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1
Thành phần hóa học phần dưới mặt đất của cây Lạc Tân Phụ (Astilbe rivularis Buch.-Ham. ex D. Don) / Nguyễn Đức Hùng, Nguyễn Quốc Tuấn, Hà Thanh Hòa, Hà Quang Lợi, Đinh Thị Quỳnh Anh, Nguyễn Minh Khởi, Phương Thiện Thương, Phạm Quốc Tuấn // Tạp chí Dược học . - 2018. - tr. 84-88. - ISSN:



Ký hiệu phân loại (DDC): 615
In phytochemical study of the perennial herb Astilbe rivularis (Buch.-Ham. ex D. Don.) (Saxifragaceae) usually used in folk and traditional medicine for treatment of ulcer, inflammation, body ache, diarrhea, and dysentery, five natural compounds were isolated from the plant underground parts collected in Sa Pa district (Lao Cai province, North Vietnam) and spectrocopically identified as aquilegiolide (1), menisdaurilide (2), glochidionolactone A (3), astilbin (4), and (+)-catechin (5) by ESI-MS, 1H-NMR, 13C-NMR in reference to the literature. Of them, the occurence of compounds 1-3 in this plant was reported for the first time.
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2
Tối ưu hóa công thức bào chế tiểu phân Nano Dihydroartemisinin với chất mang Eudragit EPO / Nguyễn Ngọc Chiến, Lê Thị Phương, Trần Trịnh Công // Tạp chí Dược học . - 2018. - tr. 3-6. - ISSN:



Ký hiệu phân loại (DDC): 615
Dihydroartemisinin-loaded Eudragit EPO-based nanoparticles were made by oil/water emulsion evaporation. Influence of several formulation factors on physicochemical characteristics of nanoparticles was evaluated to optimize the formulation. Experiments were designed by Modde 8.0 and analyzed by FormRule 2.0 and InForm 3.1 to determine the impacts of three independent variables (ratio of dihydroartemisinin to Eudragit EPO, concentrations of Cremophor A25 and volume of aqueous phase) on some response variables (particle size, polydispersity index, zeta potential, loading capacity and encapsulation efficiency). The optimized formulation was obtained with size of 170 nm, PDI below 0.3, zeta potential of 23.7 mV, encapsulation efficiency of 42.3 % and loading capacity of 11.21 %.
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3
Tổng hợp một số dẫn chất 6-(n-butylamino)-2-Arylquinazolin-4(3H)-on hướng kháng ung thư / Lê Nguyễn Thành, Trần Minh Huệ, Ngô Xuân Hoàng, Hoàng Thu Trang, Đinh Ngọc Thức, Văn Thị Mỹ Huệ // Tạp chí Dược học . - 2018. - tr. 75-80. - ISSN:



Ký hiệu phân loại (DDC): 615
A series of 2-arylquinazolin-4(3H)-on was designed in expectaion of anticancer effects. Substitutions at C6 and C2’ position of the structures were introduced. Targeted compound 6a-d were obtained by a 3-steps pathway from 2-amino-5-butylaminobenzamid and corresponding aldehydes. Cytotoxicity of the synthesized compounds were tested against two cancer cell lines (human epidermic carcinoma-KB and hepatocellular carcinoma-HepG2). As expected, all the tested compounds exhibited stronger cytotoxicity than ellipticine. Notably, compound 6c and 6d exposed the desirable activity 18 - 27 times as strong as ellipticine with IC50 ranging at 0,09-0,12 mM. These findings clarified why the 2-arylquinazolin-4(3H)-on derivatives with 2’-substitution have been considered as very potential anticancer agents.
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4
Tổng hợp và thử hoạt tính sinh học của một số dẫn chất Benzamid có nhân Quinazolin / Nguyễn Thị Thuận, Nguyễn Hải Nam, Đoàn Thanh Hiếu // Tạp chí Dược học . - 2018. - tr. 41-44. - ISSN:



Ký hiệu phân loại (DDC): 615
A series of 6 novel benzamid incorporating quinazoline heterocycles (4a-f) were synthesized as novel histone deacetylases inhibitors. By bioevaluation, these quinazoline-based benzamide showed potent cytotoxicity against the following three human cancer cell lines: SW620 (colon), PC-3 (prostate) and NCI-H23 (lung), displaying the potency 5 - up to 10-fold higher than SAHA (suberoylanilidehydroxamic acid, vorinostat). Also, these compounds were comparable to SAHA in inhibiting HDACs with IC50 values within the sub-micromolar range. Of these, two compounds (4c) and (4f) were HDAC inhibitors even more potent than SAHA in Hela extract assay and expected to be promising anticancer drug candidates.
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5
Tổng hợp và xác định độ tinh khiết tạp chất liên quan D (ethyl 5-amino-1H-pyrazol-4-carboxylat) của Alopurinol / Nguyễn Trần Vân Anh, Lữ Thiện Phúc, Phạm Lê Ngọc Yến, Nguyễn Đức Tuấn // Tạp chí Dược học . - 2018. - tr. 32-36. - ISSN:



Ký hiệu phân loại (DDC): 615
Allopurinol impurity D (ethyl 5-amino-1H-pyrazole-4-carboxylate) was synthesized from ethyl (ethoxymethylene) cyanoacetate and hydrazine in the yield of 61.3 % (0.28 gram). By using HPLC – PDA, its chromatographic purity was determined over 99.0 %. As such, the obtained allopurinol impurity D was fairly satisfactory for establishment of the reference substance. Moreover, an HPLC method for purity determination of impurity D was developed as: column - XtimateR C18 (5 µm; 250 4.6 mm); Detector – UV (247 nm; Mobile phase - methanol and water (40:60, v/v); Flow rate - 1.0 mL/min. Validation in observance to ICH guidelines, the method showed to hand wide linearity range (25.16 – 503.10 µg/ml), high precision (RSD £ 0.03 %). The method showed good selectivity, wide linearity range and high precision.
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