• Title/Summary/Keyword: Antiviral Drug

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Formulation and Evaluation of Moisture-activated Acyclovir Patches (수분 감응성 아시클로버 패취제의 설계 및 평가)

  • Kim, Ah-Mee;Gwak, Hye-Sun;Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.36 no.6
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    • pp.393-399
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    • 2006
  • This study was aimed to design, formulate and characterize the moisture-activated patches containing acyclovir for antiviral action. Gel intermediates for film-type patches were prepared with mucoadhesive polymer, viscosity builders, enhancers and acyclovir. Patches containing acyclovir were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane, and of drug flux through the hairless mouse skin. Film-type patches obtained were uniform in the thickness and showed a mucoadhesive property when contacted with moisture. The formulation was optimized, which consisted of $Cantrez^{\circledR}$ AN-169(2%), $Kollidon^{\circledR}$ VA 64(1%), $Natrosol^{\circledR}$(1%), hydroxypropyl-$\beta$-cyclodextrin(1%) and dimethylsulfoxide(0.5%). Release rates of acyclovir patches increased dose-dependently. The addition of terpenes such as d-limonene or cineole increased release rates of acyclovir, but decreased permeation rates. The permeation rates were enhanced by 2 and 2.5 times by the addition of glycyrrhizic acid ammonium salt and sodium glycocholate, respectively, compared with that of no enhancer. These results suggest that it may be feasible to deliver acyclovir through the skin or gingival mucosa from the moisture-activated patches.

Antiherpetic Activities of Natural Quercitrin Alone and in Combinations with Nucleoside Antiherpetic Agents (천연 Quercitrin의 항허피스바이러스작용과 Nucleoside계 항허피스바이러스제와의 병용효과)

  • 김영소;어성국;김홍진;이도익;김기호;한성순
    • Biomolecules & Therapeutics
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    • v.7 no.2
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    • pp.158-163
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    • 1999
  • In order to find less toxic antiherpetic agents, antiviral activities of quercitrin against two strains of pathogenic viruses such as herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) were determined in Vero cells using plaque reduction assay in vitro. Quercitrin showed a concentration-dependent decrease in plaque formation of HSV-1 and HSV-2. It also exhibited more potent antiherpetic activity on HSV-1 with 50% effective concentration (EC$_{50}$) of 20.4 $\mu$g/ml than on HSV-2 with EC$_{50}$ of 30.4 $\mu$g/ml. The combined antiherpetic effects of quercitrin with nucleoside antiherpetic agents, acyclovir and vidarabine, were examined on the multiplication of these two strains of herpesviruses in Vero cells by the combination assay. The results of combination assay were evaluated by the combination index (CI) that was calculated by the multiple drug effect analysis. The combinations of quercitrin with acyclovir and vidarabine on HSV-1 showed more potent synergism with CI values of 0.27-0.81 for 50%, 70%, 90% effective levels than those on HSV-2 with CI values of 1.03~2.20..20.

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Subacute Toxicity of G009, a Polysaccharide Isolated from Ganoderma lucidum IY009 (영지버섯으로부터 분리한 단백다당체, G009의 아급성독성시험)

  • 서경원;조일상;오미현;이경민;김효정
    • Journal of Food Hygiene and Safety
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    • v.11 no.4
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    • pp.261-271
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    • 1996
  • It has been reported that G009, polysaccharide isolated from Ganoderma lucidum IY009 has various pharmacological effects, such as antinflamatory, antiviral, anticarcinogenic and immunmodulation effects. The purpose of this study was to determine the subacute toxicity of orally administered G009 in Sprague-Dawley rats. Groups of 40 male and 40 female rats were gavaged with 0, 500, 1,000 or 2,000 mg/kg/day for 30 days. No drug-related deaths and clinical morbidities were resulted. There was no drug-related effect on the body weight gain, food consumption and water consumption. Statistically significant changes were observed in several hematological and biochemical parameters of G009-treated groups; however, most of these changes were within normal range and had no relationship to dosage. Urinalysis and bone marrow biopsy showed no remarkable changes in all treated groups. Gross necropsy and hisopathology revealed no evidence of specific toxicity related to G009. Our data indicate that no-observed effect level of G009 is estimated to be above 2,000 mg/kg/day in rats.

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Microencapsulation of Isoprinosine with Ethylcellulose

  • Kim, Chong-Kook;Hwang, Sung-Joo
    • Archives of Pharmacal Research
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    • v.14 no.4
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    • pp.298-304
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    • 1991
  • Isoprinosine, an antiviral agent with a bitter taste, has been clinically used up to a maximum of 4 g daily in 4-8 doses. In this investigation, isoprinosine was microencapsulated with ethylcellulose 22 cps, 50 cps and 100 cps by means of polymer deposition from cyclohexane through temperature change. Complete removal of cyclohexane from the microcapsules was necessary, since ethylcellulose-coated microcapsules obtained from cyclohexane medium were heavily solvated with cyclohexane and formed lumps even after drying. The displacement of cyclohexane by n-hexane during isolation of microcapsules (Method III) or the freezing of the anal-washed microcapsules before drying (Mothod II) provided the dried products which were more discrete microcapsules than those which were simply dried in the air overnight (Method I). Method III was especially the most effective procedure in preparing finer and more discrete microcapsules. The drug-release from microcapsules was influenced by the ratio of core to wall, the viscosity grade of ethylcellulose and the overall microcapsule size. The release rate was adequately fitted to both the first-order and the diffusion-controlled processes. It is therefore possible to design the release-controlled microcapsules with ethylcellulose of different viscosity along with various core to wall ratio.

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Inhibition of HBV ]Replication by the Extract of Phyllanthus ussuriensis (여우주머니(Phyllanthus ussuriensis) 추출물의 B헝 간염바이러스 증식 억제)

  • Kim, Chul-Young;Kim, Jeong-Min;Kim, Tae-Gyun;Kim, Seung-Hee;Huh, Hoon
    • Biomolecules & Therapeutics
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    • v.6 no.2
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    • pp.139-144
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    • 1998
  • Abstract -Phyllanthus ussuriensis which belongs to Euphorbiaceae has been used as a component of Korean traditional remedy against hepatitis and jaundice. Aqueous methanolic extract of P. ussuriensis was tested for antiviral activity of hepatitis B virus (HBV) in HepG2 2.2.15 cells which were derived through transfection of cloned HBV DNA into HepG2 human hrpatoblastoma cells. P. ussuriensis extract decreased the levels of extracellular HBV virion DNA and inhibited HBV replication at concentrations ranging from 50 to 500$\mu$g/ml. Partitioning of water suspension of the extract revealed that the activity mainly resides in the EtOAc fraction. Consecutive purification of the EtOAc fraction by silica-gel column chromatography resulted in the two active anti-HBV fractions. Southern blot analysis shows that the action mechanisms or active site of the two fractions seems to be different in terms of their inhibition of HBV replication steps.

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Pharmacologic therapy for nonalcoholic steatohepatitis focusing on pathophysiology

  • Yoon, In Cheol;Eun, Jong Ryeol
    • Journal of Yeungnam Medical Science
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    • v.36 no.2
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    • pp.67-77
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    • 2019
  • The paradigm of chronic liver diseases has been shifting. Although hepatitis B and C viral infections are still the main causes of liver cirrhosis and hepatocellular carcinoma (HCC), the introduction of effective antiviral drugs may control or cure them in the near future. In contrast, the burden of nonalcoholic fatty liver disease (NAFLD) has been increasing for decades, and 25 to 30% of the general population in Korea is estimated to have NAFLD. Over 10% of NAFLD patients may have nonalcoholic steatohepatitis (NASH), a severe form of NAFLD. NASH can progress to cirrhosis and HCC. NASH is currently the second leading cause to be placed on the liver transplantation list in the United States. NAFLD is associated with obesity, type 2 diabetes, dyslipidemia, and metabolic syndrome. The pathophysiology is complex and associated with lipotoxicity, inflammatory cytokines, apoptosis, and insulin resistance. The only proven effective treatment is weight reduction by diet and exercise. However, this may not be effective for advanced fibrosis or cirrhosis. Therefore, effective drugs are urgently needed for treating these conditions. Unfortunately, no drugs have been approved for the treatment of NASH. Many pharmaceutical companies are trying to develop new drugs for the treatment of NASH. Some of them are in phase 2 or 3 clinical trials. Here, pharmacologic therapies in clinical trials, as well as the basic principles of drug therapy, will be reviewed, focusing on pathophysiology.

Current diagnosis and treatment of vestibular neuritis: a narrative review

  • Ba, Chang Hoon;Na, Hyung Gyun;Choi, Yoon Seok
    • Journal of Yeungnam Medical Science
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    • v.39 no.2
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    • pp.81-88
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    • 2022
  • Vertigo is the sensation of self-motion of the head or body when no self-motion is occurring or the sensation of distorted self-motion during an otherwise normal head movement. Representative peripheral vertigo disorders include benign paroxysmal positional vertigo, Ménière disease, and vestibular neuritis. Vestibular neuritis, also known as vestibular neuronitis, is the third most common peripheral vestibular disorder after benign paroxysmal positional vertigo and Ménière disease. The cause of vestibular neuritis remains unclear. However, a viral infection of the vestibular nerve or ischemia of the anterior vestibular artery is known to cause vestibular neuritis. In addition, recent studies on immune-mediated mechanisms as the cause of vestibular neuritis have been reported. The characteristic clinical features of vestibular neuritis are abrupt true-whirling vertigo lasting for more than 24 hours, and no presence of cochlear symptoms and other neurological symptoms and signs. To accurately diagnose vestibular neuritis, various diagnostic tests such as the head impulse test, bithermal caloric test, and vestibular-evoked myogenic potential test are conducted. Various treatments for vestibular neuritis have been reported, which are largely divided into symptomatic therapy, specific drug therapy, and vestibular rehabilitation therapy. Symptomatic therapies include generalized supportive care and administration of vestibular suppressants and antiemetics. Specific drug therapies include steroid therapy, antiviral therapy, and vasodilator therapy. Vestibular rehabilitation therapies include generalized vestibular and customized vestibular exercises.

Shikonin ameliorates salivary gland damage and inflammation in a mouse model of Sjögren's syndrome by modulating MAPK signaling pathway

  • Wenjing Guo;Xin Wang;Chao Sun;Jian Wang;Tao Wang
    • The Korean Journal of Physiology and Pharmacology
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    • v.27 no.4
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    • pp.357-364
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    • 2023
  • Sjögren syndrome (SS) is a systemic inflammatory autoimmune disease that involves exocrine glands. Shikonin is extracted from comfrey, which is conventionally used as an anti-tumor, antibacterial, and antiviral drug in China. However, the application of Shikonin in SS remains unreported. This study aimed to verify the potential functions of Shikonin in SS progression. Firstly, non-obese diabetic mice were used as the SS mouse model, with C57BL/6 mice serving as the healthy control. It was demonstrated that the salivary gland damage and inflammation were aggravated in the SS mouse model. Shikonin improved salivary gland function decline and injury in the SS mouse model. Moreover, Shikonin reduced inflammatory cytokines and immune infiltration in the SS mouse model. Further experiments discovered that Shikonin attenuated the MAPK signaling pathway in the SS mouse model. Lastly, inhibition of the MAPK signaling pathway combined with Shikonin treatment further alleviated the symptoms of SS. In conclusion, Shikonin ameliorated salivary gland damage and inflammation in a mouse model of SS by modulating the MAPK signaling pathway. Our findings indicate that Shikonin may be a useful drug for SS treatment.

Contamination and Detoxification of Aflatoxins (아플라톡신 오염 및 저감화 방안)

  • Cho, So-Yean;Kang, In-Ho;Shim, Young-Hoon;Yang, Dong-Hyug;Oh, Seh-Wook;Lee, Byung-Hee;Hyeon, Seong-Ye;Chang, Seung-Yeup;Jeong, Choon-Sik;Lee, Yong-Soo;Kim, Young-Shik;Kang, Shin-Jung
    • Korean Journal of Pharmacognosy
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    • v.38 no.3 s.150
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    • pp.205-216
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    • 2007
  • South Korea is the representative consumption country of herbal medicines and most of herbal medicines circulating in Korea have been importing from the developing countries of Southeast Asia such as China, Vietnam, Indonesia and so forth. Domestic hygiene and safety are continuously proposed because herbal medicines which are circulating have the possibility could remain contaminants or residues. Physicochemical contaminants such as heavy metals, persistent organic pollutants, radionucleosides, microbial toxins, biological contaminants such as microorganisms and animals, agrochemical residues such as pesticides, substances used for fumigation, antiviral agents, and solvent residues are classified as major contaminants and residues in herbal medicines from 2005 September WHO.$^{1)}$ Currently our administration have established a permission standard and the inspection criteria against the heavy metal, the residual pesticides and a residual sulfur dioxide. Furthermore our administration is continuously monitoring and conducting researches for the policies and their scientific ground against herbal medicines. But the appearances or discoveries of the harmful new species due to environmental and industrial developments are becoming social problems. Therefore it may be necessary to continuously consider and investigate regarding hereupon. Recently, the contamination of the mycotoxins against foods such as cereals, nuts and the powdered red pepper have developed and started became problematic issue, and possibility of contamination against the herbal medicine is proposed. And since populations who are using the herbal medicines very limited to several nations, recognition and researches about contamination of mycotoxins in herbal medicines are very insufficient. Therefore it will be need to more focus on the international regulation of quality control and safety for herbal medicines. Now on, we are going to introduce the importance, occurrence, characteristic properties, World-wide research trends and detoxification of aflatoxins, which is known as the most potent mutagen, carcinogen and teratogen mycotoxins.

MEDICINAL BENEFITS OF ADHATODA VASICA NEES.-IN UNANI AND CONTEMPORARY MEDICINE

  • Khan, Rabia;Shamsi, Yasmeen;Nikhat, Sadia
    • CELLMED
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    • v.10 no.2
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    • pp.13.1-13.7
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    • 2020
  • Arusa (Adhatoda vasica) is an important medicinal plant widely used in Unani system of medicine of (Family-Acanthaceae). The leaves of Adhatoda vasica contain several biologically active phytochemicals such as alkaloids, tannins, saponins, phenolics and flavonoids. It mainly consists of pyrroquinazoline, alkaloids, viz. vasicine, vasicol, vasicinone, peganine along with other minor constituents. The plant possesses diverse pharmacological activities, In Unani system of medicine, the drug is described as having dafa-e-tashannuj (anti-spasmodic), qatil-e-jarasim (antibiotic), mukhrij-e-balgham (expectorant), dafa-e-humma (antipyretic) properties due to which it is prescribed in a wide range of ailments like influenza, tuberculosis, bronchitis, gastric ulcers etc. Leaf juice is beneficial in the treatment of dysentery and diarrhoea. Various other activities like radio modulation, hypoglycaemic effect, cardiovascular protection, antitubercular, antiviral, hepatoprotective and antioxidant activity have also been reported.