Novel berberine derivatives: Design, synthesis, antimicrobial effects, and molecular docking studies / 中国天然药物

A series of berberine derivatives were synthesized by introducing substituted benzyl groups at C-9. All these synthesized compounds (4a-4m) were screened for their in vitro antibacterial activity against four Gram-positive bacteria and four Gram-negative bacteria and evaluated for their antifungal activity against three pathogenic fungal strains. All these compounds displayed good antibacterial and antifungal activities, compared to reference drugs including Ciprofloxacin and Fluconazole; Compounds 4f, 4g, and 4l showed the highest antibacterial and antifungal activities. Moreover, all the synthesized compounds were docked into topoisomerase II-DNA complex, which is a crucial drug target for the treatment of microbial infections. Docking results showed that H-bond, π-π stacked, π-cationic, and π-anionic interactions were responsible for the strong binding of the compounds with the target protein-DNA complex.

Novel berberine derivatives: Design, synthesis, antimicrobial effects, and molecular docking studies / 中国天然药物

A series of berberine derivatives were synthesized by introducing substituted benzyl groups at C-9. All these synthesized compounds (4a-4m) were screened for their in vitro antibacterial activity against four Gram-positive bacteria and four Gram-negative bacteria and evaluated for their antifungal activity against three pathogenic fungal strains. All these compounds displayed good antibacterial and antifungal activities, compared to reference drugs including Ciprofloxacin and Fluconazole; Compounds 4f, 4g, and 4l showed the highest antibacterial and antifungal activities. Moreover, all the synthesized compounds were docked into topoisomerase II-DNA complex, which is a crucial drug target for the treatment of microbial infections. Docking results showed that H-bond, π-π stacked, π-cationic, and π-anionic interactions were responsible for the strong binding of the compounds with the target protein-DNA complex.

Synthesis and evaluation of benzylisoquinoline derivatives for their inhibition on pancreatic lipase and preadipocyte proliferation / 中国天然药物

The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bischler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, and the products were obtained by reductions. All these compounds were identified by MS, (1)H NMR and (13)C NMR. The inhibitory activities on pancreatic lipase and preadipocyte proliferation for the synthesized compounds and alkaloids from Nulembo nucifera were assessed in vitro. Most of the compounds showed inhibitory activities on both pancreatic lipase and preadipocyte proliferation. Particularly, compounds 7p-7u and 9d-9f exhibited significant inhibitory activity on pancreatic lipase while compounds 7c, 7d, 7f, 7g, 7i, and 7j potently inhibited the proliferation of 3T3-L1 preadipocytes. Our results provided a basis for future evaluation and development of these compounds as leads for therapeutics for human diseases.

Cytotoxic alkaloids from stems of Nelumbo nucifera / 中国中药杂志

Chemical investigation was carried out to study the alkaloids from stems of Nelumbo nucifera and their cytotoxic activities. The constituents were separated by column chromatography, and their structures were elucidated by spectroscopic data analyses. The isolated compounds were evaluated for their cytotoxic activities by MTr method. Fifteen compounds were isolated from the total alkaloids extract and identified as asimilobine (1), isococlaurine (2), N-acetylnorarmepavine (3), crykonisine (4), velucryptine (5), pycnarrhine (6), liriodenine (7), nuciferine (8), nornuciferine (9), armepavine (10), N-methylasimilobine (11), coclaurine (12), N-norarmepavine (13), N-methylcoclaurine (14) and lysicamine (15). Compounds 1-7 and 12-15 were isolated from stems of this plant for the first time, and compounds 2-6 were firstly isolated from the family Nelumbonaceae. Compounds 7-10, 13 and 14 showed significant cytotoxic activities against HL-60 carcinoma cell line with inhibitory ratios of 51.36%, 59.09%, 52.51%, 53.93%, 51.43%, and 64.31% at concentration of 1 x 10(-5) mol x L(-1), respectively.

Chemical constituents from Hedyotis diffusa / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents from Hedyotis diffusa.</p><p><b>METHOD</b>The compounds were isolated and purified by various chromatographic techniques and identified by their physicochemical properties and spectral data.</p><p><b>RESULT</b>Eight compounds were isolated and identified as octadecyl (E)-p-coumarate (1), p-E-methoxy-cinnamic acid (2), ferulic acid (3), scopoletin (4), succinic acid (5), aurantiamide acetate (6), rubiadin (7), robustaquinone D (8).</p><p><b>CONCLUSION</b>Compounds 1-8 were obtained from genus Hedyotis for the first time.</p>

Studies on chemical constituents in root tuber of Cynanchum auriculatum / 中国中药杂志

<p><b>OBJECTIVE</b>To study chemical constituents from Cynanchum auriculatum.</p><p><b>METHOD</b>The chemical components were isolated and purified by silca gel, sephedex-LH-20 and ODS column chromatography. The chemical structures were elucidated on the basis of physicochemical properties and spectral data.</p><p><b>RESULT</b>Thirteen compounds were isolated and identified as: caudatin (1), metaplexigenin (2), cynauricuoside A (3), succinic acid (4), azelaic acid (5), wilforibiose (6), sucrose (7), 1-O-hexadecanolenin (8), beta-amyrin acetate (9), cynanchone A (10), acetylquinol (11), beta-sitosterol (12), daucosterol (13).</p><p><b>CONCLUSION</b>Compounds 4-9 were obtained from this plant for the first time.</p>

A new alkaloid from Opuntia vulgaris / 药学学报

<p><b>AIM</b>To study the chemical constituents of the stems of Opuntia vulgaris Mill(Cactaceae).</p><p><b>METHODS</b>The compounds of Opuntia vulgaris were isolated by chromatography of Amberlite Dowex 50 and silica gel, and identified by means of UV, IR, MS, 1D and 2D NMR.</p><p><b>RESULTS</b>Three compounds were isolated and identified as: opuntin B(I), 4-hydroxyproline(II) and tyrosine(III).</p><p><b>CONCLUSION</b>Compound I is a new alkaloid.</p>