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1.
The alkaloids of Strychnos icaja (Loganiaceae) have been studied. An extract from Zaire leaf material yielded nine alkaloids, comprising novacine, the new base 21,22-α-epoxy-4,14-dihydroxy-3-methoxy-N-methyl-sec.-pseudostrychnine, and seven others of known structure previously obtained from the plant. Cameroun leaf material gave five alkaloids, of which one, 21,22-α-epoxy-3,4-dimethoxy-N-methyl-sec.-pseudostrychnine, is new. Fruits from Gabon afforded eight alkaloids; two of them are new and are formulated as 21,22-α-epoxy-4-methoxy-N-methyl-sec.-pseudostrychnine and the corresponding 14-hydroxy derivative.  相似文献   

2.
Evidence is presented for the probable identity of strychnicine, a Strychnos alkaloid isolated by Boorsma in 1902 but no longer available, with vomicine (4-hydroxy-N-methyl-sec.-pseudostrychnine). A product obtained in 1966 by Hifny Saber et al. and identified by them as strychnicine is different from Boorsma's compound and its nature remains uncertain.  相似文献   

3.
Two homologous series of n-paraffins and sec-alcohols from C20 to C34 or C35 were isolated a wax constituents of a liverwort, Isotachis japonica. In both series, odd-members were predominant compared with even-members: the ratio of the total amount of odd- to total amounts of even-members was 3·9 in the n-paraffin homologues, and 16·5 in the sec-alcohol homologues.  相似文献   

4.
The activity of two scavenging deep-sea fishes occupying the same niche in overlapping depth zones were compared by in situ measurements of swimming speeds, tail-beat frequencies and by arrival time at baits. At 4800 m on the Porcupine Abyssal Plain, the grenadier Coryphaenoides (Nematonurus) armatus was the dominant scavenger, arriving at baits after 30 min, and swimming at relatively slow speeds of 0.17 body lengths (BL) sec-1. At 2500 m in the relatively food rich Porcupine Seabight both C. (N.) armatus and the blue-hake, Antimora rostrata, were attracted to bait, but A. rostrata was always the first to arrive and most of the bait was consumed before the C. (N.) armatus arrived. A. rostrata swam at mean speeds of 0.39 BL sec-1, similar to related shallow water species at equivalent temperatures. Observations on tail-beat frequency from video sequences confirmed the greater activity of A. rostrata. The data indicate that, given sufficient food supply, high pressure and low temperature do not limit activity levels of demersal deep-sea fishes. Low activity of C. (N.) armatus is an adaptation to poor food supply in the abyss, where these fishes dominate, but prevents it competing with the more active A. rostrata in shallower depths.  相似文献   

5.
With our lead compound (E)-3-(4-chlorophenyl)-2-(1H-pyrrole-2-carbonyl)acrylonitrile (1) inducing 50% growth inhibition of 11 cancer cell lines at 27–61 μM, potency enhancements were rapidly established through the synthesis of a series of focused compound libraries. Six highly focused libraries (46 compounds in total) were synthesised. Each library allowed the identification of a new lead compound, viz Library A identified (E)-3-(pentafluorophenyl)-2-(1H-pyrrole-2-carbonyl)acrylonitrile (11) and (E)-3-(1H-indol-3-yl)-2-(1H-pyrrole-2-carbonyl)acrylonitrile (13) as inhibitors with improved cytotoxicity. Synthesis of discrete libraries of amidoacrylamide analogues (Ar–CC(CN)–Ar?Ar–CC(CN)–C(O)NH)–Ar) resulted in a series of analogues significantly more potent that the lead, 1. Three furan three analogues: (E)-3-(5-chlorofuran-2-yl)-2-cyano-N-(4-methoxybenzyl)acrylamide (33), (E)-3-(5-bromofuran-2-yl)-2-cyano-N-(4-methoxybenzyl)acrylamide (34) and (E)-2-cyano-3-(furan-3-yl)-N-(4-methoxybenzyl)acrylamide (37) returned broad spectrum growth inhibition (GI50 values of 5–16 μM). Replacement of the furan moiety with simple aromatics gave an additional three analogues: (E)-2-cyano-N-(4-methoxybenzyl)-3-phenylacrylamide (39), (E)-3-(4-chlorophenyl)-2-cyano-N-(4-methoxybenzyl)acrylamide (41) and (E)-2-cyano-N-(4-methoxyphenyl)-3-(naphthalen-1-yl)acrylamide (45) with GI50 values of 7–24 μM. The final library retained the aromatic substituents but introduced a 3,4-dichlorbenzylamine moiety to afford the 1-naphthyl substituted 52, which was the most potent broad spectrum cytotoxic analogue produced here in with an average GI50 = 8.6 μM. This represents a fivefold potency enhancement relative to 1 and a new cytotoxic scaffold suitable for further development.  相似文献   

6.
A comprehensive phytochemical study of the stem bark of Strychnos icaja was done for the first time and led to the isolation of two new monoindole alkaloids 15-hydroxyvomicine (1) and 12-methoxyicajine (2) along with 13 known alkaloids: the monoindoles N-methyl-sec-iso-pseudostrychnine (3), vomicine (4), icajine (5), 19,20-α-epoxy-12-methoxyicajine (6), 19,20-α-epoxy-12,15-dihydroxy-11-methoxyicajine (7), 19,20-α-epoxy-15-hydroxynovacine (8), 15-hydroxyicajine (9), 12-hydroxystrychnine (10), strychnine (11) and the tertiary bisindoles sungucine (12), isosungucine (13), strychnogucine C (14) and bisnordihydrotoxiferine (15). Apart from 10 and 11, the other alkaloids were isolated for the first time from the stem bark of this plant. The hemisynthetic derivative, Nb-chloromethosungucine (16) and the previously reported synthetic compound 3 were isolated from a natural source for the first time. Fractions and some isolated compounds were tested against the chloroquine-sensitive 3D7 strain of Plasmodium falciparum. The bisindole alkaloids were most active with IC50 ranging from 0.72 to 3.41 μg/ml whilst the monomers 1 and 3 were slightly active (IC50 39.92 and 40.27 μg/ml respectively) and 6 inactive. The structures of the compounds were determined based on the analysis of their spectral data. The full 1H and 13C NMR data of compounds 3, 6 and 7 are also reported in the present work for the first time.  相似文献   

7.
Using a liquid chromatography method that separates the two sulfonium diastereoisomers of adenosylmethionine, we have found that immature soybeans, soybean callus culture, radish leaves, yeast and rat liver contain only the (S)-sulfonium form of S-adenosylmethionine. Our findings contradict the suggestion by Stolowitz and Minch that 10–20% of naturally-occurring adenosylmethionine may have the (R)-configuration at the sulfonium pole. Absence of the (R)-sulfonium isomer of adenosylmethionine in biological materials indicates that the (R)-sulfonium form of adenosylmethionine present in commercial adenosylmethionine samples is an artifact of the isolation procedure. Our method of measuring the isomers of adenosylmethionine enabled us to readily determine the rate of racemization and hydrolysis of adenosylmethionine. Our rate constants for racemization (Kr) and hydrolysis (Kh) were 2.4 × 10?6 sec?1 and 12.3 × 10-?6 sec?1, respectively; values which are noticeably different from those of Wu and co-workers which were obtained with a more complicated method (Kr = 8 × 10?1 sec?1; Kh = 6 × 10?6 sec?1). We believe the absence of the (R)-isomer in vivo is best explained by stabilization of the (S)-isomer as suggested by Wu et al. Although the tissues we have analysed contained the (S)-sulfonium form of adenosylmethionine exclusively, when ethionine-resistant soybean cell lines were given ethionine, they accumulated both sulfonium diastereoisomers of adenosylethionine.  相似文献   

8.
The sec, rac-CH3Co(H2O)L2+ (L=5,7,7,12,14,14-hexamethyl-1,4,8,11-tetraazacyclotetradeca-4,11-diene) was prepared successfully via meso-CH3Co(H2O)L2+ in aqueous solution. The isomerizations from meso-RCo(H2O)L2+ (R=CH3, C2H5 and C3H7) and sec, rac-CH3Co(H2O)L2+ to pri, rac-RCo(H2O)L2+ were both base catalyzed in aqueous solution. The kinetic results showed the reaction to be first order in both organocobalt complex and hydroxide ion with the reactivity order for the alkyl group being C3H7 ∼ C2H5 ? CH3. However, the conversion from the most steric hindered isomer form of sec, rac- was slow. The ratio of the isomerization rate constants between meso-CH3Co(H2O)L2+ and sec, rac-CH3Co(H2O)L2+ to pri, rac-CH3Co(H2O)L2+ is almost a factor of 100. The thermodynamic activation parameters for these isomerization reactions were investigated.  相似文献   

9.
Basic c-type cytochromes homologous with plant and animal mitochondrial cytochrome c have been isolated and purified from Rhodymenia palmata and Porphyra umbilicalis. The N-terminal regions have been analysed using a Beckman 890C automatic sequencer. When compared to animal cytochrome c, the Rhodymenia cytochrome c has an unblocked N-terminal tail of 10 amino acids, whereas Porphyra has an unblocked N-terminal tail of only a single amino acid.  相似文献   

10.
Until the mid-1990s, the only microsporidium known to infect bees of the genus Apis was Nosema apis. A second species, Nosema ceranae, was first identified in 1996 from Asian honey bees; it is postulated that this parasite was transmitted from the Asian honey bee, Apis cerana, to the European honey bee, Apis mellifera. Currently, N. ceranae is found on all continents and has often been associated with honey bee colony collapse and other reports of high bee losses. Samples of Africanized drones collected in 1979, preserved in alcohol, were analyzed by light microscopy to count spores and were subjected to DNA extraction, after which duplex PCR was conducted. All molecular analyses (triplicate) indicated that the drones were infected with both N. ceranae and N. apis. PCR products were sequenced and matched to sequences reported in the GenBank (Acc. Nos. JQ639316.1 and JQ639301.1). The venation pattern of the wings of these males was compared to those of the current population living in the same area and with the pattern of drones collected in 1968 from Ribeirão Preto, SP, Brazil, from a location close to where African swarms first escaped in 1956. The morphometric results indicated that the population collected in 1979 was significantly different from the current living population, confirming its antiquity. Considering that the use of molecular tools for identifying Nosema species is relatively recent, it is possible that previous reports of infections (which used only light microscopy, without ultrastructural analysis) wrongly identified N. ceranae as N. apis. Although we can conclude that N. ceranae has been affecting Africanized honeybees in Brazil for at least 34 years, the impact of this pathogen remains unclear.  相似文献   

11.
The environmental pollutant 4-sec-butylphenol (4-sec-BP) which possesses estrogenic properties was transformed by the aerobic Gram-positive bacteria Mycobacterium neoaurum and Nocardia cyriacigeorgica into three main products (P1–P3) which were isolated and structurally characterized in detail. Two of them were products of a process resembling anaerobic metabolism of alkylphenols based on modifications of the alkyl side chain of 4-sec-BP. The first product (P1) was identified as 4-(2-hydroxy-1-methylpropyl)-phenol. The second product P2 was isolated as a mixture of at least four structures which could be identified as I 4-sec-butylidenecyclohexa-2,5-dienone; II 4-(1-methylenepropyl)-phenol; III 4-(1-methylpropenyl)-phenol; and IV 4-(1-methylallyl)-phenol. In contrast to P1 and P2, the third product (P3) resulted from a modification of the hydroxyl group of 4-sec-BP. This product was only formed by M. neoaurum and was identified as the glucoside conjugate 4-sec-butylphenol-α-d-glucopyranoside. Since in general, fungi synthesize sugar conjugates to detoxify hazardous pollutants, the formation of this conjugate is a peculiarity of M. neoaurum. Thus, altogether, six products were formed from 4-sec-BP and different transformation pathways are introduced. The hydroxylating and glucosylating capacity of the characterized bacteria open up applications in environmental protection.  相似文献   

12.
《Palaeoworld》2023,32(3):555-572
The study examines the taxonomy of the newly excavated Nyctereutes material from Dafnero-3 (Greece) and the unpublished specimens from Varshets (Bulgaria). One cranium and a hemimandible from Dafnero-3 site are ascribed to the species Nyctereutes megamastoides, already known from Dafnero-1 and other Early Pleistocene sites of Greece. Two additional crania and a hemimandible from Dafnero-3, along with the Varshets dental material are attributed to N. tingi. This species was previously reported in the Early Pliocene Megalo Emvolon fauna of northern Greece but the record has been challenged and a review is provided. The new findings of Dafnero-3, and Varshets, extend the presence of N. tingi in southeastern Europe until the beginning of the middle Villafranchian and confirm the geographic expansion of the taxon towards West. Moreover, the co-existence of N. tingi and N. megamastoides in Dafnero-3 is reported for the first time in Europe. A paleoecological analysis based on the lower molar method agrees with the existing hypothesis of a more omnivorous N. megamastoides and a more carnivorous N. tingi ecomorph, which further justifies their local co-existence. Additionally, the quantitative analyses of N. tingi from Dafnero-3, and Varshets reveal a possible succession from N. tingi to N. vulpinus, as already supported by previous studies.  相似文献   

13.
The structures of the solvated iron(II) and iron(III) ions have been studied in solution and solid state by extended X-ray absorption fine structure (EXAFS) in three oxygen donor solvents, water, dimethylsulfoxide (Me2SO), N,N′-dimethylpropyleneurea (DMPU), and one sulfur donor solvent, N,N-dimethylthioformamide (DMTF); these solvents have different coordination and solvation properties. In addition, the structure of hexakis(dimethylsulfoxide)iron(III) perchlorate has been determined crystallographically to support the determination of the corresponding solvate in solution. The hydrated, the dimethylsulfoxide and N,N-dimethylthioformamide solvated iron(II) ions show regular octahedral coordination in both solution and solid state with mean Fe-O, Fe-O, and Fe-S bond distances of 2.10, 2.10, and 2.52 Å, respectively, whereas the N,N′-dimethylpropyleneurea iron(II) solvate is five-coordinated, d(Fe-O) = 2.06 Å. The compounds vary in color from light green (hydrate) to dark orange or red (DMPU). The hydrated iron(III) ion in aqueous solution and the dimethylsulfoxide solvated iron(III) ions in solution and solid state show the expected octahedral coordination, the Fe-O bond distances are 2.00 Å for both, whereas the N,N′-dimethylpropyleneurea iron(III) solvate is found to be five-coordinated with a mean Fe-O bond distance of 1.99 Å. The N,N-dimethylthioformamide solvated iron(III) ion in the solid perchlorate salt is tetrahedrally four-coordinated, the mean Fe-S bond distance is 2.20 Å. Iron(III) is reduced with time to iron(II) in N,N-dimethylthioformamide solution. The compounds vary in color from pale yellow (hydrate) to blackish red (DMPU).  相似文献   

14.
Pseudomonas aeruginosa strains resistant towards all currently available antibiotics are increasingly encountered, raising the need for new anti-pseudomonal drugs. We therefore conducted a medium-throughput screen of a small-molecule collection resulting in the identification of the N-alkylated 3,6-dihalogenocarbazol 1-(sec-butylamino)-3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol (MIC = 18.5 μg mL−1). This compound, compound 1, is bacteriostatic towards a broad spectrum of Gram-positive and Gram-negative pathogens, including P. aeruginosa. Importantly, 1 also eradicates mature biofilms of P. aeruginosa. 1 displays no cytotoxicity against various human cell types, pointing to its potential for further development as a novel antibacterial drug.  相似文献   

15.
16.
Nicotiana benthamiana is a model plant utilised internationally in plant virology because of its apparent hyper-susceptibility to virus infection. Previously, others showed that all laboratory accessions of N. benthamiana have a very narrow genetic basis, probably originating from a single source. It is unknown if responses to virus infection exhibited by the laboratory accession are typical of the species as a whole. To test this, 23 accessions of N. benthamiana were collected from wild populations and challenged with one to four viruses. Additionally, accessions of 21 other Nicotiana species and subspecies from Australia, one from Peru and one from Namibia were tested for susceptibility to the viruses, and for the presence of a mutated RNA-dependent RNA polymerase I allele (Nb-RDR1m) described previously from a laboratory accession of N. benthamiana. All Australian Nicotiana accessions tested were susceptible to virus infections, although there was symptom variability within and between species. The most striking difference was that plants of a laboratory accession of N. benthamiana (RA-4) exhibited hypersensitivity to Yellow tailflower mild mottle tobamovirus infection and died, whereas plants of wild N. benthamiana accessions responded with non-necrotic symptoms. Plants of certain N. occidentalis accessions also exhibited initial hypersensitivity to Yellow tailflower mild mottle virus resembling that of N. benthamiana RA-4 plants, but later recovered. The mutant Nb-RDR1m allele was identified from N. benthamiana RA-4 but not from any of 51 other Nicotiana accessions, including wild accessions of N. benthamiana, demonstrating that the accession of N. benthamiana used widely in laboratories is unusual.  相似文献   

17.
Two new phenolic derivatives, dianthramide A and B, were isolated from Dianthus caryophyllus tissues elicited with mycelial extracts of Phytophthora parasitica. The purified substances were identified on the basis of their spectral data and were characterized as N-salicyl-4-methoxyanthranilic acid (dianthramide A) and N-salicyl-4-hydroxyanthranilic acid methyl ester (dianthramide B). Dianthramides A and B co-occur in carnation tissues with the known phytoalexin dianthalexin.  相似文献   

18.
The reaction of the cytochrome c oxidase (ferrocytochrome c:oxygen oxidoreductase, EC 1.9.3.1) of Paracoccus denitrificans cytoplasmic membranes with the endogenous cytochrome c of the membranes was studied, as well as its interaction with added exogenous cytochrome c from P. denitrificans or bovine heart. The polarographic method was employed, using N,N,N′,N′-tetramethyl-p-phenylenediamine plus ascorbate to reduce the cytochrome c. We found that overall electron transport can proceed maximally while the cytochrome c remains membrane bound; NADH or succinoxidase activities were not inhibited by the addition of substances which bind the P. denitrificans cytochrome c strongly. In contrast to our observations with the spectrophotometric method (Smith, L., Davies, H.C. and Nava, M.E. (1976) Biochemistry 15, 5827–5831), in the polarographic assays the membrane-bound oxidase reacts with about equal rapidity with exogenous bovine and P. denitrificans cytochromes c. The reaction of the oxidase with the endogenous cytochrome c proceeds at high rates and preferentially to that with exogenous cytochrome c; the reaction with the latter, but not the former is inhibited by positively charged poly(l-lysine). The cytochrome c and the oxidase appear to be very closely associated on the membrane.  相似文献   

19.
Screening for extra-genital Chlamydia trachomatis and Neisseria gonorrhoeae infections is a crucial component for sexually transmitted diseases management, even if at present days no commercial methods have been approved for use on pharyngeal and rectal specimens by the US FDA or have received the conformity CE marking. Here we report the analytical sensitivities of the Versant CT/GC 1.0 assay (Siemens Healthcare Diagnostics, Tarrytown, NY, USA) on rectal and pharyngeal swabs, and an evaluation about the suitability for this assay with two widely used swab collection devices (E-Swab and eNAT, Copan, Brescia, Italy). The limits of detection for rectal and pharyngeal specimens with the Versant assay were 10 copies/ml and 1.0 copies/ml, for C. trachomatis and N. gonorrhoeae, respectively. False positive results due to the presence of non-gonococcal Neisseria species were excluded when clinical rectal and pharyngeal samples containing organisms identified as N. meningitidis, N. sicca, N. flavescens and N. subflava were tested. Due to its sensitivity and specificity, the Versant assay represents a good choice for the diagnosis of chlamydial and/or gonococcal infections not only in genito-urinary samples, but also on rectal and pharyngeal swabs.  相似文献   

20.
The microsporidium Nosema ceranae is an emergent pathogen of European honeybees Apis mellifera. Using a PCR-RFLP diagnosis, 29 samples of infected honeybees obtained in 2007-2008 (N = 26), 2004 (N = 2) and before 1990 (N = 1) were analyzed for the presence of Nosema apis and N. ceranae. Only N. ceranae was found in all samples, indicating that this species dispersed to Uruguay (and likely the region) at some time before 1990. The presence of N. ceranae in Uruguay is not associated with an increase of Nosemosis, and its role in colony loss seems to be irrelevant.  相似文献   

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