Terrein is a small-molecule polyketide compound with a simple structure mainly isolated from fungi. Since its discovery in 1935, many scholars have conducted a series of research on its structure identification, isolation source, production increase, synthesis and biological activity. Studies have shown that terrein has a variety of biological activities, not only can inhibit melanin production and epidermal hyperplasia, but also has anti-cancer, anti-inflammatory, anti-angiopoietic secretion, antibacterial, insecticidal activities, and so on. It has potential application prospects in beauty, medicine, agriculture and other fields. This article reviews the process of structural identification of terrein since 1935, and summarizes the latest advances in its isolation, source, production increase, synthesis, and biological activity evaluation, with a view to providing a reference and helping for the in-depth research of terrein.

a,b ( a 海南师范大学化学与化工学院 热带药用资源化学教育部重点实验室 海口 571158) ( b 海南师范大学化学与化工学院 热带药用植物化学海南省重点实验室 海口 571158) ( c 海南科技职业大学 药食同源植物资源海南省重点实验室 海口 571126) 摘要 从蓝花黄芩内生真菌土曲霉(Aspergillus terreus) HQ100X-1 发酵产物中分离得到 2 个新化合物[terrustone (1)和 asperteretone G (2)], 10 个已知化合物(3～12), terrustone (1)为具有 4 个连续手性中心的三羟基环戊酮类化合物, 它们的 结构以及绝对构型是通过 1D/2D NMR 结合电子圆二色谱(ECD)计算来确定. 抗菌实验表明, 化合物 rbrolide R (4)对金 黄色葡萄球菌有一定的抑菌活性, 其最低抑菌浓度(MIC)值为 2.5 μg/mL.

Colon cancer stem cells (cCSCs) are highly tumorigenic and resistant to traditional chemotherapeutic drugs. Therefore, they are an essential factor in colorectal cancer (CRC) metastasis and recurrence. Dendritic cells (DCs) could bind to the tumor cells and form the fusion cells (FCs). And these FCs could inhibit the development of malignant tumors. Furthermore, the cytokine induced killer (CIK) cells (CD3+ /CD56+ T lymphocytes) could also apply for the immunotherapy of cancer. And compound Kushen injection (CKI) is a traditional Chinese medicine (TCM) which has been used for the treatment of various tumors. However, whether the dendritic-colon cancer stem cell fusion cells (DC-cCSC FCs) could activate the CIK cells and kill the colon cancer stem cells is unknown. And whether the CKI could enhance the lethal effect is still unclear. In this study, we collected peripheral blood samples from healthy participants to acquire mononuclear cells and induced DC and CIK cells. Meanwhile, the CD44+ cells (cCSCs) were screened from SW480 cells. Next, the DC-cCSC FCs were established for the next experiments. At last, CCK-8 assays were performed to determine the effect of DC-cCSC FCs and CKI on the viability of cCSCs. We found that DC-cCSC FCs enhanced the proliferation of CIK cells and induce the CIK cells to secrete more IL-12. The DC-cCSC FCs enhanced the inhibitory effect of CIK cells on cCSCs. Furthermore, application of CKI enhanced the killing rates of DC-cCSC FCs and CIK cells on cCSCs. CIK cells activated by the DC-cCSC FCs had the lethal effect on the cCSCs. Furthermore, CKI enhanced this lethal effect of DC-cCSC FCs and CIK cells.

Colorectal cancer (CRC) is a common malignancy with poor prognosis. This study aimed to explore the role of deubiquitinase 3 (DUB3) in CRC cell migration and angiogenesis as well as its molecular mechanism. HCT116 cells were transfected with DUB3 or EZH2 siRNA, or vectors overexpressing EZH2/HIF-1α. CCK8 and colony formation assay were used to assess cell proliferation; wound healing assay and Transwell assay were performed to determine cell migration and invasion; angiogenesis in CRC was detected using tube formation assay; WB was used to measure the protein levels of DUB3, EZH2, p65, p-p65, and HIF-1α. DUB3 downregulation inhibited proliferation, migration, invasion, and angiogenesis in CRC cells. Moreover, DUB3 could positively regulate NF-κB/HIF-1α pathway through EZH2. Overexpression of HIF-1α reversed the effects of DUB3 knockdown on CRC cell proliferation, migration, invasion, and angiogenesis. DUB3 contributes to CRC metastasis and angiogenesis by regulating NF-κB/HIF-1α pathway via EZH2, which may indicate a novel insight for the pathogenesis of CRC.

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