Cytotoxicity and Antitumor Activity of Arglabin and its Derivatives.

Background: At present, more than 8000 sesquiterpene lactones have been isolated and described from natural sources, a significant part of which has cytotoxicity and antitumor activity. One of the practically available sesquiterpene lactones is arglabin, which, as a renewable material, is used for the synthesis of new compounds. The article presents data on the study of cytotoxicity and antitumor activity of the arglabin and its derivatives using molecular modeling methods and, in the experiment and .

Reaction Products of β-Aminopropioamidoximes Nitrobenzenesulfochlorination: Linear and Rearranged to Spiropyrazolinium Salts with Antidiabetic Activity.

Nitrobenzenesulfochlorination of β-aminopropioamidoximes leads to a set of products depending on the structure of the initial interacting substances and reaction conditions. Amidoximes, functionalized at the terminal C atom with six-membered -heterocycles (piperidine, morpholine, thiomorpholine and phenylpiperazine), as a result of the spontaneous intramolecular heterocyclization of the intermediate reaction product of an S2 substitution of a hydrogen atom in the oxime group of the amidoxime fragment by a nitrobenzenesulfonyl group, produce spiropyrazolinium or -nitrobenzenesulfonates. An exception is -nitrobenzenesulfochlorination of β-(thiomorpholin-1-yl)propioamidoxime, which is regioselective at room temperature, producing two spiropyrazolinium salts (-nitrobezenesulfonate and chloride), and regiospecific at the boiling point of the solvent, when only chloride is formed.

Syntheses Based on 3,4α-Epoxy-1,5,7α,6β(H)-guai-10(14),11(13)-dien-6,12-olide.

The sesquiterpene γ-lactone estafiatin , the molecule of which has a structure of 3,4α-epoxy-1,5,7α,6β(H)-guai-10(14),11(13)-dien-6,12-olide, is characteristic of plants of the genera L. and L. of the family.

Synthesis and biological evaluation of new derivatives of grossheimin.

Grossheimin 1 is a polyfunctionalized sesquiterpene, featuring, in addition to the exomethylene-γ-lactone group, also an additional exocyclic double bond, a hydroxyl, and a ketone carbonyl. These functional groups have been modified, generally in an orthogonal way, by arylation of the exomethylene, by the introduction of heteroatoms associated to oxygen-, nitrogen- and phosphorous functionalities, and by acylation. A selection of the analogues was investigated for bioactivity, showing that the introduction of a substituent at C-13 is not detrimental, and can modulate potency independently from retention or reduction of the C-11 - C-13 exomethylene double bond and the effect of this maneuver on Michael reactivity.

The preparation and properties of 1,1-difluorocyclopropane derivatives.

Recently, the functionalization of organic molecules with fluorine substituents has grown rapidly due to its applications in such fields as medicine, agriculture or materials sciences. The aim of this article is to review the importance of 1,1-difluorocyclopropane derivatives in synthesis. It will examine the role of the fluorine substituents in both ring-forming and ring-opening reactions, as well as methods for obtaining difluorocyclopropanes as single enantiomers.

Analysis of arglabin and its derivatives using high-performance liquid chromatography.

Introduction: The chemical modification of arglabin, a natural sesquiterpene lactone, has garnered significant attention because it comprises a guaianolide structure that exhibits antitumour and immunomodulating properties. Its primarily derived from Artemisia glabella Kar. et Kir.

Neoadjuvant Therapy with Drug Arglabin for Breast Cancer with Expression of H-Ras Oncoproteins.

Backgrounds: In breast cancer, blocking of Ras signaling and inhibition of H-Ras is quite promising. H-Ras may become a target for farnesyl transferase inhibitors, and in combination with other immunohistochemical factors it will contribute to the progression of a breast tumor.

Purpose: The aim of this study was to evaluate the effectiveness of neoadjuvant therapy for breast cancer with the inclusion of farnesyl transferase inhibitor, arglabin interfering with the expression and concentration of H-Ras oncoproteins.

Experimental study of antiparkinsonian action of the harmine hydrochloride original compound.

Background: The effects of chemical products on the nervous system have been studied by various scientists. In this work, the antiparkinsonian action of a water-soluble form of harmine hydrochloride was studied. The present studies aim to research antiparkinsonian action of the harmine hydrochloride original compound.

Composition of essential oil of the aerial parts of L. growing wild in Northern Kazakhstan.

The aim of the study was to investigate volatile compounds from the aerial parts of L. of the family Violaceae grown wild in Northern Kazakhstan for the first time. is a common and widespread species of the temperate northern hemisphere.

Protein tyrosine phosphatase 1B (PTP1B) inhibitors as potential anti-diabetes agents: patent review (2015-2018).

: Protein tyrosine phosphatase 1B (PTP1B) inhibition has been recommended as a crucial strategy to enhance insulin sensitivity in various cells and this fact is supported by human genetic data. PTP1B inhibitors improve the sensitivity of the insulin receptor and have the ability to cure insulin resistance-related diseases. In the latter years, targeting PTP1B inhibitors is being considered an attractive target to treat T2DM and therefore libraries of PTP1B inhibitors are being suggested as potent antidiabetic drugs.

Inhibition of T Cell Receptor Activation by Semi-Synthetic Sesquiterpene Lactone Derivatives and Molecular Modeling of Their Interaction with Glutathione and Tyrosine Kinase ZAP-70.

A variety of natural compounds have been shown to modulate T cell receptor (TCR) activation, including natural sesquiterpene lactones (SLs). In the present studies, we evaluated the biological activity of 11 novel semi-synthetic SLs to determine their ability to modulate TCR activation. Of these compounds, α -epoxyarglabin, cytisinyl epoxyarglabin, 1 β ,10 α -epoxyargolide, and chloroacetate grosheimin inhibited anti-CD3-induced Ca mobilization and extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation in Jurkat T cells.

Bioavailability and structural study of 20-hydroxyecdysone complexes with cyclodextrins.

20-Hydroxyecdysterone - (2β,3β,5β,22R)-2,3,14,20,22,25-hexahydroxycholest-7-en-6-one was isolated in satisfactory yield using ethanol extraction from the aerial part of Silene wolgensis (Hornem.) Otth; sometimes Silene wolgensis (Willd.) Bess.

The natural sesquiterpene lactones arglabin, grosheimin, agracin, parthenolide, and estafiatin inhibit T cell receptor (TCR) activation.

Inhibition of the T cell receptor (TCR) pathway represents an effective strategy for the treatment of T cell-mediated inflammatory and autoimmune diseases. To identify natural compounds that could inhibit inflammatory T cell responses, we screened 13 sesquiterpene lactones, including achillin, arglabin, argolide, argracin, 3β-hydroxyarhalin, artesin, artemisinin, estafiatin, grosheimin, grossmisin, leucomisine, parthenolide, and taurine, for their ability to modulate activation-induced Ca mobilization in Jurkat T cells. Five of the compounds (arglabin, grosheimin, argracin, parthenolide, and estafiatin) inhibited anti-CD3-induced mobilization of intercellular Ca ([Ca⁺]) in Jurkat cells, with the most potent being parthenolide and argacin (IC = 5.

Chemical Composition of the Essential Oil of the Boreal Relict of Pyrola rotundifolia L. from Northern Kazakhstan.

In Kazakhstan Pyrola rotundifolia L. is the plant-relict in the flora of insular pine forests of the region of low hillocks and declivities in Kazakhstan - a group of insular pine forests of Kokshetau, Bayanaul and Karkaralinsk. In this study, the essential oils from dried aerial parts of P.

(1S*,3R*,5S*,7S*)-4,4,8,8-Tetra-chloro-1-isopropyl-5-methyl-tri-cyclo-[5.1.0.0(3,5)]octa-ne.

The title compound, C12H16Cl4, is a derivative of the natural product 1-isopropyl-4-methyl-cyclo-hexa-1,4-diene, and represents a diastereomer with two trans-fused cyclo-propane rings. Both enanti-omers are present in the non-centrosymmetric polar space group Pna21. The central cyclo-hexane ring is planar within 0.