• Biomolecules & Therapeutics
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• 제21권3호
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• pp.181-189
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• 2013

Motilitone$^{(R)}$ (DA-9701) is a new herbal drug that was launched for the treatment of functional dyspepsia in December 2011 in Korea. The heterogeneous symptom pattern and multiple causes of functional dyspepsia have resulted in multiple drug target strategies for its treatment. DA-9701, a compound consisting of a combination of Corydalis Tuber and Pharbitidis Semen, has being developed for treatment of functional dyspepsia. It has multiple mechanisms of action such as fundus relaxation, visceral analgesia, and prokinetic effects. Furthermore, it was found to significantly enhance meal-induced gastric accommodation and increase gastric compliance in dogs. DA-9701 also showed an analgesic effect in rats with colorectal distension induced visceral hypersensitivity and an antinociceptive effect in beagle dogs with gastric distension-induced nociception. The pharmacological effects of DA-9701 also include conventional effects, such as enhanced gastric emptying and gastrointestinal transit. The safety profile of DA-9701 is also preferable to that of other treatments.

• 약학회지
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• 제39권5호
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• pp.471-479
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• 1995

The recombinant human epidermal growth factor(DWP 401) was investigated on the pharrnacological actions. DWP 401 had no effects on the hexobarbital-induced sleeping time, locomotor activity, rotarod test, body temperature, analgesic action and anticonvulsant action in mice. It also had no influences on the isolated tracheal muscle and ileum of guinea-pig, isolated uterus and fundus strip of rats. Slight hypotensive action with effect on respiration was revealed at a dose of 8 g/kg i.v. of DWP 401 in rabbits. DWP 401 exhibited a weak inhibitory action of glucose tolerance in normal rats, significantly lowered the blood glucose contents in adrenalectomized rats at .a concentration of 160 g,/kg, and produced a significant inhibitory effect on leucocyte migration in CMC-pouch of rats at a concentration of 32 g/rat. Furthermore, DWP 401 showed a significant decrease on gastric juice volume and acidity. However. DWP 401 had no intestinal propulsion rate and influence on urine excretion.

• Biomolecules & Therapeutics
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• 제11권1호
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• pp.41-50
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• 2003

General pharmacological properties of DA-8159, a new pyrazolopyrimidinone derivative were examined in laboratory animals to investigate its safety profile. The oral administration of DA-8159 (1, 5 or 30 mg/kg) in mice and rats had no effect on general behaviors and central nervous system of the animals in test systems, such as hexobarbital-induced sleeping time, motor coordination, normal body temperature, writhing syndromes induced by 0.75% acetic acid solution, chemo-shock produced by pentetrazole solution and rotar rod test. Anesthetized cats treated intravenously with DA-8159 (0.1, 0.3, 1, 3 or 10 mg/kg) showed transient and mild decrease in blood pressure. However, heart rate, respiration rate and tidal volume were not changed by intravenous DA-8159. In the isolated organs including ileum, heart (sinus rate of atria and contractility of papillary muscle), trachea of guinea pigs and phrenic nerve of rats, DA-8159 ($10^{-8}$ ∼$10^{-5}$ mg/L) did not elicit any effect or inhibitory action on the chemically or electrically stimulated contraction. DA-8159 did not influence gastric secretion, pH and total acid output in rats and intestinal propulsion in mice. The administration of DA-8159 in rats had no effect on the platelet aggregation induced by ADP in rabbit plasma, urinary volume and electrolyte ion ($Na^{+}$, $K^{+}$, $Cl^{-}$) excretion in rats. Prothrombin time (PT) of the rats showed a mild but significant increase after administration of DA-8159. Activated partial thromboplastin time (APTT), however, was not affected by DA-8159. These results indicate that DA-8159 does not exert any of serious pharmacological effects.

• 동의생리병리학회지
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• 제26권3호
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• pp.306-313
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• 2012

Herbal medicines are medicinal products containing a single or a mixture of two or more different herbal substances or herbal preparations as active principles. Recently, much attention has been paid to developing various kinds of fermented herbal extracts, a new type of traditional herbal medicine in the field of Korean traditional medicine. The fermentation of medicinal herbs is intended to exert a favorable influence on bioestability, bioavaliablilty and pharmacological activity of herbal extract in the gastrointestinal tract as well as intensifying the nutritional and pharmacological aspects of the medicinal herbs. The purpose of this study was to investigate biological activities of fermented Rehmanniae Radix by lactic acid bacteria at $30^{\circ}C$ for 3 days in comparison with those for Rehmanniae Radix The fermented Rehmanniae Radix exhibited different chemical profile to Rehmanniae Radix generated with HPLC, indicating production of new ingredients during fermentation. Rehmanniae Radix served as good nutritional sources for the growth of lactic acid bacteria showing increased number of bacteria during fermentation. Toxic effect of the fermented Rehmanniae Radix to cells were not seen judged by the MTT assay. The fermented Rehmanniae Radix exhibited better antioxidant effect than non-fermented Rehmanniae Radix analyzed by a SOD-likely assay. Both hypoglycemic and hypotensive effects of the fermented Rehmanniae Radix were also detected and better than those for Rehmanniae Radix in showing dose-dependent inhibitory effects on alpha-glucosidase and ACE, respectively. In conclusion, fermented Rehmanniae Radix appears to have more biological activities than non-feremented Rehmanniae Radix showing not only antioxidant effect but also cardiovascular protection.

• Journal of Ginseng Research
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• 제38권1호
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• pp.66-72
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• 2014

Panax ginseng is one of the most important medicinal plants in Asia. Triterpene saponins, known as ginsenosides, are the major pharmacological compounds in P. ginseng. The present study was conducted to evaluate the changes in ginsenoside composition according to the foliation stage of P. ginseng cultured in a hydroponic system. Among the three tested growth stages (closed, intermediate, and opened), the highest amount of total ginsenoside in the main and fine roots was in the intermediate stage. In the leaves, the highest amount of total ginsenoside was in the opened stage. The total ginsenoside content of the ginseng leaf was markedly increased in the transition from the closed to intermediate stage, and increased more slowly from the intermediate to opened leaf stage, suggesting active biosynthesis of ginsenosides in the leaf. Conversely, the total ginsenoside content of the main and fine roots decreased from the intermediate to opened leaf stage. This suggests movement of ginsenosides during foliation from the root to the leaf, or vice versa. The difference in the composition of ginsenosides between the leaf and root in each stage of foliation suggests that the ginsenoside profile is affected by foliation stage, and this profile differs in each organ of the plant. These results suggest that protopanaxadiol- and protopanaxatriol(PPT)-type ginsenosides are produced according to growth stage to meet different needs in the growth and defense of ginseng. The higher content of PPT-type ginsenosides in leaves could be related to the positive correlation between light and PPT-type ginsenosides.

• Biomolecules & Therapeutics
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• 제31권6호
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• pp.619-628
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• 2023

In the modern era, chronic kidney failure due to diabetes has spread across the globe. Prunetin (PRU), a component of herbal medicines, has a broad variety of pharmacological activities; these may help to slow the onset of diabetic kidney disease. The anti-nephropathic effects of PRU have not yet been reported. The present study explored the potential nephroprotective actions of PRU in diabetic rats. For 28 days, nephropathic rats were given oral doses of PRU (20, 40, and 80 mg/kg). Body weight, blood urea, creatinine, total protein, lipid profile, liver marker enzymes, carbohydrate metabolic enzymes, C-reactive protein, antioxidants, lipid peroxidative indicators, and the expression of insulin receptor substrate 1 (IRS-1) and glucose transporter 2 (GLUT-2) mRNA genes were all examined. Histological examinations of the kidneys, liver, and pancreas were also performed. The oral treatment of PRU drastically lowered the blood glucose, HbA1c, blood urea, creatinine, serum glutamic-oxaloacetic transaminase, serum glutamic pyruvic transaminase, alkaline phosphatase, lipid profile, and hexokinase. Meanwhile, the levels of fructose 1,6-bisphosphatase, glucose-6-phosphatase, and phosphoenol pyruvate carboxykinase were all elevated, but glucose-6-phosphate dehydrogenase dropped significantly. Inflammatory marker antioxidants and lipid peroxidative markers were also less persistent due to this administration. PRU upregulated the IRS-1 and GLUT-2 gene expression in the nephropathic group. The possible renoprotective properties of PRU were validated by histopathology of the liver, kidney, and pancreatic tissues. It is therefore proposed that PRU (80 mg/kg) has considerable renoprotective benefits in diabetic nephropathy in rats.

• Archives of Pharmacal Research
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• 제23권1호
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• pp.79-86
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• 2000

Heterokaryotic nuclear hybrids overcoming the natural barriers of incompatibility have been studied in basidiomycetes. To produce these nuclear hybrids between incompatible mushrooms, which have several potent pharmacological effects, nuclear transfer was performed between Lentinula edodes and Coriolus versicolor. Nuclei from serine auxotrophs of Lentinula edodes, $LE207(Ser^{-})$ were transferred into the protoplasts of arginine auxotrophs of Coriolus versicolor, $CV17(Ser^{-})$using 30% polyethylene glycol 4000 in 10 mM $Cacl_{2}$-glycine solution (pH 8.0). Nulcear transfer progenies were selected by nutritional complementation on minimal media supplemented with 0.6 M sucrose. The progenies were classified based on colony morphology to L. edodes-like, C, versicolor-like and non-parental type. Most of the progenies grew slower than either parent. The number of nuclei per cell was similar but the DNA content varied between progenies. The isozyme patterns of nuclear hybrids resembled either of the parent porfiles or showed a mixed profile.

• Journal of Microbiology and Biotechnology
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• 제26권1호
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• pp.28-37
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• 2016

Numerous plants have been documented to contain phenolic compounds. Thymol is one among these phenolic compounds that possess a repertoire of pharmacological activities, including anti-inflammatory, anticancer, antioxidant, antibacterial, and antimicrobial effects. Despite of the plethora of affects elicited by thymol, its activity profile on gastric cancer cells is not explored. In this study, we discovered that thymol exerts anticancer effects by suppressing cell growth, inducing apoptosis, producing intracellular reactive oxygen species, depolarizing mitochondrial membrane potential, and activating the proapoptotic mitochondrial proteins Bax, cysteine aspartases (caspases), and poly ADP ribose polymerase in human gastric AGS cells. The outcomes of this study displayed that thymol, via an intrinsic mitochondrial pathway, was responsible for inducing apoptosis in gastric AGS cells. Hence, thymol might serve as a tentative agent in the future to treat cancer.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.53-53
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• 1993

In considering the mechanism of action of the calcium antagonists, it is important to realize that there are three distinct receptor types and that the new classification divides these three drugs as members of the dihydropyridine, phenylalkylamines and benzothiazipines, respectively. The World Health Organization as well as the International Union of Pharmacology and Cardiology have adopted this classification. Unlike every other class of drugs, such as the alpha and beta adrenergic blocking agents, diuretics, etc., the calcium antagonists need to be thought of as three distinct drug classes. The reason they share some, but not all of the pharmacological profile is that they all act at specific receptor domains present in one large protein of 165 daltons present in all excitable tissue. This protein along with several other subunits make up what is known as the voltage-dependent calcium channel (the so-called "L"type, L-VDCC). The mechanism of action of the three drugs involve first a specfic binding and then an inhibition of the movement of calcium into the cell Some of these drugs, such as diltiazem, may have other interesting intracellular effects perhaps associated with protection of the mitochondria during ischemic insults. The nature of the receptor is being explored by molecular genetic techniques, and we have recently cloned two of the major subunits; some of the data will be presented.

• Journal of Ginseng Research
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• 제38권3호
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• pp.161-166
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• 2014

Ginseng is widely used for its promising healing and restorative properties as well as for its possible tonic effect in traditional medicine. Nowadays, many studies focus on purified individual ginsenoside, an important constituent in ginseng, and study its specific mechanism of action instead of whole-plant extracts on cardiovascular diseases (CVDs). Of the various ginsenosides, purified ginsenosides such as Rb1, Rg1, Rg3, Rh1, Re, and Rd are the most frequently studied. Although there are many reports on the molecular mechanisms and medical applications of ginsenosides in the treatment of CVDs, many concerns exist in their application. This review discusses current works on the countless pharmacological functions and the potential benefits of ginseng in the area of CVDs. Results: Both in vitro and in vivo results indicate that ginseng has potentially positive effects on heart disease through its various properties including antioxidation, reduced platelet adhesion, vasomotor regulation, improving lipid profiles, and influencing various ion channels. To date, approximately 40 ginsenosides have been identified, and each has a different mechanism of action owing to the differences in chemical structure. This review aims to present comprehensive information on the traditional uses, phytochemistry, and pharmacology of ginseng, especially in the control of hypertension and cardiovascular function. In addition, the review also provides an insight into the opportunities for future research and development on the biological activities of ginseng.