• 제목/요약/키워드: Anti-HIV-1

검색결과 121건 처리시간 0.023초

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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    • 제83권1호
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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.

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

  • 홍준희;박정하;송지연;최보길;정병호;김중협;이종교;정원근;천문우
    • 약학회지
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    • 제38권6호
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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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    • 제33권7호
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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.

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

  • 지근호;정태혁;김영태
    • 생명과학회지
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    • 제25권1호
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    • pp.29-36
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    • 2015
  • 천연의 붉은 색소인 prodigiosin은 Serratia marcescens에 의해서 생산되며 이는 pyrrolylpyrromethane 골격으로 구성되어 있다. 이 색소는 그 분자가 가진 특성 때문에 넓은 범위에서 활용되고 있다. 또한 항암제, 면역억제제, 항진균제, 살조제 등 다양한 분야의 효과가 보고되소 있다. Methicillin-resistant Staphylococcus aureus (MRSA)는 세계적으로 가장 주요한 원내 감염균으로써, 미국에서 해마다 HIV로 사망하는 수보다 더 많은 사망률을 보이고 있다. 그러므로 MRSA에 대한 새로운 치료제의 개발이 매우 중요하며 급박한 문제이다. 본 연구에서는 중증오염도를 가진 하천수로부터 Serratia sp. PDGS 120915를 분리하였으며 항 MRSA 활성을 가진 prodigiosin에 대하여 연구하였다. 본 연구를 위하여 HPLC를 이용하여 물질을 정제하였으며, 분리된 물질의 항 MRSA 활성을 확인하였다. Prodigiosin의 MRSA에 대한 최소억제농도(Minimal inhibitory concentration; MIC)는 $32{\mu}g/ml$이었으며, 분할저해농도(Fractional inhibitory concentration; FIC)는 ampicillin과 penicillin에서 상승작용이 있는 것으로 나타났다.

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

  • 박기동
    • Tuberculosis and Respiratory Diseases
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    • 제52권6호
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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
    • 통합자연과학논문집
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    • 제8권2호
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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 $100{\mu}M$.

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

  • 박현정;이상협
    • 약학회지
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    • 제54권1호
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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.

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

  • 이계원;이주연;조영호
    • KSBB Journal
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    • 제25권1호
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    • pp.18-24
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    • 2010
  • 본 연구에서는 가래나무 추출물의 항산화 효과와 티로시나제 활성 저해, 멜라닌 생성 및 티로시나제 합성 억제효과를 측정하고 이 추출물을 함유하는 제품의 임상시험을 실시하여 미백 화장품 소재로서의 개발 가능성을 관찰하였다. 가래나무 추출물은 농도 의존적으로 DPPH radical과 초산소 음이온 라디칼을 소거하였고, $SC_{50}$값은 각각 $20\;{\mu}g/mL$$25\;{\mu}g/mL$ 이었다. B16/BL6 멜라노마 세포를 이용하여 세포내 티로시나제 활성, 멜라닌 생성 및 티로시나제 합성 억제 효과를 측정한 결과 농도 의존적으로 티로시나제의 활성 및 멜라닌 생성을 억제하였으며, 티로시나제 단백질의 합성도 감소시켰다. 또한, 임상시험을 통하여 가래나무 추출물을 함유한 화장품이 대조 제품에 비해 통계적으로 유의한 피부 미백 효과가 있음을 확인하였다. 이상의 결과를 종합해 볼 때 가래나무 추출물은 색소침착 방지와 개선에 효과있는 새로운 미백 원료로 개발할 수 있을 것으로 사료된다.