Bioactivity and chemical composition of the essential oil from the leaves of Guatteria australis A.St.-Hil

Essential oil from the leaves of Guatteria australis was obtained by hydrodistillation, analyzed by Gas Chromatography coupled to Mass Spectromery (GC–MS) and their antiproliferative, antileishmanial, antibacterial, antifungal and antioxidant activities were also evaluated. Twenty-three compounds were identified among which germacrene B (50.66%), germacrene D (22.22%) and (E)-caryophyllene (8.99%) were the main compounds. The highest antiproliferative activity was observed against NCI-ADR/RES (TGI = 31.08 μg/ml) and HT-29 (TGI = 32.81 μg/ml) cell lines. It also showed good antileishmanial activity against Leishmania infantum (IC₅₀ = 30.71 μg/ml). On the other hand, the oil exhibited a small effect against Staphylococcus aureus ATCC 6538, S. aureus ATCC 14458 and Escherichia coli ATCC 10799 (MIC = 250 μg/ml), as well as small antioxidant activity (457 μmol TE/g) assessed through ORAC_FL assay. These results represent the first report regarding chemical composition and bioactivity of G. australis essential oil.     

新型2-[4-(取代苯甲酰氨基)苯基]苯并噻唑的合成及生物活性

以2-氨基苯硫酚和对氨基苯甲酸为起始原料,设计并合成了5个新型的苯并噻唑衍生物(4a~4e),其结构经1H NMR,IR,MS(EI)和元素分析表征。采用菌丝生长速率法初步研究了4a~4e的生物活性。结果表明:用药浓度为100 mg·L~(-1)时,4b和4c对西瓜枯萎病菌有一定抑制效果,抑制率分别为47%和43%。     

2-氰基-3-取代胺基-3-[2-(4-氟苯基)-乙胺基]丙烯酸乙酯类化合物的合成及生物活性研究

以氰基乙酸乙酯为原料,经与二硫化碳、硫酸二甲酯反应合成了2-氰基-3,3-二甲硫基丙烯酸乙酯(1),然后引入对氟苯乙胺得到化合物(3),其与脂肪胺反应合成了新型含对氟苯乙氨基的2-氰基丙烯酸乙酯类化合物5a～5h,其结构经元素分析,IR1H NMR和13C NMR等确证.初步生物活性试验表明,部分化合物具有一定抗烟草花叶病毒活性.     

新型含2-取代-1,3-噻唑烷环的噻唑酰胺类化合物的合成与生物活性研究

为了寻找新的含噻唑杂环的先导化合物,利用¨(2-氰基亚胺基-1,3-噻唑烷-3-基)甲基]-2-氨基噻唑与取代苯甲酰氯(或乙酰氯)在吡啶存在下发生缩合反应,合成了19个新型含2-取代-1,3-噻唑烷环的噻唑酰胺类化合物4.经1HNMR和元素分析对目标化合物的结构进行了表征,经MS进一步证实了化合物4s的结构,并通过X射线单晶衍射分析测定了化合物4a的晶体结构.对所合成的目标化合物进行了生物活性测试,部分化合物表现出一定的杀菌和植物生长调节活性.     

The Occurrence and Biological Activity of Tormentic Acid—A Review

This review focuses on the natural sources and pharmacological activity of tormentic acid (TA; 2α,3β,19α-trihydroxyurs-2-en-28-oic acid). The current knowledge of its occurrence in various plant species and families is summarized. Biological activity (e.g., anti-inflammatory, antidiabetic, antihyperlipidemic, hepatoprotective, cardioprotective, neuroprotective, anti-cancer, anti-osteoarthritic, antinociceptive, antioxidative, anti-melanogenic, cytotoxic, antimicrobial, and antiparasitic) confirmed in in vitro and in vivo studies is compiled and described. Biochemical mechanisms affected by TA are indicated. Moreover, issues related to the biotechnological methods of production, effective eluents, and TA derivatives are presented.     

Molecular Control of Bioactivity in Sol-Gel Glasses

Bioactive materials can be divided into: Class A bioactive glasses which exhibit rapid bonding to bone and soft connective tissue and are osteoproductive, and osteoconductive; and Class B bioactive ceramics, which bond slowly only to bone and are only osteoconductive. Bioactive sol-gel glasses composed of SiO2-CaO-P2O5 have Class A behavior in vitro and in vivo and also resorb as they enhance the proliferation of new trabecular bone.     

Synthesis and bactericidal activities of novel pyrazole-1-carbothioamide derivatives

4-(2-Hydroxy-phenyl)-but-3-en-2-one (1) was prepared via condensation of salicylaldehyde with acetone, and then reaction of the ketone 1 with thiosemicarbazide was accompanied by cyclization to give substituted pyrazole (2). Seven new 5-(2-hydroxy-phenyl)-3-methyl-4,5-dihydropyrazole-1-carbothioamide derivatives (3a–3g) were synthesized by the acylation of 2 and characterized by means of elemental analysis, infrared (IR), and ¹H nuclear magnetic resonance (NMR). The compounds 3c, 3d, and 3g showed certain bactericidal activity against E. coli; while compound 3g showed certain bactericidal activity against P. vulgaris. Translated from Chinese Journal of Applied Chemistry, 2006, 23(12): 1355–1358 [译自: 应用化学]     

取代酰胺类化合物的合成及其生物活性

为优化抗倒胺结构。合成了３０种化合物，用ＩＲ，１ＨＮＭＲ及元素分析确定了结构，并进行了水稻发芽试验及田间试验。     

Effects on the Thermal Properties and Bioactivity of Substitution of CaO by M2O3 (M=La, Y, Al) in Wollastonite Glass

The effects on the thermal properties and bioactivity of the substitution of CaO by La₂O₃, Y₂O₃ and Al₂O₃ in a glass of composition CaO·SiO₂ were studied and compared. The trivalent metal oxides were all effective in raising the glass transformation and softening temperatures when they replaced CaO in the glass of composition CaO·SiO₂. The experimental results suggest that Al₂O₃ plays the role of a glass-former, while La₂O₃ and Y₂O₃ behave as glass-modifiers. The tendency to devitrify appears to be the lower, the farther the glass composition is from those of the crystalline phases, owing to the need for diffusion over longer distances, the greater the composition difference. The substitution with the trivalent metal oxides is detrimental to the bioactivity, which is preserved only in the event of very small degrees of substitution. The most negative role appears to be played by Al₂O₃. This revised version was published online in July 2006 with corrections to the Cover Date.     

Study of the crystal shape and its influence on the anti‐tumor activity of tumor necrosis factor‐related apoptosis‐inducing ligand (Apo2L/TRAIL)

This paper describes a method about the crystal shape control improving the anti‐tumor activity of tumor necrosis factor‐related apoptosis‐inducing ligand (Apo2L/TRAIL) in a batch cooling suspension crystallization by selecting pH values as a controllable variable. Three shaped TRAIL crystals could be obtained under different pH conditions, among which the hexagonal plate crystals had the highest specific activities against tumor cell line. The relationship among pH values, trimer contents and the specific activities of crystals and the purified TRAIL solutions were investigated. The results showed that different trimer contents resulted from pH altering in crystals and protein solutions is a main reason for their different specific activities. The studies may supply a new method to improve the bioactivity of TRAIL agent during its production and storage. (© 2008 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)