The antiparasitic properties of the Saussurea salsa (Pall.) Spreng. extract and its cynaropicrin fraction have been studied on a model of opisthorchosis in golden hamsters. The tested substances produced a dose-dependent therapeutic effect comparable with that of the reference antihelminthic drug biltricide (praziquantel).
molecular structure of which was confirmed by an XSA, were produced by reacting α-santonin and chlorine in aqueous acetonitrile. It was found that 2-chloro-α-santonin is highly effective against trichomonas.One of the most efficient synthetic pathways to chloro-derivatives of terpenoids is the reaction of terpene enones with gaseous chlorine [1][2][3]. Japanese researchers observed that the chemo-and stereoselectivity of the reaction of chlorine with α-santonin (1) depended on the nature of the solvent [1].In order to expand the list of available potentially biologically active chloro-derivatives of lactone 1, we carried out for the first time the chlorination of 1 in aqueous acetonitrile. Two reaction products, chloroepoxide 2 and chloride 3, were isolated in yields of 20 and 60%, respectively.The structures of chlorination products 2 and 3 were confirmed by UV, IR, and PMR spectra (see Experimental). The molecular structure of 3 was established by an x-ray structure analysis (XSA). It has the structure 2-chloro-3-oxo-7α,6,11β(H)-eudesm-1,4-dien-12,6-olide (Fig. 1).Six-membered rings A and B are pseudo-trans-fused. Ring A is planar within 0.02 Å. Ring B has the 7α,10β-chair conformation. Ring B is trans-fused to the lactone (C). Ring C has the 7α-envelope conformation. The conformation of 3 is similar to that of the previously studied 2-bromo-α-santonin [4]. Differences in the corresponding torsion angles are less than 2.8°. Table 1 gives the atomic coordinates of 3.The preparation in two steps of 3 from 1 by chlorination in CHCl 3 followed by dehydrochlorination in the presence of N,N-dimethylaniline has been described [1]. Four steps were required to prepare 2 [1].The reason that 3 forms upon chlorination in aqueous CH 3 CN is that the solvent itself is weakly basic. Scheme 1 shows the probable pathway for formation of 2. The appearance of the epoxy group in the 4,5-position can be explained by the presence of water in the reaction mixture. In order to check the correctness of this hypothesis, we carried out 10 model experiments using weighed portions (25 mg) of 1 for each experiment and CH 3 CN:H 2 O solvent mixtures with water content from 0 to 50%. Then, chlorination was carried out under identical conditions until starting 1 was fully converted. The solvent was distilled off, The solid was extracted with ethylacetate. The resulting extracts were left in vials until the solvent was completely evaporated. The solids were analyzed by HPLC. Table 2 gives the analytical results.
Neurogenesis is one of the most important phenomenona affecting human life. This process consists of proliferation, migration and differentiation of neuroblasts and synaptic integrations of newborn neurons. Proliferation of new cells continues into old age, also in humans, although the most extensive process of cell formation occurs during the prenatal period. It is possible to distinguish two regions in the brain responsible for neurogenesis: the dentate gyrus (DG) of the hippocampus and the sub-ventricular zone (SVZ). Hippocampal neurogenesis is very sensitive to various physiological and pathological stimuli. The functional integration of the newly-born dentate granule cells into hippocampal circuitry, and their ability to mediate long-term potentiation in DG, has led to the hypothesis that neurogenesis in the adult brain may play a key role in learning and memory function, as well as cognitive dysfunction in some diseases. Brain disorders, such as neurodegenerative diseases or traumatic brain injuries, significantly affect migration, proliferation and differentiation of neural cells. In searching for the best neurological drugs protecting neuronal cells, stimulating neurogenesis, while also developing no side-effects, endocannabinoids proved to be a strong group of substances having many beneficial properties. Therefore, the latest data is reviewed of the various experimental studies concerning the analysis of the most commonly studied cannabinoids and their impact on neurogenesis.
The ways of searching of herbal antiparasitic means for the alternative treatment of the prevailing diseases – lambliasis and opisthorchosis – have been examined.
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