are recommended.     

Evaluation of Some Plants Used in Turkish Folk Medicine for Their Anti-inflammatory and Antinociceptive Activities

Abstract

Ethanol and aqueous extracts obtained from 11 plant species from 11 families selected based on their use in Turkish folk medicine, including Isatis glauca. Aucher x Boiss. subsp glauca. (herb) (Brassicaceae), Tamus communis. L. (herb and root) (Dioscoreaceae), Rumex crispus. L. (herb) (Polygonaceae), Daphne oleoides. Schreber (aerial parts) (Thymeleaceae), Laurus nobilis. L. (leaves and seeds) (Lauraceae), Ranunculus tricophyllus. Chaix (herb) (Ranunculaceae), Anchusa azurea. Miller var. azurea. (herb) (Boraginaceae), Calluna vulgaris. L. (herb) (Ericaceae), Prunella vulgaris. L. (herb) (Lamiaceae), Scabiosa rotata. Bieb. (herb) (Dipsacaceae), and Arceuthobium oxycedri. (DC.) Bieb. (herb) (Loranthaceae), were evaluated for their in vivo. anti-inflammatory and antinociceptive activities. Among the plant extracts studied, the ethanol extracts of Laurus nobilis. seed and Calluna vulgaris. herb and the aqueous and ethanol extracts of Arceuthobium oxycedri. herb displayed significant anti-inflammatory activity using carrageenan-induced hind paw edema model in mice without inducing any gastric damage. The ethanol extracts of Isatis glauca. subsp. glauca., Calluna vulgaris., Laurus nobilis. (seeds) as well as the aqueous and ethanol extracts of Arceuthobium oxycedri. were also shown to possess significant antinociceptive activity in varying degrees against p.-benzoquinone-induced abdominal contraction test in mice.     

Antifungal efficacy of ten selected South African plant species against Cryptococcus neoformans

Fungal infections are a major threat to public health care. Cryptococcosis in humans and animals, caused by Cryptococcus neoformans, is a life-threatening disease. In a random antifungal screening of acetone leaf extracts of 400 tree species against Cryptococcus neoformans, the following plant species had good activity: Zanthoxylum capense (Thunb.) Harv. (Rutaceae), Morusmesozygia Stapf (Moraceae), Calodendrum capense (L.f.) Thunb. (Rutaceae), Catha transvaalensis Codd (Celastraceae), Cussonia zuluensis Strey (Araliaceae), Ochna natalitia (Meisn.) Walp. (Ochnaceae), Croton sylvaticus Hochst. ex C. Krauss (Euphorbiaceae), Maytenus undata (Thunb.) Blakelock (Celastraceae), Celtis africana Burm.f. (Ulmaceae), and Cassine aethiopica Thunb. (Celastraceae). Hexane, dichloromethane, acetone, and methanol extracts of these 10 plants were tested against Cryptococcus neoformans using bioautography and microdilution assays. Acetone extracted the highest quantity of plant material. Dichloromethane and hexane extracts of Maytenus undata showed clear bands in bioautography while the other species did not produce good results in bioautography. Maytenus undata extracts had promising antifungal activity against C. neoformans, with average minimum inhibitory concentration (MIC) of 0.09?mg/mL after 24?h and 0.18?mg/mL after 48?h incubation. Croton sylvaticus and Catha transvaalensis extracts also had good activity, with average MIC values of 0.07?mg/mL and 0.09?mg/mL, respectively. Because of the clear bands on bioautograms and low MIC values compared to the other plant species investigated, M. undata was identified as a good candidate for further studies.     

雌二醇11位含氧取代物的合成

为了进行抗辐射损伤药物的研究,参照文献从△⁹⁽¹¹⁾-雌二醇合成了11α-甲氧基雌二醇(12),对一些方法进行了改进。并从其中间体(3)合成了11α-羟基雌二醇(11)、11β-羟基雌二醇(13)、11β-甲氧基雌二醇(14)和11α-甲氧基-9β-雌二醇(15)。产物及关键中间体的核磁共振氢谱、质谱、元素分析等符合其结构。     

民族药小槐花质量标志物候选成分的研究

目的：开展对豆科山蚂蝗属药用植物小槐花（Desmodium caudatum（Thunb.）DC.）叶的化学成分研究,为小槐花质量标准体系的建立提供物质基础。方法：将小槐花叶经70%乙醇提取后,综合运用大孔吸附树脂柱色谱、硅胶柱色谱、制备型高效液相色谱等方法分离和纯化小槐花叶的化学成分,根据所得单体理化性质及波谱数据鉴定各化合物结构。结果：从小槐花叶中分离鉴定了13个化合物：清缸酒酚（1）、柠檬酚（2）、8-异戊烯基山柰酚（3）、二氢山柰酚（4）、neophellamuretin（5）、异柠檬酚（6）、槲皮素（7）、山柰酚（8）、牡荆素（9）、当药黄素（10）、大豆皂醇 B（11）、黄槿酮A （12）、黄槿酮 D （13）,其中化合物7、8、12和13为小槐花中各药用部位均含有的成分。结论：化合物7、8、12和13可作为小槐花的候选质控成分。     

Evaluation of antibacterial activity of Australian basidiomycetous macrofungi using a high-throughput 96-well plate assay

Context: The production of antimicrobial compounds by macrofungi is not unexpected because they have to compete with other organisms for survival in their natural hostile environment. Previous studies have indicated that macrofungi contain secondary metabolites with a range of pharmacological activities including antimicrobial agents.

Objective: To investigate macrofungi for antimicrobial activity due to the increasing need for new antimicrobials as a result of resistance in the bacterial community to existing treatments.

Materials and methods: Forty-seven different specimens of macrofungi were collected across Queensland, Australia. Freeze-dried fruiting bodies were sequentially extracted with three solvents: water, ethanol, and hexane. These extracts were tested against representative Gram+ve, Staphylococcus aureus and Gram?ve, Escherichia coli bacteria.

Results and discussion: Overall water and ethanol extracts were more effective against S. aureus than E. coli, whereas a small number of hexane extracts showed better results for their antimicrobial potential against E. coli at higher concentrations only. Encouraging results were found for a number of macrofungi in the genera Agaricus (Agaricaceae), Amanita (Amanitaceae), Boletus (Boletaceae), Cantharellus (Cantharellaceae), Fomitopsis (Fomitopsidaceae), Hohenbuehelia (Pleurotaceae), Lentinus (Polyporaceae), Ramaria (Gomphaceae), and Strobilomyces (Boletaceae) showing good growth inhibition of the pathogens tested.

Conclusion: The present study establishes the antimicrobial potential of a sample of Australian macrofungi that can serve as potential candidates for the development of new antibiotics.     

Assessment of asymptomatic liver fibrosis in alcoholic patients using fibroscan: prospective comparison with seven non-invasive laboratory tests

Background Systematic screening for liver fibrosis in heavy‐drinking patients is a challenge. Aims To assess Fibroscan for non‐invasive diagnosis of asymptomatic liver fibrosis in alcohol abuse patients, to determine diagnostic liver stiffness cut‐off values and to compare performance of Fibroscan with seven non‐invasive laboratory tests. Methods One hundred and three alcoholic patients were studied. Liver fibrosis was staged by METAVIR system. Fibroscan, Fibrotest, Fibrometer, Hepascore, APRI, PGA, PGAA and hyaluronic acid tests were performed. Liver stiffness cut‐offs were determined using receiver‐operating characteristic (ROC) curves. Results Liver stiffness was correlated with fibrosis (r = 0.72, P < 0.014), with median at 5.7, 6.3, 8.4, 15 and 47.3 kPa for F0 (n = 8), F1 (n = 18), F2 (n = 24), F3 (n = 20) and F4 (n = 33) stage fibrosis respectively. For Fibroscan, areas under ROC curves (AUROCs) were 0.84 (95% CI: 0.73–0.95) (F ≥ 1), 0.91 (0.85–0.98) (F ≥ 2), 0.90 (0.82–0.97) (F ≥ 3) and 0.92 (0.87–0.98) (F = 4), yielding diagnostic stiffness cut‐offs of 5.9 (F ≥ 1), 7.8 (F ≥ 2), 11 (F ≥ 3) and 19.5 (F4) kPa. Sensitivity, specificity, PPV and NPV were 80%, 90.5%, 93% and 70% for F ≥ 2, and 85.7%, 84.2%, 68.6% and 87.9% for F = 4. Performance of Fibroscan was higher than seven laboratory tests, for which AUROCs ranged from 0.66 to 0.77 (F ≥ 1), from 0.54 to 0.82 (F ≥ 2), from 0.43 to 0.88 (F ≥ 3) and from 0.56 to 0.89 (F = 4), with significant difference only vs. APRI (P < 0.001) and Hepascore (P = 0.04). Combining Fibroscan with each tests did not improve performance. Conclusions Fibroscan is effective to assess liver fibrosis in alcoholic patients. Instant screening of liver fibrosis in heavy drinkers is feasible without liver biopsy.