• Archives of Pharmacal Research
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• 제25권4호
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• pp.397-415
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• 2002

This paper deals with a crucial mechanism for interaction of basic drugs and cardiac glycosides at the hepatic uptake level. Available literature data is provided and new material is presented to picture the differential transport inhibition of bulky (type2) cationic drugs by a number of cardiac glycosides in rat liver. It is shown that the so called organic anion transporting peptide 2 (oatp2) is the likely interaction site: differential inhibition patterns as observed in oocytes expressing oatp2, could be clearly identified also in isolated rat hepatocytes, isolated perfused rat liver and the rat in vivo. The anticipation of transport interactions at the hepatic clearance level should be based on data on the relative affinities of interacting substrates for the transport systems involved along with knowledge on the pharmacokinetics of these agents as well as the chosen dose regimen in the studied species. This review highlights the importance of multispecific tranporter systems such as OATP, accommodating a broad spectrum of organic compounds of various charge, implying potential transport interactions that can affect body distribution and organ clearance.

• 대한약리학회지
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• 제22권1호
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• pp.1-23
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• 1986

• Toxicological Research
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• 제35권3호
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• pp.233-239
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• 2019

Nerium oleander (N. oleander) is a well-known poisonous shrub that is frequently grown in gardens and public areas and contains numerous toxic compounds. The major toxic components are the cardiac glycosides oleandrin and neriin. The aim of our study was to evaluate the toxic effects of an ethanolic N. oleander leaf extract on haematological, cardiac, inflammatory, and serum biochemical parameters, as well as histopathological changes in the heart. N. oleander extract was orally administered for 14 and 30 consecutive days at doses of 100 and 200 mg of dried extract/kg of body weight in 0.5 mL of saline. The results showed significant increases in mean corpuscular volume, white blood cell counts, platelet counts, interleukins (IL-1 and IL-6), tumour necrosis factor alpha, C reactive protein, alanine aminotransferase, lactate dehydrogenase, creatine kinase and creatine kinase MB, especially at high doses. Marked pathological changes were perceived in the heart tissue. Thus, it can be concluded that exposure to N. oleander leaf extract adversely affects the heart and liver.

• 약학회지
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• 제30권4호
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• pp.198-201
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• 1986

The successful elucidation of the opiate receptor and its natural ligands has generated speculation that other drugs might interact with cellular sites designed to accommodate endogenous mediators. The properties of binding sites for the cardiac glycosides(CG), together wit the potency and specificity of the digitalis drugs suggest that CG mimic an endogenous digitalis-like factor. Recenthy, several laboratories have reported the potency in mammalian tissues and fluids of unidentified materials that share certain specific propeties of the CG. Identification of body's own digitalis might yield a natural co pound whose synthetic analogs may provide safer and more effective drugs than can be achieved by structural edification of the CG of plant origin.

• 대한임상독성학회지
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• 제4권1호
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• pp.58-60
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• 2006

The venom gland of Toad contains large quantities of cardiac glycosides, and toad venom poisoning is similar to digitalis toxicity and carries a high mortality. Sometimes after ingestion of aphrodisiac pills which contain dried toad, a patient develops gastrointestinal symptoms and bradycardia, psychoneurologic symptoms. We have experienced 2 cases of toad venom intoxication, who ingested asian toads. Patients were presented to our ED with nausea, vomiting, and abdominal pain. The patients were peformed monitoring and conservative treatment and were fully recovered. Toad venom intoxication should be considered in patients with clinical manifestation of gastrointestinal irritation, cardiac arrhythmias, hyperkalemia, and detectable serum digoxin level without current medication of digoxin.

• Journal of Ginseng Research
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• 제45권1호
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• pp.22-31
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• 2021

Atherosclerosis (AS) is a leading cause of cardiovascular diseases (CVDs) and it results in a high rate of death worldwide, with an increased prevalence with age despite advances in lifestyle management and drug therapy. Atherosclerosis is a chronic progressive inflammatory process, and it mainly presents with lipid accumulation, foam cell proliferation, inflammatory response, atherosclerotic plaque formation and rupture, thrombosis, and vascular calcification. Therefore, there is a great need for reliable therapeutic drugs or remedies to cure or alleviate atherosclerosis and reduce the societal burden. Ginsenosides are natural steroid glycosides and triterpene saponins obtained mainly from the plant ginseng. Several recent studies have reported that ginsenosides have a variety of pharmacological activities against several diseases including inflammation, cancer and cardiovascular diseases. This review focuses on describing the different pharmacological functions and underlying mechanisms of various active ginsenosides (Rb1,-Rd, -F, -Rg1, -Rg2, and -Rg3, and compound K) for atherosclerosis, which could provide useful insights for developing novel and effective anti-cardiovascular drugs.

• 통합자연과학논문집
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• 제9권1호
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• pp.72-79
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• 2016

Hexane, ethyl acetate and methanol extracts of whole plant of Boerhavia diffusa were screened for phytochemical and biological activities. Qualitative phytochemical screening via colorimetric method and the quantitative estimation of phenolic and flavonoid content were performed. Antioxidant assay using DPPH scavenging method was studied. Antimicrobial screening of plant extracts was done by cup diffusion technique. Cytotoxic activity of B. diffusa was studied by brine shrimp bioassay and anthelminthic activity was evaluated in vitro in Pheretima posthuma. This study revealed B. diffusa as a source of various phyto-constituents such as alkaloids, glycosides, saponins, tannins, carbohydrates, cardiac glycosides, flavonoids and terpenoids. Quantitative estimation of total phenol was found to be maximum in BEE i.e. $29.73{\pm}0.88$, BME $19.8{\pm}2.02$ and in BHE $9.15{\pm}0.304mgGAE/g$. Similarly, the total flavonoid content was found to be $17.44{\pm}0.75$ in BEE, $14.43{\pm}0.23$ in BHE and 3.678 mg QE/g in BME. Ethyl acetate extract showed its antibacterial activity against all tested pathogens except Escherichia coli whereas Staphylococcus aureus and Salmonella Typhi were resistant to methanol and hexane extract. The zone of inhibition (ZOI) of ethyl acetate extract against S. Typhi and B. cereus was found to be 18 mm and 14 mm respectively. The MIC value of BEE in S. Typhi was $3.125{\mu}g/ml$ and in B. cereus was $12.5{\mu}g/ml$. The preliminary screening of anticancer property of B. diffusa i.e. BSLT in methanol was found to be $165.19{\mu}g/ml$. B. diffusa was also found to contain anthelmintic property. The study helped in further exploration of medicinal properties of B. diffusa by phytochemical screening and biological activities paving the path for study and investigation in this plant.

• 대한약리학회지
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• 제8권1호
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• pp.67-75
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• 1972

Many studies on the mechanism of the inotropic action of cardiac glycosides have shown the possible intimate relationship between the mobilization of intracellular calcium and inotropic effect. Evidence obtained from recent studies suggests that cardiac glycosides may increase the intracellular $Ca^{++}$ concentration through the release of this ion from cellular or intracellular membrane. It seemed imperative to study the effect of ouabain on the interaction between mitochondria and $Ca^{++}$, because mitochondria are known to have a rather powerful $Ca^{++}$ pump mechanism which may have an important role on the regulation of intracellular $Ca^{++}$ concentration. The present investigations was made into the effect of ouabain on $Ca^{++}$ untake of mitochondria in the presence of ATP and its dependence on $K^+$ and $Na^+$ in the medium. The results are summarized as follows: 1. The rate of rise in the turbidity of superprecipitation was solely influenced by ionic strength of the medium, not by the species of ion, i.e. $Na^+$ or $K^+$. The higher ionic strength suppressed and the lower enhanced the rate of superprecipitation respectively. 2. No effect of ouabain was found on the rate of superprecipitation. 3. Mitochondria depressed the rate of superpretipitation, and the depressed rate of superprecipitation by mitochondria was reversed by ouabain, and the degree of this reversal was almost identical in $Na^+$ and $K^+$ medium. 4. $Ca^{++}$ uptake of mitochondria was inhibited by ouabain in the presence of ATP and the degree of inhibition showed the dose-response manner in terms of concentration of ouabain. 5. In the absence of ATP, mitochondria took or the $Ca^{++}$ in initial period but released it later. Such uptake and release of $Ca^{++}$ was not influenced by ouabain. 6. It is suggested that intracellular calcium mobilization by ouabain through the action upon the mitochondria was due to inhibition on ATP-dependent $Ca^{++}$ uptake by this agent, not to the action upon so called binding.

• 대한약리학회지
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• 제12권1호
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• pp.31-44
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• 1976

It has been reported that many of the effects of digitalis glycosides could be mediated partly through the central nervous system. In this study the effects of ouabain given directly into the lateral ventricle of the brain on the renal function of the rabbit were investigated. Intraventricular ouabain elicited antidiuresis in doses ranging from 0.1 to $3\;{\mu}g$, exhibiting a rough dose-response relationship, and decreased the renal plasma flow, glomerular filtration rate and urinary excretion of sodium and potassium, concomitant with the decrease of urine flow. These decreases in urine flow, excretory rate of electrolytes significantly correlated with the decrease in renal plasma flow or glomerular filtration rate, suggesting that the antidiuresis might have been induced by the hemodynamic changes. Intravenous ouabain in a dose of $1\;{\mu}g$ did not affect the renal function. Systemic blood pressure as well as cardiac activity was not affected by the intraventricular ouabain. Effects of the intraventricular ouabain on renal function were abolished by the intravenous phentolamine-pretreatment but not affected by intraventricular phentolamine-pretreatment. Neither vasopressin infusion nor hydration did affect the renal effects of intraventricular ouabain. From these observations, it is suggested that the antidiuresis of intraventricular ouabain is induced by the increased sympathetic influence to the kidney.

• 한국미생물·생명공학회지
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• 제42권2호
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• pp.152-161
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• 2014

The in vitro antimicrobial potential of the unexplored Moringa oleifera seed coat (SC) was evaluated against some Gram-positive and Gram-negative bacteria and yeast pathogens. Antimicrobial studies with various solvent extracts indicated ethyl acetate to be the best extractant, which was used for the rest of the antimicrobial studies as it tested neither toxic nor mutagenic. Gram-positive bacteria including a methicillin resistant Staphylococcus aureus (MRSA) strain were more susceptible with a minimum inhibitory concentration (MIC) range of 0.03-0.04 mg/ml. The antimicrobial pharmacodynamics of the extract exhibited both concentration-dependent and time-dependent killing. Most of the test organisms exhibited a short post antibiotic effect (PAE) except Enterococcus faecalis, Staphylococcus aureus, and Klebsiella pneumoniae 1, which exhibited longer PAEs. Amongst the major phytoconstituents established, flavonoids, diterpenes, triterpenes and cardiac glycosides exhibited inhibitory properties against most of the test organisms. The identified active phytochemicals of the M. oleifera seed coat exhibited antimicrobial potential against a wide range of medically important pathogens including the multidrug-resistant bugs. Hence, the M. oleifera seed coat, which is usually regarded as an agri-residue, could be a source of potential candidates for the development of drugs or drug leads of broad spectrum that includes multidrug-resistant bugs, which are one of the greatest concerns of the $21^{st}$ century.