• Title/Summary/Keyword: anti HIV-1

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Effectiveness of Intravenous Isoniazid and Ethambutol Administration in Patients with Tuberculosis Meningoencephalitis and HIV Infection

  • Butov, Dmytro;Feshchenko, Yurii;Kuzhko, Mykhailo;Gumenuik, Mykola;Yurko, Kateryna;Grygorova, Alina;Tkachenko, Anton;Nekrasova, Natalia;Tlustova, Tetiana;Kikinchuk, Vasyl;Peshenko, Alexandr;Butova, Tetiana
    • Tuberculosis and Respiratory Diseases
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    • v.83 no.1
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    • pp.96-103
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    • 2020
  • Background: The aim of this study was to investigate the effectiveness of intravenous isoniazid (H) and ethambutol (E) administered in patients with new sputum positive drug-susceptible pulmonary tuberculosis (TB) with tuberculous meningoencephalitis (TM) and human immunodeficiency virus (HIV) co-infection in the intensive phase of treatment. Methods: Fifty-four patients with TB/TM and HIV co-infection were enrolled for this study. Group 1 comprised of 23 patients treated with E and H intravenously, while rifampicin and pyrazinamide were prescribed orally. Group 2 consisted of 31 patients treated with the first-line anti-TB drugs orally. The concentrations of H and E in blood serum were detected using a chromatographic method. Results: A significant improvement in the clinical symptoms and X-ray signs in patients treated intravenously with H and E was observed and compared to group 2. The sputum Mycobacterium tuberculosis positivity was observed during the second month of the treatment in 25.0% of patients from group 1 and 76.1% of the patients from the control group (p=0.003). In addition, nine patients (39.1%) died up to 6 months when H and E were prescribed intravenously compared with 22 (70.9%) in group 2 (p=0.023). Conclusion: In TB/TM with HIV, the intravenous H and E treatment was more effective than oral H and E treatment at 2 months of intensive treatment in sputum conversion as well as in clinical improvement, accompanied by significantly higher mean serum concentrations. In addition, the mortality rate was lower in intravenous H and E treatment compared to oral treatment.

Synthesis of L-1,3-Dioxolane and L-1,3-Oxathiolane Pyrimidine Nucleosides (L-1,3-Dioxolane 및 L-1,3-Oxathiolane 피리미딘 뉴크레오사이드의 합성)

  • Hong, Joon-Hee;Park, Jeong-Ha;Song, Ji-Yeon;Choi, Bo-Gil;Chung, Byung-Ho;Kim, Joong-Hyup;Lee, Chong-Kyo;Chung, Won-Keun;Chun, Moon-Woo
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.775-781
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    • 1994
  • $({\pm})-Dioxolane-T$ and$({\pm})-BCH-189$ are know to possess anti-HIV activities, and less to xicities compared to other dideoxynucleoside AIDS drugs. We have synthesized 34 different enantiomerically pure nucleosides by glycosylation of L-1,3-dioxolanyl acetate and L-1,3-oxathiolanyl acetate sugar moieties with uracil or 6-azauracil with alkyl chains$(C_1-C_3)$ on 5 or 6 position.

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Immunostimulatory Activity of Syneilesis palmata Leaves through Macrophage Activation and Macrophage Autophagy in Mouse Macrophages, RAW264.7 Cells

  • So Jung Park;Jeong Won Choi;Hyeok Jin Choi;Seung Woo Im;Jin Boo Jeong
    • Journal of Microbiology and Biotechnology
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    • v.33 no.7
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    • pp.934-940
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    • 2023
  • Syneilesis palmata (SP) is a traditional medicinal plant. SP has been reported to have anti-inflammatory, anticancer, and anti-human immunodeficiency virus (HIV) activities. However, there is currently no research available on the immunostimulatory activity of SP. Therefore, in this study, we report that S. palmata leaves (SPL) activate macrophages. Increased secretion of both immunostimulatory mediators and phagocytic activity was observed in SPL-treated RAW264.7 cells. However, this effect was reversed by the inhibition of TLR2/4. In addition, inhibition of p38 decreased the secretion of immunostimulatory mediators induced by SPL, and inhibition of TLR2/4 decreased the phosphorylation of p38 induced by SPL. SPL augmented p62/SQSTM1 and LC3-II expression. The increase in protein levels of p62/SQSTM1 and LC3-II induced by SPL was decreased by the inhibition of TLR2/4. The results obtained from this study suggest that SPL activates macrophages via TLR2/4-dependent p38 activation and induces autophagy in macrophages via TLR2/4 stimulation.

Anti-MRSA Properties of Prodigiosin from Serratia sp. PDGS 120915 (Serratia sp. PDGS 120915가 생산하는 prodigiosin의 항 MRSA 특성에 관한 연구)

  • Ji, Keunho;Jeong, Tae Hyug;Kim, Young Tae
    • Journal of Life Science
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    • v.25 no.1
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    • pp.29-36
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    • 2015
  • Prodigiosin, a member of natural red pigment family, is produced by Serratia marcescens, and characterized by a common pyrrolylpyrromethane skeleton. This pigment has been reported with the effects of anticancer, immunosuppressant, antifungal, and algicidal activities. Methicillin-resistant Staphylococcus aureus (MRSA) is a major cause of hospital infections. In this study, anti-MRSA properties of prodigiosin isolated from Serratia sp. PDGS 120915 were investigated. We identified and purified prodigiosin using high performance liquid chromatography (HPLC) and evaluated anti-MRSA activity. Purified prodigiosin inhibited the growth of MRSA. The minimum inhibitory concentrations (MICs) of prodigiosin were determined to $32{\mu}g/ml$ against the MRSA strains. Fractional inhibitory concentration (FIC) indices of ampicillin and penicillin were indicated synergistic effects of prodigiosin on MRSA.

Tuberculosis Management of Private Health Care Institution : Current Situation and Task (민간 의료기관 결핵관리의 오늘과 내일)

  • Park, Ki-Dong
    • Tuberculosis and Respiratory Diseases
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    • v.52 no.6
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    • pp.579-589
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    • 2002
  • Since the inception of the National Tuberculosis Control Program in 1962, the incidence of tuberculosis and its associated mortality has declined dramatically due to effective anti-tuberculosis drugs and a systematic control program. The prevalence of radiographically active tuberculosis has fallen from 5.1% in 1965 to 1.0% in 1995. However, tuberculosis is still a major problem, as the mortality rate is still higher compared to other developed countries. Furthermore, tuberculosis is currently re-emerging in HIV/AIDS epidemic countries. In order to lower the tuberculosis death rate to the levels of developed countries, the tuberculosis control efforts in private healthcare institutions and the national tuberculosis control program in the public sector, need to work together more effectively and efficiently. In this paper, the quthor reviewed the current situation regarding tuberculosis management in private healthcare institutions of Korea based on the literature and the National Health Insurance Claim data, and the future tasks of tuberculosis management are suggested.

Design and Synthesis of Novel 2'(β)-Fluoro-3'(α)-hydroxy-threose Nucleosides: Iso-FMAU Analogues as Potent Antiviral Agents

  • Kim, Seyeon;Jee, Jun-Pil;Hong, Joon Hee
    • Journal of Integrative Natural Science
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    • v.8 no.2
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    • pp.99-106
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    • 2015
  • Novel 2'(${\beta}$)-fluoro-3'(${\alpha}$)-hydroxy-threose nucleosides (iso-FMAU) as antiviral agents were designed and racemically synthesized from Solketal. Condensation successfully proceeded from a glycosyl donor 9 under $Vorbr{\ddot{u}}ggen$ conditions yielded the nucleoside analogues. Ammonolysis and hydrolysis of isopropylidene protection group gave the desired nucleoside analogues 12, 15, 18, and 19. The antiviral activities of the synthesized compounds were evaluated against the HIV-1, HSV-1, HSV-2 and HCMV. Compound 12 displayed some anti-HCMV activity ($EC_{50}=24.7{\mu}g/ml$) without exhibiting any cytotoxicity up to $100{\mu}M$.

Studies on the Components of Valerian and Isovaleramide (Valerian의 구성성분 및 이소발레르아미드에 관한 연구)

  • Park, Hyun-Jung;Lee, Sang-Hyup
    • YAKHAK HOEJI
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    • v.54 no.1
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    • pp.1-7
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    • 2010
  • Valerian (Valeriana officinalis L.) is a perennial that has been used for medicinal purposes from the ancient times and valerian preparations including root and rhizome extracts are known to possess a variety of biological activities such as anticonvulsant, antidepressant, sleep aid, tranquilizer, and anti-HIV activities. Main components of the extracts were classified according to the structural features. Importantly, one of the main components, isovaleramide, has drawn our attention due to the concise structure, broad spectrum, and low toxicities. The general aspects including generation of this interesting molecule, a variety of activities, pharmacokinetic properties, derivatization, and fusion with other known drugs were described. Isovaleramide has been isolated from valerian probably as an isolation artifact after treatment of ammonia to prepare ammoniated tincture, and is known to exhibit anticonvulsant, anxiolytic, sedative, and sleep aid activities without distinct side effects such as excessive sedation and decreasing muscle tone. It was also found to be well absorbed into the circulation system without specific cytotoxicity and genotoxicity. The derivatives of isovaleramide, valpromide, valrocemide and valnoctamide were also briefly discussed.

Whitening Effect of the Extracts from Juglans mandshurica (가래나무 추출물의 미백효과)

  • Lee, Gye-Won;Lee, Ju-Yeon;Cho, Young-Ho
    • KSBB Journal
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    • v.25 no.1
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    • pp.18-24
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    • 2010
  • Juglans mandshurica belongs to the family Juglandaceae is known to contain a wide range of pharmacological activities including anti-cancer, anti-inflammation, astringent, and anti-human immunodeficiency virus-type 1 (HIV-1). Melanogenesis refers to the biosynthesis of melanin pigment in melanocytes. In this study, to investigate the whitening activity of the extracts from Juglans mandshurica, we measured effects on a tyrosinase activity, a melanogenesis, and a tyrosinase synthesis in the B16/BL6 melanoma cells and an antioxidant activity. The extracts significantly scavenged a 1,1-diphenyl-2-picrylhydrazyl (DPPH) and a superoxide anion radicals in a dose-dependent manner with a $SC_{50}$ value of $20\;{\mu}g/mL$ and $25\;{\mu}g/mL$, respectively. Also, the tyrosinase activity and melanogenesis were significantly inhibited by the extracts. Furthermore, the synthesis of tyrosinase protein was significantly decreased by the extracts in enzyme-linked immunosorbent assay. Double blind study on the clinical efficacy of a cream containing 2% of the extracts showed that the extracts have a significant skin whitening effect. Therefore, this study demonstrates that the extracts from Juglans mandshurica may be useful as a potential agent for skin whitening.