丹参新醌丁的分离与结构测定

丹参(Salvia miltiorrhiza)中含量较高的是以邻醌为主如丹参酮Ⅰ及丹参酮Ⅱ_A等,而以对醌存在的尚有异丹参酮等,但含量均极低。此外,国内还报道了显示酸性的丹参新醌甲、乙,丙。鉴于隐丹参酮、二氢丹参酮Ⅰ加碱开环后可转化为丹参新醌,因此如不用碱处理能否从原植物中获得新醌尚属未定。本文报道采用中性溶剂系统进行硅胶柱层析,获得了丹参新醌甲与乙,此外还得到一种新的对醌化合物,不同于已报道的异丹参酮,定名为丹参新醌     

白花丹参化学成分的研究

从白花丹参(Salvia miltiorrhiza f.alba)中分离出14个二萜醌类化合物,其中2个为新化合物,由光谱分析推定为1,2,15,16-四氢丹参醌(Ⅰ)和丹参醛(Ⅱ);另一个化合物Ⅲ与R₀-090680的结构相同。化合物Ⅰ和Ⅲ对淋巴白血病细胞P₃₈₈均有较强的抑制作用。     

丹参新酮C环酚酯衍生物的设计合成及抗肿瘤活性研究

目的：通过对丹参新酮C环邻醌位点的结构修饰,改变其脂水分配系数(CLogP),获得系列丹参新酮酚酯衍生物,进而评价其抗肿瘤活性。方法：采用氢化还原、酰化、脱保护基等方法对丹参新酮的邻醌位点进行修饰,通过引入不同酸酐、氨基酸取代基,得到丹参新酮C环酚酯衍生物,在此基础上以前列腺癌Lncap和Du145细胞株对部分化合物进行抗肿瘤活性评价。结果：共合成了9个新的丹参新酮酚酯衍生物,其中1个化合物表现出较好的抗肿瘤活性。结论：脂水分配系数的改变对丹参新酮衍生物抗肿瘤活性影响很大,适当提高水溶性,有助于增强其抗肿瘤活性,改善成药性。     

三叶鼠尾草化学成分的研究

自从丹参酮Ⅱ-A磺酸钠一类化合物应用于冠心病临床以来,我们对同科属植物中二萜醌类的化学成分进行了研究,在寻找资源和新的二萜醌类活性物质过程中,除将甘西鼠尾草褐毛变种[Salvia przewalskli Maxim Var mandarinorum(Diels) Stib]俗名紫丹参推荐工厂,作为投产之原料外,又找到了含丹参酮Ⅱ-A高达0.6%的三叶鼠尾草。     

丹参新醌丁的分离与结构测定

A new diterpenequinone named danshenxinkun Dwas isolated from Salvia miltiorrhiza Bunge. The structure of danshenxinkun-D (C₂₀H₂₁O₄) mp. 178～180℃ was put forward as (Ⅰ) by spectral analysis. The compound was shown to have antituberculosis H₃₇Rv activity in vitro.     

华北白前中的新三萜成分

从华北白前(Cynanchum hancockianum)中分离到4个新三萜类化合物,通过光谱分析(¹HNMR,¹³CNMR,2DNMR,MS,X-Ray)及化学相关等分别鉴定为华北白前醇(hancockinal,Ⅰa).新自前醇(hancolupenoI,Ⅱd),新白前酮(hancolupenone,Ⅱc)及新白前醇二十八烷酸酯(hancolupenol octacosanate,Ⅱd),均为新型骨架的化合物。     

丹参二萜醌全合成研究概况

概述了丹参的有效成分如丹参酮Ⅰ、丹参酮Ⅱ-A、隐丹参酮等9个丹参二萜醌的合成研究。     

新二萜醌——红根草对醌

红根草Saluia prionitis Hance系唇形科鼠尾草属植物,为江南民间常用草药。全草治疗腹泻菌痢,扁桃腺炎,咽喉炎,并有抗结核麻疯作用,已从其中分到新天然产物红根草邻醌和丹参酮ⅡA,丹参酮Ⅰ等二十余个化合物。本文报道新二萜醌红根草对醌的分     

丹参治疗小儿过敏性紫癜的进展

丹参始载于<神农本草经>.丹参主要含丹参酮1A、ⅡB,隐丹参酮,二氢异丹参酮Ⅰ以及多种含量较少的醌类色素,如羟基丹参酮;异丹参酮Ⅰ、Ⅱ,异隐丹参酮,次丹参醌等;另含丹参素,鼠尾草酚,原儿茶醛等酚类分.     

乌棒子甙甲和甙乙的分离鉴定

从远志科植物乌棒子(Polygala caudata Rehd et Wils)的根皮和茎皮中分得四种(口山)酮类成分和一种甾醇甙,分别鉴定为优(口山)酮(Ⅰ),豆甾醇葡萄糖甙(Ⅱ),乌棒子甙甲(wubangziside A,Ⅲ),乌棒子甙乙(wubangziside B,Ⅳ)和芒果甙(Ⅴ)。本文报道两种新(口山)酮甙乌棒子甙甲和甙乙的结构测定以及三种已知化合物的鉴定工作。     

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%.     

Chemical Composition of Essential Oils from Leaves and Twigs of Pistacia lentiscus,Pistacia lentiscus var. chia,and Pistacia terebinthus from Turkey

The composition of the essential oils from the leaves and twigs of Pistacia lentiscus L., Pistacia lentiscus var. chia (L.), and Pistacia terebinthus L. of Turkish origin were analyzed by gas chromatography/mass spectrometry (GC/MS). Seventy-seven constituents were characterized from the essential oil of P. terebinthus leaves with α-cadinol (6.9%), phytol (5.4%), δ-cadinene (5.1%), α-terpineol (5.0%), and bornyl acetate (4.4%) as major constituents. Germacrene D (10%), β-pinene (7.5%), bornyl acetate (6.0%), α-cubebene (5.9%), and cubebol (5.4%) were found to be the main components among the 61 compounds characterized in the essential oil of P. terebinthus twigs. Forty-six compounds were characterized from the essential oil of P. lentiscus twigs with sabinene (23.2%), α-pinene (19.4%), germacrene D (14.1%), limonene (6.9%), β-phellandrene (6.5%), terpinene-4-ol (5.7%), and β-caryophyllene (5.7%) as the main constituents. Terpinene-4-ol (29.2%), β-caryophyllene (29.2%), and p-cymene (7.1%) were identified as the major components among the 64 compounds characterized in the essential oil of P. lentiscus leaves. Sixty-eight compounds were found on the essential oil of P. lentiscus var. chia leaves with germacrene D (20.1%), myrcene (13.9%), β-caryophyllene (10.8%), and α-terpinyl acetate (4.8%) as the major constituents. Myrcene (27.4%), germacrene D (21.7%), and β-caryophyllene (7.2%) were found to be the main components among 50 compounds characterized in the essential oil of P. lentiscus var. chia twigs.     

香薷挥发油成分的研究

本文用GLC等方法鉴定和测定了海州香薷挥发油中对聚繖花素(10.43%)、百里香酚(30.05%)、香荆芥酚(33.39%)、α-反式-香柠檬烯(1.64%)等12个成分,并与川香薷挥发油的成分进行了分析比较。     

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.     

中药大血藤的酚性化合物

目的对中药大血藤干燥藤茎的化学成分进行研究。方法采用现代色谱技术分离化合物，运用现代波谱技术(IR，MS，¹H NMR，¹³C NMR，²DNMR)对所得化合物的结构进行鉴定。结果从大血藤的藤茎中分得10个酚类化合物，分别鉴定为1-O-(香草酸)-6-(3″,5″-二-O-甲基-没食子酰基)-β-D-葡糖苷(I)、(-)-表儿茶素(II)、阿魏酸-对羟基苯乙醇酯(III)、3-O-咖啡酰奎宁酸(IV)、3-O-咖啡酰奎宁酸甲酯(V)、罗布麻宁(VI)、香草酸(VII)、原儿茶酸(VIII)、3,4-二羟基-苯乙醇(IX)、4-羟基-苯乙醇(X)。结论化合物I为新化合物，化合物III～VI和VIII～X为首次从该植物中分得。     

栾树的化学成分

目的：分离鉴定栾树(Koelreuteria paniculata Laxm)叶的化学成分。方法：95%工业EtOH浸提,硅胶柱色谱分离,IR,MS,UV,1HNMR,¹³CNMR等方法确定结构。结果：分得14个化合物,分别为对-二没食子酰乙酯(ethyl-p-digallate)(1),间二没食子酰乙酯(ethyl-m-digallate)(2),对-二没食子酸(p-digalloyl acid)(3),间-二没食子酸(m-digalloyl acid)(4),2″-没食子酰基槲皮素苷(quercitrin-2″-gallate)(5),没食子酸(galloyl acid)(6),没食子酸乙酯(ethyl galloyl acid)(7),鞣花酸(ellagic acid)(8),槲皮苷(quercitrin)(9),金丝桃苷(hyperin)(10),山奈酚-3-O-鼠李糖苷(kaempferol-3-O-rhamnoside)(11),2″-没食子酰金丝桃苷(hyperin-2″-gallate)(12),β-谷甾醇(β-sitosterol)(13),β-谷甾醇-3-O-葡糖苷(β-sitosterol 3-O-gluceroside)(14)。结论：对-二没食子酰乙酯(ethyl-p-digallate)(1),间二没食子酰乙酯(ethyl-m-digallate)(2),对-二没食子酸(p-digalloyl acid)(3)为新化合物,化合物4,5,8～12和14系首次从该植物中分得。并首次系统归属其波谱信号。     

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.