Covalently cyclized agonist and antagonist analogues of bombesin and related peptides.

During a search for possible cyclization points in shortened, potent bombesin agonists and antagonists, it was found that the joining of amino acid residues in positions 6 and 14 by various means resulted in retention of significant binding affinity for rat pancreatic acini and murine Swiss 3T3 cells. In one series of analogues, Cys residues in these positions were used for bridging via a disulfide bond. (D)-C-Q-W-A-V-G-H-L-C-NH2 retained significant binding affinity for rat pancreatic acini cells and was a full amylase releasing agonist (EC50 187 nM). Potency was markedly increased by substituting D-Ala for Gly (EC50 67 nM compared to 10 nM for its linear counterpart) and was decreased by substituting L-Cys for D-Cys in this analogue (EC50 214 nM), thus strongly suggesting stabilization of peptide folding by the D residues. Elimination of the COOH-terminal amino acid produces competitive antagonists in the linear analogues; however, (D)-C-Q-W-A-V-G-H-C-NH2 was devoid of activity. Likewise, cyclization to position 13 with the 14 amino acids intact to give (D)-C-Q-W-A-V-G-H-C-L-NH2 resulted in an almost inactive peptide. On the other hand, as in the linear series, the reduced peptide bond analogue, (D)-C-Q-W-A-V-(D)-A-H-L-psi (CH2NH)-C-NH2, was a receptor antagonist (IC50 5.7 mM), albeit much weaker than the corresponding linear analogues, but with no residual agonist activity. Direct head-to-tail cyclization was also tried. Both cyclo[(D)-F-Q-W-A-V-G-H-L-L] (EC50 346 nM) and the shorter cyclo [Q-W-A-V-G-H-L-L] (EC50 1236 nM) were full agonists. Elimination of the COOH-terminal residue in cyclo[(D)-p-Cl-F-Q-W-A-V-(D)-A-H-L] produced an agonist (EC50 716 nM) rather than an antagonist. These results provide support for the proposal that both bombesin agonists and antagonists adopt a folded conformation at their receptor(s). Furthermore, the retention of appreciable potencies using several cyclization strategies and chain lengths suggests that further optimization of these structures both in terms of potency and ring size is possible. Since these peptides have increased conformational restriction, they should begin to serve as useful substrates for NMR and molecular modeling studies aimed at comparing the obviously subtle differences between agonist and antagonist structures.     

影响光合细菌类胡萝卜素形成因素的研究

对已初步确认为球形红假单胞菌属的S—1菌株进行了类胡萝卜素形成因素的研究。通过对光照强度、温度、pH、碳源、氮源、生长因子和无机盐成份等培养条件的探讨,找到了适合类胡萝卜素形成的条件,为开发光合细菌类胡萝卜素提供了依据。     

Reduced susceptibility to HIV-1 infection of ethyl-methanesulfonate-treated CEM subclones correlates with a blockade in their protein kinase C signaling pathway.

We have described the isolation of chemically induced CEM subclones that express CD4 receptors and bind soluble gp120, yet show a markedly reduced susceptibility to infection with HIV-1. Two subclones were found to have an abnormal response to the protein kinase C (PKC) activator PMA. PMA treatment induced CD3 and CD25 (IL-2R) receptors on the parental line and on other ethyl-methanesulfonate-derived subclones, but not on these two mutants. Direct assays of PKC activity were conducted. Total cellular PKC enzymatic activity was found to be normal in these subclones. PMA-induced CD4 down-modulation occurred normally. In addition, activation of c-raf kinase was normal. Since HIV-1 long terminal repeat contains two functional nuclear factor kB (NF-kB) regulatory elements, we studied the ability of PMA to induce NF-kB binding activity by different assays. Chloramphenicol acetyl transferase (CAT) assays using the HIV-1 (-139)long terminal repeat-CAT construct showed no PMA induction of CAT activity in these subclones (unlike the parental line and other subclones). Okadaic acid, an inhibitor of phosphatases 1 and 2A, did not overcome the defect in these subclones. Gel retardation assays, using a 32P-probe containing the HIV-1 NF-kB probe and nuclear extracts from PMA-treated cells, showed significantly reduced induction of nuclear NF-kB binding proteins in these two subclones compared with wild type CEM and a control subclone. Deoxycholate treatment of cytoplasmic extracts from these subclones released much reduced NF-kB binding proteins from their cytoplasmic pools. Thus, reduced levels of PKC-induced nuclear NF-kB activity in two T cell subclones did not affect their normal cell growth, but correlated with a pronounced reduction in their susceptibility to HIV-1 infection.     

Vibrational analysis of crystalline tri-L-alanine

We have found that tri-L-alanine (Ala3) can crystallize in a parallel-chain beta structure in addition to the previously known antiparallel-chain beta structure. Although the chain conformations in each structure are essentially similar, the ir and Raman spectra are distinctively different. We have calculated the normal modes of each structure, and can account in significant detail for these differences. This demonstrates the essential validity of our empirically refined force fields, as well as showing that deeper insights into polypeptide and protein structure can be achieved through the rigorous analyses of normal mode calculations.     

水稻食叶类害虫等量损害系统与复合防治指标

稻纵卷叶螟Cnaphalocrocis.medinalis Guenèe中华稻蝗Oxya chinensis(Thunberg)稻苞虫Parnara guttatus (Bremer et Grey)是江苏地区水稻的主要食叶类害虫,取食水稻叶片,导致光合叶面积减少.剪叶模拟试验表明,水稻不同生育阶段叶面积损失率与产量损失率呈线性相关.其回归方程分蘖期、孕穗期、腊熟期分别为 D(I_t)=72.50759I_t^1.15906、D(I_t)=141.61737I_t^1.08002、D(I_t)=25.12434I_t^1.00569.在叶面积损失率相同的情况下,产量损失率孕穗期>分蘖期>腊熟期.试验通过三种害虫的各龄取食量,不同生育阶段水稻叶面积及为害与损失率之间的关系,建立了不同生育阶段的经济允许损害水平(EIL_t).并根据各种害虫的相对潜在取食量,计算了校正等量损害系数,为制订复合防治指标提供了依据.实践证明:以等量损害为单位的复合防治指标有较大的实用价值,生态效益、经济效益、社会效益明显.     

外生菌根的形态学、解剖学及分类学研究进展

本文综述了外生菌根的形态学和解剖学特征,评价了这些特征用于外生菌根分类的价值,同时指出各种类型的形态学特征和解剖学特征与其营养吸收的关系。这些特征包括了菌根的颜色类型及变化、形状及分枝方式、外伸菌丝的多少及特征、根状菌索有无及分化、菌核有无及特征、菌套内外表面的菌丝排列及分化,菌套的切面特征,丹宁层厚度及分化、哈氏网的菌丝排列及厚度等。较详细阐述了100多年来,人们为外生菌根分类所作出的种种努力,并对各种分类方式作了简单的评价。     

中国蝼蛄菌属的研究

本文报道寄生于我国非洲蝼蛄(Gryllotalpa africana Palisot de Beauvois)上的蝼蛄菌属(Tettigomyces)11个种,其中新种1个:线状蝼蛄菌(T.filiformis Ye);国内新记录种10个:渐尖蝼蛄菌(T.acuminatus Thaxt.),非洲蝼蛄菌(T.africanus Thaxt.),短蝼蛄菌(T.brevis Thaxt.),毛生蝼蛄菌(T.chaetophilus Thaxt.),混淆蝼蛄菌(T.co-nfusus Thaxt.),蝼蛄菌(T.gryllotalpae Thaxt.),印度蝼蛄菌(T.indicus Thaxt.),间型蝼蛄菌(T.intermedius Thaxt.),翅生蝼蛄菌(T.pterophilus Thaxt.),普通蝼蛄菌(T.vulgaris Thaxt.)。本文所研究的全部标本都保存于广东省微生物研究所。     

Pulmonary vascular reactivity and hemodynamic changes in elastase-induced emphysema in hamsters.

Changes in pulmonary hemodynamics and vascular reactivity in emphysematous hamsters were studied in an isolated lung preparation perfused at constant flow with blood and 3% dextran. Hamsters were treated with intratracheal porcine pancreatic elastase at 70 days of age, and experimental studies were conducted at 1, 3, and 8 mo after treatment. Baseline pulmonary arterial pressure in elastase-treated lungs was increased compared with saline-treated control lungs 1 mo after treatment, but this increase did not progress at 3 and 8 mo. Increases in pulmonary arterial pressure in elastase-treated lungs were temporally correlated with the morphological development of emphysema and right ventricular hypertrophy; both of these were evident at 1 mo after treatment and showed little change thereafter. Pressor responses to hypoxia and angiotensin II were not different between elastase-treated and control lungs at 1 and 3 mo. At 8 mo, however, pressor responses in emphysematous lungs to 0% O2 (but not to angiotensin II) were significantly increased. This was the result of a lack of the normal age-related fall in the hypoxic pressor response. Our results suggest that the right ventricular hypertrophy found in these emphysematous animals results from a chronically increased pulmonary vascular resistance. Furthermore, increases in pulmonary vascular resistance in the early development of emphysema are likely a result of the loss of vascular beds and supporting connective tissue.     

山林原白蚁栖居地及各品级记述

瑞典白蚁专家Holmgren记载了亚洲的两种原白蚁:山林原白蚁Hodotermopsis sjstedt Holmgren(1911)和日本原白蚁Hodotermopsis japonicus Holmgren(1912)。经蔡邦华教授(1980)进一步研究认为是山林原白蚁的同物异名。作者根据浙江(龙泉)、山林原白蚁的栖居地及其巢内的诸品级发生情况,于1975—1980在龙泉进行了逐年调查。现将调查结果报道如下:     

新疆副新蚤属一新种记述(蚤目:毛蚤科)

球副新蚤Paraneopsylla globa新种 鉴别特征 本新种与深窦副新蚤(P.ioffi Tiflov,1937)的形态比较相似,其主要区别是新种第9腹板后臂前缘近端处明显前凸,后缘虽微凹但未形成深窦,端部纯圆,未形成背角;阳茎钩突除端部膜状增宽外,基部尚赘生大的球形膜状物。新种♀第7腹板端缘上叶突出比较狭小。 形态记述 头部(图1)额瘤齿状,嵌于额缘近下1/4处。下唇须约达前足基节长的3/4—4/5。额宗列3—4支宗,均较细小。眼宗列3支宗,较粗长。后头宗3列,依次为1—2、2—3、5—6支,前两列除下位宗外均较细小。 胸部(图1):前胸栉两侧共有栉刺14支,栉前有一列宗4—6支。中胸背板有两列较完整的宗,其前尚有不少小宗,颈片每侧具假宗1—3支。 部分标本后胸背板后缘有1—2个端齿。前足基节外面有宗40—50支。后足基节内面有细宗25—40支,多位于近