关于几种避孕植物药的药理初筛及成份预试

本文对云南滇西地区民间用于避孕和绝育秘方中的槌果藤,野花椒寄生、花椒寄生、螃蟹树寄生、鸡矢藤及野花椒的醇提取物进行了小鼠最大耐受量测定及小鼠抗生育实验,结果表明,花椒寄生、螃蟹树寄生的醇提取物具有明显抗生育活性,槌果藤也具有一定的抗生育作用。此外,还对槌果藤、野花椒寄生进行了化学成份预试。     

Release of arachidonate from diglyceride in human platelets requires the sequential action of a diglyceride lipase and a monoglyceride lipase

Release of arachidonate from 2-arachidonyl diglyceride by human platelet microsomes was investigated. Diglycerides labeled with ¹⁴C-stearate at sn-1 and with ³H-arachidonate at sn-2 were used as a substrate for microsomal diglyceride lipase. Diglyceride was deacylated first at sn-1 as evidenced by the accumulation of 2-arachidonyl monoglyceride but not of 1-stearoyl monoglyceride. Subsequent release of arachidonate from monoglyceride required the action of a monoglyceride lipase. Studies on substrate specificity indicated that diglyceride lipase utilized 2-arachidonyl diglyceride as the best substrate.     

Chloroplast DNA variation and phylogeographic patterns in the Chinese endemic marsh herb Sagittaria potamogetifolia

We examined chloroplast DNA (cpDNA) atpB–rbcL intergenic spacer sequences variation within Sagittaria potamogetifolia, an endangered and endemic marsh herb in China. Sequence data were obtained from 54 individuals in six extant populations of the species. Sequences appeared to evolve neutral (Tajima's criterion D = −1.59826, 0.1 > P > 0.05 and Fu and Li's tests D* = −1.44484, P > 0.1; F* = −1.83446, P > 0.1). Eleven haplotypes were identified in S. potamogetifolia. A relatively high level of haplotype diversity (h = 0.0.699) and low level of nucleotide diversity (pi = 0.0035 ± 0.0020) were detected in S. potamogetifolia. Pairwise comparisons of F_st and Nm deduced from cpDNA variation suggested no significant genetic differentiation between populations of S. potamogetifolia excepted for the WY-1 population. Low genetic differentiation among populations and also among regions was consistently indicated by both hierarchical analyses of molecular variance (AMOVA) and the structure of a neighbor-joining tree. Lack of population differentiation between populations or between regions in cpDNA sequences may be due to effects of lower substitution rates or lineage sorting. In the minimum spanning network, all tip haplotypes except for the haplotype J were unique to a particular population, while the interior nodes except for the haplotype E were widespread (haplotype A). From nested clade analysis (NCA), the evolutionary events such as restricted gene flow with isolation by distance and allopatric fragmentation were inferred to responsible for the current distribution of S. potamogetifolia populations, as well as their genetic diversity.     

New bioactive dihydrofuranocoumarins from the roots of the Tunisian Ferula lutea (Poir.) Maire

A phytochemical investigation of the roots of Ferula lutea (Poir.) Maire led to the isolation of new dihydrofuranocoumarins as two inseparable isomers, (?)-5-hydroxyprantschimgin 1 and (?)-5-hydroxydeltoin 2, together with eight known compounds, (?)-prantschimgin 3, (?)-deltoin 4, psoralen 5, xanthotoxin 6, umbelliferone 7, caffeic acid 8, β-sitosterol 9 and stigmasterol 10. Their structures were elucidated on the basis of extensive spectroscopic methods, including 1D and 2D NMR experiments and mass spectroscopy analysis, as well as by comparison with literature data. The anti-acetylcholinesterase and cytotoxic effects of the isolates and antioxidant activities of the mixture (1+2) were also evaluated in this work. Results showed that the mixture (1+2) has the most cytotoxic activity with IC₅₀ values 0.29 ± 0.05 and 1.61 ± 0.57 μM against the cell lines HT-29 and HCT 116, respectively. The greatest acetylcholinesterase inhibitory activity (IC₅₀ = 0.76 ± 0.03) was exhibited by the xanthotoxin 6. In addition, the mixture (1+2) was investigated for its antioxidant activity and showed IC₅₀ values 18.56, 13.06, 7.59, and 4.81 μM towards DPPH free radical scavenging, ABTS radical monocation, singlet oxygen and hydrogen peroxide, respectively.     

In vitro testing of the biological activity ofRubia cordifolia leaves on primateStrongyloides species

ChimpanzeesPan troglodytes in Kibale National Park, Uganda occasionally swallow entire leaves ofRubia cordifolia (Rubiaceae) without chewing them. The leaves are subsequently egested with minimal damage and no sign of any significant digestion. Similar behavior reported elsewhere has been proposed to have medicinal effects. Here we test the hypothesis that chemical components in swallowed leaves have negative effects on intestinal nematodes. We used anin vitro assay to detect the effects of methanol extracts ofR. cordifolia leaves on nematodes,Strongyloides spp., cultured from feces. Control extracts were distilled water, methanol solution, and methanol extracts of food items that were chewed, rather than swallowed, by chimpanzees. Effects of experimental or control solutions were assayed by nematode motility. There was no difference in nematode motility among control and experimental extracts. This study therefore did not support the hypothesis of pharmacological self-medication via leaf swallowing.     

Chemical activators: A novel and sustainable management approach for Meloidogyne incognita (Kofoid and White) Chitwood in Chamomilla recutita L

Use of chemical activator for the management of root-knot disease in medicinal and aromatic plants can become an attractive alternative to traditionally used nematicides. Large numbers of chemical molecules are present in the plants and are involved in the induction of different types of proteins. The purpose of our research study is to explore the possibilities of resistance factors that are inherent in the plant by treating them with few chemical activators to activate against root-knot nematode infection. Efforts were made to achieve a satisfactory suppression of root-knot nematode, Meloidogyne incognita, a serious menace to successful cultivation of chamomile, Matricaria recutita L. Rauch (syn. Matricaria chamomilla L. Fain. Asteraceae) causing root-knot disease through use of different chemical activators. Here we examined selected groups of resistance activator viz. Isonicotinamide, 2-chloronicotinic acid, 5-nitrosalicylic acid, 4-chlorosalicylic acid, DL-2 aminobutyric acid, 2-aminobutyric acid, O-acetylsalicylic acid, 4-amino salicylic acid, salicylic acid and these were used as soil drench using 3 week old seedlings transplanted to root-knot nematode infested pots. Maximum reduction in root-knot severity and nematode population occurred with 4-chlorosalicylic acid, O-acetyl salicylic acid, 2-chloronicotinic acid and gave significant flower yield advantages. Present experiment suggests a strong possibility of these activators in integrated management for protection against plant parasitic nematodes.     

A new target for Alzheimer’s disease: A small molecule SERCA activator is neuroprotective in vitro and improves memory and cognition in APP/PS1 mice

Amongst the cellular cacophony of altered signals in Alzheimer’s disease (AD), disrupted Ca²⁺ homeostasis and consequential endoplasmic reticulum (ER) stress signals have been recognized as key determinants of neuron fate. This altered Ca²⁺ state is accompanied by a failing sarco/endoplasmic reticulum Ca²⁺-ATPase (SERCA) pump, which has been recognized as a causal feature of the underlying disease state. Repair of the Ca²⁺ dyshomeostasis represents a putative drug target via alleviation of ER stress and rescue of injured neurons, effectively modifying the AD state. Herein, we report a small molecule SERCA activator that rescues brain cells and raises ER Ca²⁺ in vitro, and shows efficacy in the APP/PS1 double transgenic mouse model of Alzheimer’s disease. These results support SERCA activation as a therapeutic target for AD.     

A gold nanoparticle-mediated enzyme bioreactor for inhibitor screening by capillary electrophoresis

A facile protocol to prepare highly effective and durable in-line enzyme bioreactors inside capillary electrophoresis (CE) columns was developed. To demonstrate the methodology, l-glutamic dehydrogenase (GLDH) was selected as the model enzyme. GLDH was first immobilized onto 38-nm-diameter gold nanoparticles (GNPs), and the functionalized GNPs were then assembled on the inner wall at the inlet end of the CE capillary treated with polyethyleneimine (PEI), producing an in-line GLDH bioreactor. Compared with a GLDH bioreactor prepared by immobilizing GLDH directly on PEI-treated capillary, the GNP-mediated bioreactor showed a higher enzymatic activity and a much better stability. The in-capillary enzyme bioreactor was proven to be very useful for screening of GLDH inhibitors deploying the GLDH-catalyzed α-ketoglutaric acid reaction. The screening assay was preliminarily validated by using a known GLDH inhibitor, namely perphenazine. A Z′ factor value of 0.95 (n = 10) was obtained, indicating that the screening results were highly reliable. Screening of GLDH inhibitors present in medicinal plant extracts by the proposed method was demonstrated. The inhibition percentages were found to be 53% for Radix scutellariae, 45% for Radix codonopsis, 37% for Radix paeoniae alba, and 0% for the other 22 extracts tested at a concentration of 0.6 mg extract/ml.     

Phenological growth stages of North American ginseng (Panax quinquefolius)

The BBCH (Biologische Bundesanstalt, Bundessortenamt, Chemische Industrie) scale is used to describe the phonological growth stages of North American ginseng (Panax quinquefolius). Eight principal growth stages for germination and bud development, leaf development (crop canopy), root and perennating bud formation, peduncle elongation and inflorescence development, flowering and fruit set, development of fruit, ripening of fruit and senescence, and 42 secondary growth stages are described. A practical use of the scale is proposed with reference to the timing of application of agrochemicals for disease control.     

中药渣蚓粪对玉米生长及土壤肥力特性的影响

采用盆栽试验,研究了中药渣蚓粪对玉米生长及土壤肥力的影响.结果表明: 随着蚓粪施用量的增加,玉米的株高、茎粗、叶面积、叶绿素含量均显著增加;生长60 d收获时,多数蚓粪处理的土壤容重显著降低;蚓粪处理的土壤pH显著高于对照和相应的化肥处理.蚓粪处理的土壤全氮、有机质含量也明显高于化肥处理,且随蚓粪施用量的增加,效果越趋显著.中药渣蚓粪可作为一种高效有机肥,其合理施用有助于改善土壤物理结构,缓解土壤的酸化进程,提高土壤有机质和氮素含量,有效促进作物生长.