江西省缓步动物四个新纪录种记述

本文报道了江西省缓步动物4个新记录种:双裂角棘影熊虫Cornechiniscus lobatusRamazzotti,1943(异缓步纲,棘影熊虫科),节值大生熊虫Macrobiotus harmsworthiMurray,1907(真缓步纲,大生熊虫科),胡氏大生熊虫Macrobiotus hufelandiSchultze,1833(大生熊虫科)和杜氏高生熊虫Hypsibius dujardiniDoyére,1840(高生熊虫科)。     

缓步动物门三新种及一新记录种记述

记述了得自云南省和河南省苔藓与丝状绿藻中的缓步动物门三新种和一新记录种:异缓步纲棘影熊虫科的西藏角棘影熊虫新记录种 Cornechiniscus tibetanus)Maucci, 1979)和石林假棘影熊虫,新种 Pseudechiniscus shilinensis sp. nov.;真缓步纲大生熊虫科的河南趾生熊虫,新种 Dactylobiotus henanensis sp. nov.;高生熊虫科的昆明高生熊虫,新种 Hypsibius kunmingensis sp. nov..       

中国缓步动物门二新种及三新纪录种和亚种(异缓步纲,棘影熊虫科;真缓步纲,小斑熊虫科,大生熊虫科,高生熊虫科)

记述采自河南省洛阳市、湖北省京山县和四川省都江堰市的缓步动物门2新种及3新纪录种和亚种：异缓步纲棘影熊虫科的四棘棘影熊虫,新纪录Echiniscus quadrispinosus Richters,1902;真缓步纲小斑熊虫科的都江小斑熊虫,新种Milnesium dujiangensis sp.nov,大生熊虫科的节值大生熊虫戴冠亚种,新纪录Macrobiotus harmsworthi coronatus Barros,1942;高生熊虫科的大指等高熊虫,新纪录Isohypsibius macrodactylus(Maucci,1978)和京山等高熊虫,新种Isohysibius jingshanessis sp.nov.     

四川省缓步动物2新纪录种记述

记述了四川省绵阳缓步动物2个新纪录种。它们是缓步动物门（Tardigrada）、真缓步纲（Eutardigrada）、近爪目（Parachela）、大生熊虫科（Marcobiotidate）,Doryphoribius属的Doryphoribius qinlingensis Li,Su＆Yu和缓步动物门、异缓步纲（Heterotardigrada）、棘影目（Echiniscoidea）、棘影科（Fchiniscidae）、角棘影属（Cornechiniscus）的Cornechiniscus lobatus Ramazzotti。     

青海省缓步动物区系初步调查

记述了青海省发现的14种缓步动物,它们属于2纲、3目、4科、10属.2种(叉状大生熊虫Macrobiotus furciger Murray,1906和马氏等高熊虫Isohypsibius marcellinoi Binda & Pilato,1971)是中国新纪录种,12种(叶状角棘影熊虫Cornechiniscus lobatus Ramazzotti,1943、加拿大棘影熊虫Echiniscus canadensis Murray,1910、文氏棘影熊虫Echiniscus wendti Richters, 1903、小刻面假棘影熊虫Pseudechiniscus facettalis Petersen,1951、缓步米氏熊虫Milnesium tardigradum Doyére,1840、哈氏大生熊虫Macrobiotus hamsworthi Murray,1907、胡氏大生熊虫Macrobiotus hufelandi Schultze,1833、瑞氏大生熊虫Macrobiotus richtersi Murray, 1911、介小生熊虫Minibiotus intermedius Palte,1889、苏格兰双相熊虫Diphascon scoticum Murray,1905、黄色腹矛熊虫Doryphoribius flavus Iharos,1966和杜氏高生熊虫Hypsibius dujardini Doyére,1840)是青海省新纪录种.本文系青海省对该类动物的首次报道.     

陕西省缓步动物二新纪录种记述

记述了陕西省2个缓步动物新纪录种,它们是Doryphoribius citrinusMaucci,1972(真缓步纲,高生熊虫科)和Echiniscus testudoDoyére,1840(异缓步纲,棘影科)。     

云南省丽江苔藓中缓步动物(异缓步纲:棘节目:棘影熊虫科;真缓步纲:近爪目:大生熊虫科,高生熊虫科)

记述了采自云南省丽江县的缓步动物13种,包括：安哥拉棘影熊虫Echiniscus angolensis da Cunha etal,凹口棘影熊虫Echiniscus cavagnaroi Schuster,米吉棘影熊虫Echiniscus migiurtynus Franceschi,华美假棘影熊虫Pseudechiniscus facettalis Petersen,丽江苔小猪熊虫Bryodelphax lijian-gensis sp.nov,隐匿大生熊虫Macrobiotus adelges Dastych,云杉大生熊虫Macrobiotus yunshanensis sp.nov,华丽大生熊虫Macrobiotus richtersiJ.Murr,双甲高生熊虫Hypsibius biscuitiformis Bartos,锐齿高生熊虫Hypsibius runae Bartos。棒形双相熊虫Diphascon clavatum(Bartos)。云南等高熊虫Isohypsibius yunnanensis spnov,隆肿等高熊虫Isohypsibius tuberculatus(Plate)。本文所用标本均保存在中国科学院水生生物研究所。     

中国神农架国家森林公园苔藓中的缓步动物

记述了采自湖北省西部神农架国家森林公园苔藓中的缓步动物12种,包括:日本棘影熊虫Echiniscus japonicus Morikawa,1951;双粒棘影熊虫Echiniscus bigranulatus Richters,1907中国新纪录种;华美假棘影熊虫Pseudechiniscus facettalis Petersen,1951;于猪假棘影熊虫Pseudechiniscus suillus(Ehrenberg,1853);迟缓小斑熊虫Milnesium tardigradum(Doyère,1840);隐匿大生熊虫Macrobiotus adelges Dastych,1977;锦葵大生熊虫Macrobiotus hibiscus Barros,1942中国新纪录种;胡芬大生熊虫Macrobiotus hufelandi Schultze,1833;华丽大生熊虫Macrobiotus richtersi Murray,1911;陆栖大生熊虫Macrobiotus terricola Mihel(c)I(c),1949;水生趾生熊虫Dactylobiotus aquatilis Yang,1999;金猴等高熊虫Isohypsibius jinhouensis sp. Nov..所有的标本均保存于中国科学院水生生物研究所.     

中国缓步动物门两新纪录种

报道了我国缓步动物门2新纪录种,即加拿大棘影熊虫Echiniscus canadensis Murray,1910和日本棘影熊虫Echiniscus japonicus Morikawa,1951.两新纪录种均采自秦岭地区,海拔1500 m.运用扫描电子显微镜对加拿大棘影熊虫背板上的纹饰进行了观察和描述.在光学显微镜下观察到的加拿大棘影熊虫背板上多边形中央的小点实际上是一些深凹陷.     

吉林和湖北缓步动物二新纪录

记述了吉林省和湖北省2个缓步动物新纪录。它们是Macrobiotus harmsworthi Murray,1907;Macrobiotus hufelandi Schultze,1833。2个种同属于缓步动物门(TaNigrada)、真缓步纲(Eutardigrada)、并爪H(Parachela)、大生熊虫科(Macrobiotidae)、大生熊虫属(Macrobiotus)。     

Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban.

The peptide oxytocin (OT) antagonist atosiban, approved for tocolytic use in Europe (under the tradename Tractocile), represents an important new therapeutic advance for the treatment of premature labor. This paper presents some new peptide OT antagonists which offer promise as superior tocolytics. The solid phase synthesis is reported of four pairs of L and D-2-naphthylalanine (L/D-2Nal) position-2 modified analogs of the following four oxytocin (OT) antagonists: des-9-glycinamide [1-(beta-mercapto-beta,beta-pentamethylene propionic acid), 2-O-methyltyrosine, 4-threonine]ornithine-vasotocin (desGly-NH(2),d(CH(2))(5)[Tyr(Me)(2),Thr(4)]OVT) (A); the Tyr-NH(2) (9) analog of (A), d(CH(2))(5)[Tyr(Me)(2),Thr(4),Tyr-NH(2) (9)]OVT (B); the Eda(9) analog of (A), d(CH(2))(5)[Tyr(Me)(2),Thr(4),Eda(9)]OVT (C); and the retro COCH(2)Ph(4-0H)(10) modified analog of (C), d(CH(2))(5)[Tyr(Me)(2),Thr(4),Eda(9)<-- COCH(2)Ph(4-0H)(10)]OVT (D). The eight new analogs of A-D are (1) desGly-NH(2),d(CH(2))(5)[D-2Nal(2),Thr(4)]OVT, (2) desGly-NH(2),d(CH(2))(5)[2-Nal(2),Thr(4)]OVT, (3) d(CH(2))(5)[D-2Nal(2),Thr(4),Tyr-NH(2) (9)]OVT, (4) d(CH(2))(5)[2Nal(2),Thr(4),Tyr-NH(2) (9)]OVT, (5) d(CH(2))(5)[D-2Nal(2),Thr(4),Eda(9)]OVT, (6) d(CH(2))(5)[2Nal(2),Thr(4),Eda(9)]OVT, (7) d(CH(2))(5)[D-2Nal(2),Thr(4),Eda(9)<-- COCH(2)Ph(4-0H)(10)]OVT, (8) d(CH(2))(5)[2Nal(2),Thr(4),Eda(9)<-- COCH(2)Ph(4-OH)(10)]OVT. Peptides 1-8 were evaluated for agonistic and antagonistic activities in in vitro and in vivo rat bioassays, in rat OT receptor (rOTR) binding assays and in human OT receptor (hOTR) and human vasopressin (VP) vasopressor (V(1a)) receptor (hV(1a)R) binding assays. Also reported are the hOTR and hV(1a)R affinity data for atosiban and for B. None of the eight peptides exhibit oxytocic or vasopressor agonism. Peptides 1-8 exhibit weak antidiuretic agonism (activities in the range 0.014-0.21 U/mg). Peptides 1-6 exhibit potent in vitro (no Mg(2+)) OT antagonism (anti-OT pA(2) values range from 7.63 to 8.08). Peptides 7 and 8 are weaker OT antagonists. Peptides 1-6 are all OT antagonists in vivo (estimated in vivo anti-OT pA(2) values in the range 6.94-7.23). Peptides 1-8 exhibit vasopressor antagonism, anti-V(1a) pA(2) values in the range 5.1-7.65. Peptides 1-8 exhibit high affinities for the rOTR (K(i) values = 0.3-7.8 nM). Peptides 1-4 and B exhibit surprisingly very high affinities for the hOTR; their K(i) values are 0.17, 0.29, 0.07, 0.14 and 0.59 nM, respectively. Peptides 1-4 and B exhibit respectively 449, 263, 1091, 546 and 129 times greater affinity for the hOTR than atosiban (K(i) = 76.4 nM). Peptides 1-4 exhibit high affinities for the hV(1a)R (K(i)s = 1.1 nM, 1.3 nM, 0.19 nM and 0.54 nM, all higher than the hV1(a)R affinities exhibited by atosiban (K(i) = 5.1 nM) and by B (K(i) = 5.26 nM). Because of their strikingly higher affinities for the hOTR than atosiban, peptides 1-4 and B exhibit gains in anti hOT/anti hV(1a) receptor selectivity compared with atosiban of 93, 64, 39, 56 and 127, respectively. These OT antagonists are thus promising candidates for development as potential new tocolytic agents.     

不同浓度Ni、Cu处理对骆驼蓬光合作用和叶绿素荧光特性的影响水

以骆驼蓬幼苗为材料,采用盆栽试验研究不同浓度(0、50、100、200、400 mg·kg-1)Ni、Cu处理对骆驼蓬叶片光合作用、叶绿素荧光特性及生长状况的影响.结果表明:随着Ni浓度的增加,骆驼蓬幼苗叶片的光合色素含量、净光合速率(Pn)、气孔导度(Gs)、蒸腾速率(Tr)、PS Ⅱ最大光化学效率(Fv/Fm)、PS Ⅱ电子传递量子产率(φpsⅡ)、光化学猝灭系数(qp)及各项生长指标均呈显著下降趋势,而细胞间隙CO2浓度(Ci)和非光化学猝灭系数(qn)呈显著增加趋势,其中Pn的下降主要是由非气孔限制所致;骆驼蓬幼苗叶片的光合色素含量、Pn、Gs、Tr、Ci、Fv/Fm、φpsⅡ、qp及各项生长指标均在50 mg·kg-1Cu处理时达到峰值,叶绿素a和b、Pn、Gs、Tr、Ci、Fv/Fm及各项生长指标值在100 mg·kg-1Cu处理时仍微高于对照,而后随Cu浓度的增加,光合色素含量、Pn、Gs、Tr、Ci、Fv/Fm、φpsⅡ、qp及各项生长指标均呈下降趋势,qN呈增加趋势,其中Pn的下降主要是由气孔限制所致.     

Characterisation and biological activity of Glu3 amino acid substituted GIP receptor antagonists

Glucose-dependent insulinotropic polypeptide (GIP) is an important gastrointestinal hormone, which regulates insulin release and glucose homeostasis, but is rapidly inactivated by enzymatic N-terminal truncation. Here we report the enzyme resistance and biological activity of several Glu(3)-substituted analogues of GIP namely; (Ala(3))GIP, (Lys(3))GIP, (Phe(3))GIP, (Trp(3))GIP and (Tyr(3))GIP. Only (Lys(3))GIP demonstrated moderately enhanced resistance to DPP-IV (p<0.05 to p<0.01) compared to native GIP. All analogues demonstrated a decreased potency in cAMP production (EC(50) 1.47 to 11.02 nM; p<0.01 to p<0.001) with (Lys(3))GIP and (Phe(3))GIP significantly inhibiting GIP-stimulated cAMP production (p<0.05). In BRIN-BD11 cells, (Lys(3))GIP, (Phe(3))GIP, (Trp(3))GIP and (Tyr(3))GIP did not stimulate insulin secretion with both (Lys(3))GIP and (Phe(3))GIP significantly inhibiting GIP-stimulated insulin secretion (p<0.05). Injection of each GIP analogue together with glucose in ob/ob mice significantly increased the glycaemic excursion compared to control (p<0.05 to p<0.001). This was associated with lack of significant insulin responses. (Ala(3))GIP, (Phe(3))GIP and (Tyr(3))GIP, when administered together with GIP, significantly reduced plasma insulin (p<0.05 to p<0.01) and impaired the glucose-lowering ability (p<0.05 to p<0.01) of the native peptide. The DPP-IV resistance and GIP antagonism observed were similar but less pronounced than (Pro(3))GIP. These data demonstrate that position 3 amino acid substitution of GIP with (Ala(3)), (Phe(3)), (Tyr(3)) or (Pro(3)) provides a new class of functional GIP receptor antagonists.     

Biological screening of rain forest plot trees from Palawan Island (Philippines)

Study plots totaling 0.2 Ha were established in primary forest in the highlands of central Palawan Island, Philippines. Samples of various anatomical parts [typically leaf + twig (If/tw), stem bark (sb), and root (rt)] were collected from all tree species represented within the plots by individuals having a diameter at breast height > or = 10 cm. In all, 211 distinct samples were obtained from 68 tree species, representing 35 families (not including samples from 4 indeterminate species). Methanol extracts of these samples were tested in in vitro antiplasmodial, brine shrimp toxicity, and cytotoxicity assays. The following samples showed an IC50 < or = 10 microg/mL against either chloroquine-sensitive or chloroquine-resistant clones of Plasmodium falciparum: Acronychia laurifolia (sb), Agathis celebica (lf/tw), Aglaia sp. 1 (sb), Aglaia sp. 2 (lf/tw, rt), Bhesa sp. 1 (rt), Cinnamomum griffithii (lf/tw), Croton leiophyllus (rt), Dysoxylum cauliflorum (rt), Garcinia macgregorii (sb), Lithocarpus sp. 1 (rt, sb), Meliosma pinnata ssp. macrophylla (lf/tw, rt), Myristica guatteriifolia (lf/tw), Ochrosia glomerata (rt, sb), Swintonia foxworthyi (lf/tw), Syzygium sp. 1 (rt), Turpinia pomifera (rt), and Xanthophyllum flavescens (sb). Secondly, those samples which displayed > or = 50% immobilization of brine shrimp at 100 microg/mL were: Acronychia laurifolia (lf/tw/fruit, rt, sb), Agathis celebica (lf/tw, sb), Aglaia sp. 1 (lf/tw), Alphonsea sp. 1 (rt), Ardisia iwahigensis (lf/tw), Arthrophyllum ahernianum (lf/tw, rt, sb), Castanopsis cf. evansii (rt), Cinnamomum griffithii (lf/tw, rt), Croton argyratus (lf/tw), C. leiophyllus (lf/tw, rt), Dysoxylum cauliflorum (fruit, lf/tw, rt), Euonymus javanicus (rt), Glochidion sp. 1 (rt), Polyosma sp. 1 (rt), Symplocos polyandra (rt), Timonius gammillii (sb), and Xanthophyllum flavescens (rt). Lastly, samples which exhibited an IC50 < or = 20 microg/mL against one or more of the cancer cell lines employed (LU1, KB, KB-V1, P-388, LNCaP, or ZR-75-1) include: Acronychia laurifolia (lf/tw/fruit, rt, sb), Aglaia sp. 1 (sb), Aglaia sp. 2 (rt), Alphonsea sp. 1 (rt), Ardisia iwahigensis (lf/tw, rt, sb), Astronia cumingiana (sb), Croton argyratus (lf/tw, rt, sb), C. leiophyllus (lf/tw, rt), Dimorphocalyx murina (lf/tw, rt, sb), Lithocarpus caudatifolius (rt, sb), Litsea cf. sibuyanensis (rt), Syzygium cf. attenuatum (rt, sb), S. confertum (sb), Ternstroemia gitingensis (rt), and Ternstroemia sp. 1 (rt, sb).     

攀援孔药花化学成分研究

从攀援孔药花全草95%乙醇提取物中首次分离得到19个化合物,通过波谱数据或与已知物对照,它们分别鉴定为:(2S,3S,4R)-2-[(2R)-2-羟基-二十一酰胺基]-二十一烷-1,3,4-三醇(1)、(2S,3S,4R)-2-二十四酰胺基-十八烷-1,3,4-三醇(2)、胡萝卜甙(3)、β-谷甾醇(4)、(20S,22E,24R)-5α,8α-表二氧-麦角甾-6,22-二烯-3β-醇(5)、6β-羟基-豆甾-4-烯-3-酮(6)、十六烷酸-1-甘油酯(7)、桦木酸(8)、大黄素(9)、二十二烷酸-1-甘油酯(10)、对羟基苯甲醛(11)、十七烷酸-1-甘油酯(12)、金色酰胺醇乙酸酯(13)、十九烷酸-1-甘油酯(14)、棕榈酸(15)(、E)-p-香豆酸(16)、(22E,24S)-24-甲基-5α-胆甾-7,22-二烯-3β,5α,6β-三醇(17)、2-去氧-β-蜕皮激素(18)和auranamide(19)。     

Biosynthetic studies on the alpha-glucosidase inhibitor acarbose: the chemical synthesis of isotopically labeled 2-epi-5-epi-valiolone analogs

2-epi-5-epi-valiolone is a cyclization product of the C(7) sugar phosphate, sedoheptulose 7-phosphate, involved in the biosynthesis of the aminocyclitol moieties of acarbose, validamycin, and pyralomicin. As part of our investigation into the pathway from 2-epi-5-epi-valiolone to the valienamine moiety of acarbose, we prepared 1-epi-5-epi-(6-(2)H(2))valiolol [(6-(2)H(2))-6], 5-epi-(6-(2)H(2))valiolol [(6-(2)H(2))-17], 1-epi-2-epi-5-epi-(6-(2)H(2))valiolol [(6-(2)H(2))-12] and 2-epi-5-epi-(6-(2)H(2))valiolamine [(6-(2)H(2))-11]. Compounds (6-(2)H(2))-6 and (6-(2)H(2))-17 were synthesized from 2,3,4,6-tetra-O-benzyl-D-glucopyranose in 10 and seven steps, respectively, whereas (6-(2)H(2))-12 and (6-(2)H(2))-11 were synthesized from 2,3,4,6-tetra-O-benzyl-D-mannopyranose in eight and 10 steps, respectively.     

Position 4 analogues of [deamino-Cys(1)] arginine vasopressin exhibit striking species differences for human and rat V(2)/V(1b) receptor selectivity.

Arginine vasopressin (AVP) mediates a wide variety of biological actions by acting on three distinct G-protein coupled receptors, termed V(1a) (vascular), V(1b) (pituitary) and V(2) (renal). It also binds to the oxytocin (OT) receptor. As part of a program aimed at the design of selective agonists for the human V(1b) receptor, we recently reported the human V(1b), V(1a), V(2) and OT receptor affinities of the following position 4 substituted analogues of [deamino-Cys(1)] arginine vasopressin (dAVP)-(1) d[Leu(4)]AVP, (2) d[Orn(4)]AVP, (3) d[Lys(4)]AVP, (4) d[Har(4)]AVP, (5) d[Arg(4)]AVP, (6) d[Val(4)]AVP, (7) d[Ala(4)]AVP, (8) d[Abu(4)]AVP, (9) d[Nva(4)]AVP, (10) d[Nle(4)]AVP, (11) d[Ile(4)]AVP, (12) d[Phe(4)]AVP, (13) d[Asn(4)]AVP, (14) d[Thr(4)]AVP: (15) d[Dap(4)]AVP. With the exception of Nos. 7 and 12, all peptides exhibit very high affinities for the human V(1b) receptor. Furthermore, peptides 1-4 exhibit high selectivities for the human V(1b) receptor with respect to the V(1a), V(2) and OT receptors and, with d[Cha(4)]AVP, in functional tests, are the first high affinity selective agonists for the human V(1b) receptor (Cheng LL et al., J. Med. Chem. 47: 2375-2388, 2004). We report here the pharmacological properties of peptides 1-4, 5 (from a resynthesis), 7, 9-13, 15 in rat bioassays (antidiuretic, vasopressor and oxytocic) (in vitro: no Mg(++)) with those previously reported for peptides 5, 6, 8, 14. We also report the rat V(1b), V(1a), V(2) and OT receptor affinities of peptides 1-5 and the rat V(2) receptor affinities for peptides: 7-15.The antidiuretic activities in units/mg of peptides 1-15, are: 1=378; 2=260; 3=35; 4=505; 5=748; 6=1150; 7=841; 8=1020; 9=877; 10=1141; 11=819, 12=110; 13=996; 14=758; 15=1053. Peptides 1-4 exhibit respectively the following rat and human (in brackets) V(2) receptor affinities: 1=3.1 nm (245 nm); 2=3.4 nm (1125 nm); 3=24.6 nm (11,170 nm); 4=0.6 nm (1386 nm). Their rat V(1b) receptor affinities are 1=0.02 nm; 2=0.45 nm; 3=9.8 nm; 4=0.32 nm. Their rat V(1a) receptor affinities are 1=1252 nm; 2=900 nm; 3=1478 nm; 4=32 nm. Their rat oxytocin (OT) receptor affinities are 1=481 nm; 2=997 nm; 3=5042 nm; 4=2996 nm. All four peptides have high affinities and selectivities for the rat V(1b) receptor with respect to the rat V(1a) and OT receptors. However, in contrast to their high selectivity for the human V(1b) receptor with respect to the human V(2) receptor, they are not selective for the V(1b) receptor with respect to the V(2) receptor in the rat. These findings confirm previous observations of profound species differences between the rat and human V(2) receptors. Peptides 1-4 are promising leads to the design of the first high affinity selective agonists for the rat V(1b) receptor.     

Antioxidant constituents of Nymphaea caerulea flowers

As part of an ongoing search for antioxidants from medicinal plants, 20 constituents were isolated from the Nymphaea caerulea flowers, including two 2S,3S,4S-trihydroxypentanoic acid (1), and myricetin 3-O-(3'-O-acetyl)-alpha-L-rhamnoside (2), along with the known myricetin 3-O-alpha-L-rhamnoside (3), myricetin 3-O-beta-D-glucoside (4), quercetin 3-O-(3'-O-acetyl)-alpha-L-rhamnoside (5), quercetin 3-O-alpha-L-rhamnoside (6), quercetin 3-O-beta-D-glucoside (7), kaempferol 3-O-(3'-O-acetyl)-alpha-L-rhamnoside (8), kaempferol 3-O-beta-D-glucoside (9), naringenin (10), (S)-naringenin 5-O-beta-D-glucoside (11), isosalipurposide (12), beta-sitosterol (13), beta-sitosterol palmitate (14), 24-methylenecholesterol palmitate (15), 4alpha-methyl-5alpha-ergosta-7,24(28)-diene-3beta,4beta-diol (16), ethyl gallate (17), gallic acid (18), p-coumaric acid (19), and 4-methoxybenzoic acid (20). The structures were determined by spectroscopic means. Compounds were tested for antioxidant activity and nine compounds 2-7, 11, 12 and 18 were considered active with IC(50) of 1.16, 4.1, 0.75, 1.7, 1.0, 0.34, 11.0, 1.7 and 0.95 microg/ml, respectively, while 1 was marginally active (IC(50)>31.25 microg/ml). The most promising activity was found in the EtOAc fraction (IC(50) 0.2 microg/ml). This can be attributed to the synergistic effect of the compounds present in it.     

Synthesis of bisphosphonate derivatives of ATP by T4 RNA ligase

T4 RNA ligase catalyzes the synthesis of ATP beta,gamma-bisphosphonate analogues, using the following substrates with the relative velocity rates indicated between brackets: methylenebisphosphonate (pCH(2)p) (100), clodronate (pCCl(2)p) (52), and etidronate (pC(OH)(CH(3))p) (4). The presence of pyrophosphatase about doubled the rate of these syntheses. Pamidronate (pC(OH)(CH(2)-CH(2)-NH(2))p), and alendronate (pC(OH)(CH(2)-CH(2)-CH(2)-NH(2))p) were not substrates of the reaction. Clodronate displaced the AMP moiety of the complex E-AMP in a concentration dependent manner. The K(m) values and the rate of synthesis (k(cat)) determined for the bisphosphonates as substrates of the reaction were, respectively: methylenebisphosphonate, 0.26+/-0.05 mM (0.28+/-0.05 s(-1)); clodronate, 0.54+/-0.14 mM (0.29+/-0.05 s(-1)); and etidronate, 4.3+/-0.5 mM (0.028+/-0.013 s(-1)). In the presence of GTP, and ATP or AppCCl(2)p the relative rate of synthesis of adenosine 5',5'-P(1),P(4)-tetraphosphoguanosine (Ap(4)G) was around 100% and 33%, respectively; the methylenebisphosphonate derivative of ATP (AppCH(2)p) was a very poor substrate for the synthesis of Ap(4)G. To our knowledge this report describes, for the first time, the synthesis of ATP beta,gamma-bisphosphonate analogues by an enzyme different to the classically considered aminoacyl-tRNA synthetases.     

Enantiomerically pure quaternary ammonium salts with a chiral alkyl chain N(CH3)(n-C3H7)2(sec-C4H9)I: synthesis and physical studies

A pair of enantiomerically pure quaternary ammonium salts with a chiral side chain, methyl-(R)-(1-methylpropyl)di(n-propyl)ammonium iodide 1 and methyl-(S)-(1-methylpropyl)di(n-propyl)ammonium iodide 2, and the related racemate, methyl-(rac)-(1-methylpropyl)di(n-propyl)ammonium iodide 3, were synthesized through a reductive alkylation procedure, starting from enantiomerically pure and, also, racemic forms of (rac)-(1-methylpropyl)amine. A spectroscopic chiroptical signature in solution was provided by the Raman optical activity spectra of compounds 1 and 2. The crystallographic structures of 1, 2, and 3 were examined by single crystal X-ray diffraction. 1 crystallizes in the tetragonal space group P4(3)2(1)2 (no. 96), a = b = 12.826 (2) A, c = 17.730 (2) A, V = 2916.9 (5) A(3), Z = 8, Flack coefficient 0.04 (2). 2 crystallizes in the tetragonal space group P4(1)2(1)2 (no. 92), a = b = 12.842 (1) A, c = 17.749 (2) A, V = 2927.0 (5) A(3), Z = 8, Flack coefficient 0.05 (2). The crystal structures and space groups for 1 and 2 are enantiomorphs and the crystallographic investigation confirmed the absolute configuration of the stereocenter in both compounds. 3 crystallizes in the monoclinic space group P2(1)/n(no. 14), a = 8.178 (1) A, b = 14.309 (2) A, c = 12.328 (2) A, beta = 96.811 (6) degrees, V = 1432.4 (2) A(3), Z = 4.