Three new lignan glucosides from the roots of Scutellaria baicalensis

Three new lignan glucosides, baicalensinosides A-C (1-3), were isolated from the roots of Scutellaria baicalensis. The structural elucidation was achieved by in-depth spectroscopic examinations and qualitative chemical test. Structurally, these compounds belong to the 3,4-dibenzyltetrahydrofuran-type lignan glycoside with a mono-hydroxyl substitution at the 7'-position of benzylidene group on the numbering system of lignans being one of their shared critical features. The anti-osteoporotic activity of the isolated compounds was assessed in an in vitro osteoprotegerin (OPG) transcriptional activity assay using dual luciferase reporter detection. At 10 μmol/L, compounds 1-3 increased the relative activating ratio of OPG transcription to 1.83, 0.84 and 0.98 times that of the control group, respectively.

Chemical constituents of the roots of Macleaya microcarpa and activation efficacy of benzophenanthridine alkaloids for the transcription of xbp1 gene / 药学学报

Ongoing study on the chemical constituents of the roots of Macleaya microcarpa led to the isolation of eight compounds of derivatives of triterpenes and organic acids in addition to some previously identified benzophenanthridines. The eight compounds were identified by spectroscopic methods as well as comparison with literature values as 1-oxo-2, 22 (30)-hopandien-29-oic acid (1), 3-oxo-12-oleanen-30-oic acid (2), 3α-hydroxy-12-oleanen-30-oic acid (3), 3β-hydroxy-12-oleanen-30-oic acid (4), ferulic acid (5), ferulic acid 4-O-β-D-glucoside (6), 3-O-feruloylquinic acid (7), and methyl 3-O-feruloylquinate (8). Of which, 1 is a new triterpenoid of hopanes and 2-8 are isolated from M microcarpa for the first time. In order to discover natural active compounds as potential agents of anti-ulcerative colitis (UC), an in vitro drug high-throughput screening model targeted x-box-binding protein 1 (xbp1) was employed to evaluate the activity of the major chemical constituents of M microcarpa. The result confirmed that two dihydrobenzophenanthridines, dihydrosanguinarine (9) and dihydrochelerythrine (10), showed a certain activity on activating the transcription of xbpl, a transcription factor (TF) associated with the occurrence, development, and potential treatment of UC, with their relative activating ratios being 1.76 and 1.77 times, respectively, as compared with control group.

The effect of co-inoculating human lymphatic endothelial cells on growth and metastasis of breast cancer cell and of osteosarcoma cell in nude mice / 基础医学与临床

Objective To investigate the effects of lymphangiogenesis on cancer growth and metastasis.Methods Human lymphatic endothelial cells(HLyECs)were isolated and purified from human lymph node by magnetic beads coated with antibody against human VEGFR3.Human breast cancer cell line(MDA-MB-435)or human osteosarcoma cell line(MG-63)was inoculated alone or co-inoculated with HLyECs subcutaneously into nude mice.The weight of tumor and lung surface metastasis were detected;peri-tumor lymphatic vessels were shown by Evans blue,intra-tumor lymphatic vessels were shown by immunohistochemistry for human and mouse PDPN.Conditioned medium of tumor on proliferation of HLyECs was evaluated by MTT assay.Results Compared with inoculating tumor cells alone,the growth and metastasis of MDA-MB-435 were promoted by co-inoculating HLyECs.The peritumoral and intra-tumoral lymphatic vessel density of MDA-MB-435 were increased by co-inoculating HLyECs.Both hPDPN-and mPDPN-positive lymphatic vessels were found.But co-inoculating HLyECs had no effect on lymphatic vessels density of MG-63.Neither intra-nor peri-tumor lymphatic vessels were found.The proliferation of HLyECs was increased by conditioned medium of MDA-MB-435 but not by MG-63.Conclusion Growth and lymphangiogenesis of breast cancer can be enhanced by co-inoculating lymphatic endothelial cells.