Eudistomin U is a member of a subclass of naturally occurring indole alkaloids known as β-carbolines. These molecules are reported to have diverse biological activity and high binding affinity to DNA, which make them attractive targets for total synthesis. We describe an efficient, five-step sy...
Eudistomin U is a member of the β-carboline class of heterocyclic amine-containing molecules that are capable of binding to DNA. The structure of eudistomin U is unique since it contains an indole ring at the 1-position of the pyridine ring. While simple β-carbolines are reported to intercalat...
Thirty-two new 3,9-disubstituted eudistomin U derivatives were designed and synthesized based on computer-aided drug discovery (CADD). Sixteen 3,9-disubstituted eudistomin U derivatives (6a–6p) have exhibited potent antibacterial activity. Specially, the most active compound 6p displayed better...
This study was conducted to evaluate the potency of organogermanium sanumgerman (germanium lactate citrate) as a protective agent against γ-irradiation–induced toxicity, which may be extended to affect normal organs in mice bearing solid Ehrlich tumor. Another aim was to evaluate the antitumor...
This chapter describes the development of unsaturated polyester and related resins. The morphology of these cured resins is discussed with respect to their cure chemistry and mechanical properties. The curing systems are considered with respect to the choice of manufacturing process. The need fo...
Synthetic resins are used for various applications including in paint industry to improve the glossiness, adhesiveness, hardness, and dryness of paints. Resins are essentially polymers, which are builds up from simple molecules or monomers and can be prepared mainly by either addition polymeriza...
This chapter discusses epoxy resins, which are formed from an oligomer containing at least two epoxide groups and a curing agent. The chapter explains how the formation of epoxy resins was invented and introduced to the market. A great variety of such resins and monographs is available on the ma...
Two different superplasticizers particularly cyclohexanone formaldehyde sulfanilate (CFS) and cyclohexanone glyoxylic sulfanilate (CGS) were prepared; also, their effect on mechanical and physico-chemical properties of oil well cement was assessed. The chemical structures were affirmed by FTIR t...
SummaryThe aim of the present study was to investigate the effects of dietary supplementation with the pyridoindole antioxidant stobadine on histochemical parameters in kidney of streptozotocin-induced diabetic rats. Diabetic male Wistar rats were fed a standard diet or a diet supplemented with ...
The pyridoindole derivative stobadine [(−)-cis-2,8-dimethyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido(4,3b) indole] has been described as a drug with antihypoxic and antiarrhythmic cardioprotective properties. The antioxidative properties of this compound were studied during Cu++-mediated low-density li...
1.The review summarizes the most important data known so far on chemistry, pharmacodynamics, toxicology and clinics of the investigational agent, pyridoindole stobadine.2.Stobadine was shown to be able to scavenge hydroxyl, peroxyl and alkoxyl radicals, to quench singlet oxygen, to repair oxidiz...
Doxorubicin (DOXO), a widely used chemotherapeutic agent, induces apoptosis in transformed and non-transformed cells. The apoptotic effect of DOXO has been linked to the generation of reactive oxygen species (ROS). Antioxidants may be effective in the prevention of DOX-induced apoptosis. In the ...
Stobadine was recognized early in its development as having antioxidant properties. A number of laboratories found associations between the antioxidant properties of stobadine and its potential beneficial effects. We found that stobadine acted as an antioxidant in a modification of an oxygen rad...
This study investigated the ability of stobadine, an effective cardioprotective drug with antiarrhythmic, antihypoxic and oxygen free radical scavenging properties, to protect cells against cyclophosphamide-induced toxic and cytotoxic damage in vivo and in vitro. Cyclophosphamide-induced toxic d...
Previous work has shown, that stobadine-hydrochloride (−)cis-2,8-dimethyl-2,3,4,4a,5,9b-hexahydro-14-pyrido(4,3b) indole administered in a single dose 2 mg/kg of body weight reduces cardiotoxic effect of isoproterenol (1 mg/kg) as shown by lowered serum enzyme activities of AST, CPK, LDH and ALT...
The aim of this paper is to provide a brief overview of most important results of stobadine kinetic studies in rats, dogs, and human volunteers. In these studies, stobadine dihydrochloride and stobadine dipalmitate was used for intravenous and oral administration, respectively. To evaluate kinet...
Alterations in the intestinal barrier permeability occur in a broad spectrum of abdominally related pathologies, mostly due to disturbed oxidative homeostasis and increased lipid peroxidation. 4-Hydroxynonenal (HNE), a major lipid peroxidation product, is physiologically present in healthy gastr...
Caspase-3 is responsible for the cleavage of several proteins including the nuclear enzyme poly(ADP-ribose) polymerase (PARP). Designed on the cleavage site of PARP, Ac-Asp-Glu-Val-Asp-H has been reported as a highly specific inhibitor. To overcome the susceptibility to proteolysis, the intrinsi...
The contents of oleanolic acid and its 3-0-glucuronide derivatives as well as of 3-0-glucoside derivatives were determined in vacuoles prepared from protoplasts and cell walls obtained from cells of Calendula officinalis leaves. In both cell compartments studied 37% of total cellular oleanolic a...
The radioactive precursor, [3−3H]oleanolic acid-3-O-mono-[14C]glucoside was administrated to isolated cells obtained from the leaves of Calendula officinalis. The radioactivity of the precursor was incorporated into fractions containing free oleanolic acid, individual glucosides, glucuronide F a...
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