• Journal of Ginseng Research
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• v.46 no.2
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• pp.206-213
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• 2022

Ginsenoside Rb2 is an active protopanaxadiol-type saponin, widely existing in the stem and leave of ginseng. Rb2 has recently been the focus of studies for pharmaceutical properties. This paper provides an overview of the preclinical and clinical pharmacokinetics for Rb2, which exhibit poor absorption, rapid tissue distribution and slow excretion through urine. Pharmacological studies indicate a beneficial role of Rb2 in the prevention and treatment of diabetes, obesity, tumor, photoaging, virus infection and cardiovascular problems. The underlying mechanism is involved in an inhibition of oxidative stress, ROS generation, inflammation and apoptosis via regulation of various cellular signaling pathways and molecules, including AKT/SHP, MAPK, EGFR/SOX2, TGF-β1/Smad, SIRT1, GPR120/AMPK/HO-1 and NF-κB. This work would provide a new insight into the understanding and application of Rb2. However, its therapeutic effects have not been clinically evaluated. Further studies should be aimed at the clinical treatment of Rb2.

• Toxicological Research
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• v.26 no.3
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• pp.223-232
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• 2010

Artesunate, a semi-synthetic derivative of artemisinin, is used primarily as a treatment for malaria. Its effects on the central nervous system, general behavior, and cardiovascular, respiratory, and other organ systems were studied using mice, rats, guinea pigs, and dogs. Artesunate was administered orally to mice at doses of 125, 250, and 500 mg/kg and to rats and guinea pigs at 100, 200, and 400 mg/kg. In dogs, test drugs were administered orally in gelatin capsules at doses of 50, 100, and 150 mg/kg. Artesunate induced insignificant changes in general pharmacological studies, including general behavior, motor coordination, body temperature, analgesia, convulsion modulation, blood pressure, heart rate (HR), and electrocardiogram (ECG) in dogs in vivo; respiration in guinea pigs; and gut motility or direct effects on isolated guinea pig ileum, contractile responses, and renal function. On the other hand, artesunate decreased the HR and coronary flow rate (CFR) in the rat in vitro; however, the extent of the changes was small and they were not confirmed in in vivo studies in the dog. Artesunate increased hexobarbital-induced sleeping time in a dose-related manner. Artesunate induced dose-related decreases in the volume of gastric secretions and the total acidity of gastric contents, and induced increases in pH at a dose of 400 mg/kg. However, all of these changes were observed at doses much greater than clinical therapeutic doses (2.4 mg/kg in humans, when used as an anti-malarial). Thus, it can be concluded that artesunate is safe at clinical therapeutic doses.

• Journal of Pharmacopuncture
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• v.22 no.3
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• pp.140-146
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• 2019

Objectives: Venomous fishes have different pharmacological effects and are useful. Among the venomous fish, stonefishes; especially Pseudosynanceia melanostigma has various pharmacological effects on the nervous, muscular and cardiovascular system of humans. In this study, toxicological characteristics, some blood effects, pharmacological and enzymatic properties of Pseudosynanceia melanostigma venom was investigated. Methods: Crude venom purified by using gel filtration chromatography and the molecular weights of the venom and its fractions were estimated. The approximate LD values of this venom were determinedand the effects of LD50 dose on the blood of rabbits were studied. Hemolytic and Hemorrhagic activity of the venom sample was determined. In this case coagulation tests were performed. Results: The LD50 of the Pseudosynanceia melanostigma crude venom was also determined to be $194.54{\mu}g/mouse$. The effect of two doses of LD50 showed a non-significant differences decrease in RBCs and MCV. In other cases, the results showed significant differences in WBC, Plt, Hb, MCH, MCHC and HCT; also it's showed a significant decrease. WBC count showed a significant increase with two doses of LD50 groups. The prothrombin time and partial prothrombin time were increased after venom treatment. As well as bleeding and clotting time were increased. According to the results, a minimum dose for Haemorrhagic effect $40{\mu}g$ was obtained. Conclusion: Venom of Pseudosynanceia melanostigma has inhibitory effect on platelet aggregation that can be used to design and develop of anticoagulant drugs.

• Journal of Physiology & Pathology in Korean Medicine
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• v.34 no.4
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• pp.184-190
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• 2020

This study was performed to find antibacterial substances contained in Scutellariae Radix (SR) using a systems pharmacological analysis method and to establish an effective strategy for the prevention and treatment of infectious diseases. Analysis of the main active ingredients of SR was performed using Traditional Chinese Medicine Systems Pharmacology (TCMSP) Database and Analysis Platform. 36 active compounds were screened by the parameter values of Drug-Likeness (DL), Oral Bioavailability (OB), and Caco-2 permeability (Caco-2), which were based on the drug absorption, distribution, metabolism, and excretion indicators. The UniProt database was used to obtain information on 159 genes associated with active compounds. The main active compounds with antibacterial effects were wogonin, β-sitosterol, baicalein, acacetin and oroxylin-A. Target proteins associated with the antibacterial action were chemokine ligand 2, interleukin-6, tumor necrosis factor, caspase-8,9 and mitogen-activated protein kinase 14. In the future, systems pharmacological analysis of traditional medicine will be able to make it easy to find the important mechanism of action of active substances present in natural medicines and to optimize the efficacy of medicinal effects for combinations of major ingredients to help treat certain diseases.

• Biomolecules & Therapeutics
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• v.9 no.1
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• pp.63-68
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• 2001

General pharmacological properties of (R)-JG-381 were examined in laboratory animals to investigate its safety profile. Administration of (R)-JG-381 (50 and 100 mg/kg) in mice and rats had no effects of general behaviors, central nervous system of the animals in test systems of pentobarbital-induced sleeping time, writhing syndromes induced by 0.7% acetic acid, chemo-shock produced by pentylenetetrazole, and, however, had mild effects on motor coordination. Heart rate and blood pressure were not changed by (R)-JG-381 treatment. (R)-JG-381 also showed mild effects on intestinal propulsion and gastric secretion. These results suggest that (R)-JG-381 dose not exert serious pharmacological effects.

• Biomolecules & Therapeutics
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• v.9 no.1
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• pp.51-54
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• 2001

Bufonis Venenum is a toad venom and its main components are bufadienolides, namely resibufogenin, bufalin and cinobufagin. The desensitizing effect of Bufonis Venenum is useful for the treatment of the premature ejaculation in Chinese medicine. But, minor components of Bufonis Venenum cause problems such as topical burring, pain, and erectile dysfunction. To clarify and eliminate the components responsible for these side effects, we prepared two extracts of Bufonis Venenum with either 70% ethanol or ethylacetate and tested their pharmacological effects. The extract of Bufonis Venenum with 70% ethanol produced pain response in rat hind paw, and exhibited contraction of rabbit corpus cavernosal muscle in vitro. On the other hand, the ethylacetate extract did not cause pain and smooth muscle contraction. The desensitizing effect of the ethylacetate extract was similar to that of the 70% ethanol extract. In conclusion, these results show that the extract of Bufonis Venenum with ethylacetate does not have the components causing side effects and deserve further study for therapeutic potential in premature ejaculation in men.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.217-217
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• 1994

Calcium entry blockers, capable of inhibiting transmembrane influx of extracellular calcium through specific calcium channels, are useful drugs in the treatment of angina pectoris, hypertension, cardiac arrythmia, and various cardiovascular disorders. Compounds having isoquinoline structures have recently been reported to possess calcium antagonistic action. Therefore, in the present study, we have attempted to synthesize some isoquinoline and related compound.; in order to search for potentially effective chemicals acting on cardiovascular system, and evaluated their pharmacological properties focusing on calcium antagonistic actions. Almost all of the compounds so far synthesized, had inhibitory action against phenylephrine or high potassium-induced contraction in vascular smooth muscle with different degrees of potencies depending on their structures, However, some of tetrahydroisoquinoline analogs showed directly inhibit calcium current in isolated rabbit cardiac myocytes examined by patch clamp techniques. The pharmacological properties of these compounds need more intensive investigation as to whether these chemicals may have developed as a new cardiovascular active drugs. Therefore, we are now under investigation of the mechanism of action of these compounds.

• Journal of the korean academy of Pediatric Dentistry
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• v.34 no.2
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• pp.341-348
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• 2007

We dentists perform many of routine dental procedures and must deal with much of the population's dental anxiety and fear. Dentists have used many non-pharmacological modalities initially to overcome anxiety and fear, including distraction, empathy, desensitization, and so on. However, certain patients need pharmacological backup of anxiety and fear to conquer dental treatment. This article presents four cases to introduce the methods from nitrous oxide and oxygen inhalation to general anesthesia for difficult adult dental phobic patients to deal with.

• Biomedical Science Letters
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• v.20 no.3
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• pp.117-123
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• 2014

Adenophorae Radix (AR) has been used as a traditional medicine for various diseases. However, the regulatory effects of AR in atopic dermatitis are not yet understood. This study attempted to determine the pharmacological effects of AR and its constituent on both compound 48/80 or histamine-induced scratching behaviors and 2, 4-dinitrochlrobenzene (DNCB)-induced atopic dermatitis in mice. The findings of this study demonstrated that AR reduced compound 48/80 or histamine-induced scratching behaviors in mice. Treatment of AR attenuated the AD symptoms such as eczematous, erythema and dryness and serum IgE and IL-6 levels in AD model. Additionally, AR inhibited the TNF-${\alpha}$-induced the Nuclear factor-${\kappa}B$ activation in HaCaT cells. Collectively, the findings of this study provide us with novel insights into the pharmacological actions of AR as a potential molecule for therapeutic agent against atopic dermatitis.

• Advances in Traditional Medicine
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• v.9 no.4
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• pp.269-276
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• 2009

Black pepper (family Piperaceae), is called king of spices because it is one of the oldest spice and alone accounts for about 35% of the world's total spice trade. The pepper is used in Ayurvedic medicine for the treatment of various ailments particularly neurological, broncho-pulmonary and gastrointestinal disorders. Pepper has also been reported to have various pharmacological actions but recently, it is highlighted as a bioavailability enhancer. This results in higher plasma concentration of drugs, nutrients, ions and other xenobiotics, rendering them more bioavailable for physiological as well as pharmacological actions in the body. Numerous scientific studies reported that piperine; a main bioactive compound of pepper, is responsible for its bioavailability enhancing property. It's a well known fact that pepper enhances bioavailability by inhibition of microsomal enzyme system but other mechanisms are also responsible to acts as a bioavailability enhancer. The brief overview of the mechanism of action of pepper as well as its applications as bioavailability enhancer is given in the present article.