Evaluation of chemical composition and antiedematogenic activity of the essential oil of Hyptis martiusii Benth

Evaluations of the therapeutic potential of medicinal plants and their components have been the subject of many studies. Furthermore, the biological activities of various plant species have been reported in various pieces of literature. Hyptis martiusii Benth (Lamiaceae), popularly known as “mad balm” is commonly found in the North, Southeast, and Northeast of Brazil. Its leaves are used ethnobiologically as antiulcerogenic, antimicrobial, antitumor and as insecticide. This study aimed to analyze the chemical composition of the essential oil of H. martiusii Benth (OEHM) by GC/MS as well as its possible topical activity as an antiedematogenic. This is verified by the models of ear edema induced by single (acute edema) and multiple (chronic edema) applications of croton oil topically, and systemically verified through the model of paw edema induced by carrageenan 1%. Doses of 50, 75 and 100 mg/kg OEHM were used in all tests. Chemical analysis of the oil revealed the 1,8-cineole (34.58%) and δ-carene (21:58%) as major components present in the essential oil. On the model of ear edema, acute and chronic OEHM in all the tested doses showed no significant antiedematogenic activity (p < 0.05). The systemic model of paw edema induced by carrageenin showed that a dose of 100 mg/kg effectively reduced swelling by 55.37% in the second hour evaluation when compared to the saline group. The anti-inflammatory systemic effect can give greater bioavailability of the components present in the essential oil and your interference in cytokines and leukotriene, thromboxane and prostaglandin biosynthesis. It is therefore concluded that OEHM presents systemic antiedematogenic activity but not topical activity at these doses.     

Chemical composition,antibacterial and antifungal activities of flowerhead and root essential oils of Santolina chamaecyparissus L., growing wild in Tunisia

The antimicrobial properties of essential oil from various Santolina species have not been investigated enough in the previous studies dealing with the biological activities of medicinal plants. In Tunisia, Santolina chamaecyparissus L. (Asteraceae) is the only Santolina species recorded and is used as vermifuge and emmenagogue. The chemical composition, antibacterial and antifungal properties of essential oils from the flowerheads and roots of spontaneous S. chamaecyparissus growing in Tunisia and the chemical composition which leads to the Tunisian chemotype are investigated here for the first time. Essential oils isolated by hydro distillation from flowerheads and roots of S. chamaecyparissus were analyzed by GC and GC/MS. Two methods served for antimicrobial assays of the essential oils: diffusion in a solid medium and micro-well dilution assay. Antifungal tests were carried out by the agar incorporation method. Sixty-seven constituents were identified from the essential oil of the flowerhead. The major constituents were: 1,8-cineole and β-eudesmol. Two non identified compounds were present at the highest concentration in root oil. Flowerhead oil was characterized by high contents in monoterpenes and sesquiterpenes oxygenated compounds. The flowerhead essential oil demonstrated potent of antibacterial properties against Pseudomonas aeruginosa ATCC and Enterococcus faecalis ATCC, with MIC of 0.625 μg/ml. These findings demonstrate that the flowerhead essential oils of S. chamaecyparissus have excellent antibacterial properties and for this reason they could contribute to decrease the problem of microbial resistance to antibiotics.     

Anti-oxidative effects of silkworm storage protein 1 in HeLa cell

Silkworm hemolymph contains unique proteins that exhibit anti-apoptotic activity in mammalian cells. Among them, 30 K protein, which is one of the major anti-apoptotic molecules in silkworm hemolymph, has been well investigated. However, little is known about the biological functions of storage protein 1 (SP1), another main protein in silkworm hemolymph. In this study, the anti-apoptotic and anti-oxidative activities of SP1 were analyzed. A stable cell line expressing SP1 was constructed, which showed strong anti-apoptotic effect induced by staurosporine treatment. In addition, the cell line exhibited resistance to oxidative stress caused by hydrogen peroxide. For practical applications of SP1, recombinant SP1 was produced in Escherichia coli, and the supplementation of recombinant SP1 into culture medium exhibited anti-apoptotic and anti-oxidative activities. In addition, SP1 was found to be a cell-penetrating protein and localized in the cytosol as well as on the plasma membrane. The findings showed that SP1 itself is not an anti-oxidant; rather, it mediates intracellular anti-oxidative activity. In conclusion, the cellular resistance of SP1 to apoptosis and oxidative stress will provide a new strategy that could be utilized in the bio-industry for the production of biologics as well as for the development of anti-aging cosmetics.     

血小板生成素与白介素-11治疗胃癌术后辅助化疗后血小板减少症时效及安全性的比较

目的:比较血小板生成素与白介素-11治疗胃癌患者术后化疗血小板减少症的时效和安全性。方法:术后辅助化疗出现血小板计数低于75×109/L的进展期胃癌患者68例,将其分为TPO组与IL-11组,分别为35例和33例。分别皮下注射rhTPO 15000U,每日1次;rhIL-11 1.5 mg,每日1次,当血小板计数125×109/L或比用药前上升50×109/L,即停止给药,疗程最长为14天。每3天抽取外周静脉血2 m L,通过全自动血液分析仪测定血小板计数,密切观察出现的不良反应并记录。比较两组患者不同临床病理资料、血小板计数、血小板计数升至75×109/L和125×109/L的时程、药物不良反应。结果:两组患者年龄、性别、化疗方案、血小板最低值出现的化疗周期及临床病理分期的比较均没有统计学差异(P值均0.05)。TPO组与IL-11组血小板动态值的比较,第9天出现显著差异(P=0.032)。TPO组与IL-11组血小板计数恢复至75×109/L和125×109/L所需的时间,有显著差异(P=0.041,P=0.013)。TPO组中,有3例(8.6%)患者发生不良反应,IL-11组中,有13例(39.4%)患者发生不良反应,TPO组患者出现的不良反应少且较轻微(P=0.006)。结论:rhTPO治疗胃癌患者术后化疗血小板减少症时效快,安全性好。     

Novel degraded polycyclic polyprenylated acylphloroglucinol and new polyprenylated benzophenone from Hypericum sampsonii

Norhypersampsone A (1), a novel degraded polycyclic polyprenylated acylphloroglucinol (PPAP) derivative, 3-(2-hydroxy-7-methyl-3-methyleneoct-6-enyl)-5-isoprenyl-2,4,6-trihydroxybenzophenone (2), a new polyprenylated benzophenone derivative, and nine known compounds (3–11) were isolated from Hypericum sampsonii. Their structures were elucidated by comprehensive spectroscopic techniques. Compound 1 represents a novel cyclohexenone monocyclic-PPAP formed by losing the fragment of C-2–C-4 and the side chains at C-3 and C-5 in the phloroglucinol ring. The results of the inhibitory effects of compounds 1–11 on the nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW 264.7 macrophages showed that compounds 1, 6–8, and 10 exhibited weak activities with IC₅₀ values in the range of 20.3–37.1 μM.     

Pregnane alkaloids from Sarcococca ruscifolia and their cytotoxic activity

Six pregnane alkaloids were isolated from the root of Sarcococca ruscifolia. The structures of three new alkaloids, namely, sarcorucinine E–G (1–3), were elucidated using spectroscopic methods, while three known alkaloids, namely, epipachysamine D, pachysamine M, and sarcovagine D, were identified by comparing their spectral data with those of the compounds reported earlier. All compounds were evaluated for their inhibitory activities against multiple types of cancer cells.     

Aggregation prone regions in human proteome: Insights from large‐scale data analyses

Protein aggregation leads to several burdensome human maladies, but a molecular level understanding of how human proteome has tackled the threat of aggregation is currently lacking. In this work, we survey the human proteome for incidence of aggregation prone regions (APRs), by using sequences of experimentally validated amyloid‐fibril forming peptides and via computational predictions. While approximately 30 human proteins are currently known to be amyloidogenic, we found that 260 proteins (～1% of human proteome) contain at least one experimentally validated amyloid‐fibril forming segment. Computer predictions suggest that more than 80% of the human proteins contain at least one potential APR and approximately two‐thirds (65%) contain two or more APRs; spanning 3–5% of their sequences. Sequence randomizations show that this apparently high incidence of APRs has been actually significantly reduced by unique amino acid composition and sequence patterning of human proteins. The human proteome has utilized a wide repertoire of sequence‐structural optimization strategies, most of them already known, to minimize deleterious consequences due to the presence of APRs while simultaneously taking advantage of their order promoting properties. This survey also found that APRs tend to be located near the active and ligand binding sites in human proteins, but not near the post translational modification sites. The APRs in human proteins are also preferentially found at heterotypic interfaces rather than homotypic ones. Interestingly, this survey reveals that APRs play multiple, often opposing, roles in the human protein sequence‐structure‐function relationships. Insights gained from this work have several interesting implications towards novel drug discovery and development. Proteins 2017; 85:1099–1118. © 2017 Wiley Periodicals, Inc.     

The Cultural-Historical Development of Mental Processes and the Theory of Stepwise Formation of Mental Actions and Concepts

The article examines the problem of the relationship between universal and specific forms of cultural–historical development of mental processes. From different methodological approaches, the author prefers an activity approach which emphasizes genetic primacy of external practical activity. This approach allows, according to the author, universality of internalization and at the same time ethnic uniqueness of mental processes. The article clarifies the problem of internalization through two practical examples: 1) the development of mental counting actions and 2) the process of human goal setting.