A new flavonoid derivative, (2 R, 3 R)-5,7,3',4',5'-pentamethoxyflavan-3-O-β-D-glucopyranose (1), along with ten known flavonoids, was obtained from Brandisia hancei Hook. f. via ethanol extraction and chromatographic separation. The chemical structure of compound 1, including its absolute configuration, was determined using a combination of UV, IR, HR-ESI-MS, and various NMR techniques. To assess anti-inflammatory properties, compounds 1-9 were tested for their ability to suppress nitric oxide (NO) generation in LPS-activated RAW264.7 macrophages. Screening data indicated that compounds 1 (IC50 = 112.8 μg/mL), 4 (IC50 = 16.81 μg/mL), and 8 (IC50 = 0.68 μg/mL) displayed considerable NO-inhibitory activity. Further mechanistic studies on these three isolates revealed that compound 4 markedly reduced the secretion of TNF-α and IL-6, with corresponding IC50 values of 31.08 μg/mL and 22.99 μg/mL, respectively.

Sixteen compounds including twelve previously undescribed sesquiterpenes were isolated from Salacia obovatilimba. Based on HRESIMS, IR, NMR and electronic circular dichroism (ECD) spectroscopic analysis, the previously undescribed compounds were characterized as twelve undescribed dihydro-β-agarofuran sesquiterpenoids (compounds 1-12). The structures of compounds 1 and 6 were confirmed by single-crystal X-ray diffraction. All compounds were assayed for their inhibitory effect on hSGLT2 in vitro, results suggested compounds 11 and 13 exhibited significant hSGLT2 inhibitory activity, with IC50 values of 11.9 and 9.45 nM, respectively. The probable binding potency were predicted through molecular docking by accurate models of protein-ligand complex.

Eighteen compounds including eleven previously undescribed diterpenes were isolated from the leaves of Croton mangelong. The structures were determined by HRESIMS, IR, NMR, X-ray diffraction and ECD spectroscopic analysis. All isolates were assayed for their anti-hyperglycemic activities in insulin resistance (IR) 3T3-L1 adipocytes, and compound 4 was tested for its anti-diabetic activity in vivo. Results suggested compound 4 could effectively reduce blood glucose level in diabetic SD rats in a dose of 30 mg/kg.

A new xanthone, allanxanthone F (1), and 10 known compounds were isolated from the ethanol extract of Garcinia bracteata. The structure of compound 1 was elucidated based on spectroscopic methods (UV, IR, HR-ESI-MS, and NMR). In addition, compounds 1-9 were assessed for their anti-inflammatory activities based on the expression of nitric oxide (NO) levels on lipopolysaccharide (LPS)-induced RAW264.7 macrophages, and compounds 1-3, 4 and 6-9 suggested potential anti-inflammatory activities.

Cyclin-dependent kinases (CDKs) are hyperactive in many cancers and have served as cancer therapeutic targets for decades. Palbociclib (Palb) is the first approved CDK4/6 inhibitor to treat hormone receptor (HR)-positive, HER2-negative advanced breast cancer. Acquired drug resistance is one obstacle of Palb be utilized in other cancer. CDK2 compensation of CDK4/6 loss is one of the causes that cancer cells are resistant to Palb. Hence, targeting multiple CDKs could be a novel strategy to prevent the drug resistance of cancer cells and expand the application of Palb in other cancer. In this study, we initially indicated Polyphyllin I (PPI) significantly inhibits non-small lung cancer cell (NSCLC) proliferation, promotes cell apoptosis in vitro and in vivo. Mechanistically, PPI can inhibit Rb through the p21/CDK2/Rb signaling pathway in NSCLC. A combination of PPI and Palb exerts a significant synergistic anti-cancer ability on NSCLC. Of note, PPI can reverse Palb drug resistance. Herein, we first time demonstrated PPI can disturb CDK2 function through upregulation of p21. The PPI effect on CDK2 provides a choice for a chemotherapeutic strategy for the elimination of NSCLC. Our study highlighted the clinical significance of simultaneously blocking of CDK2 and CDK4/6 for NSCLC treatment.

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

Fifteen compounds including nine new diterpenes were isolated from the roots of Croton yunnanensis. By HRESIMS, NMR, ECD data, and X-ray diffraction analysis, the new compounds were characterized as eight neo-clerodane diterpenes (compounds 1-8) and one 15,16-dinor-ent-pimarane diterpene (9). All diterpenes were assayed for their hypoglycemic activities. Compounds 1-4, 6, 7, and 10 promoted glucose uptake activity in insulin-resistant 3T3-L1 adipocytes. Compounds 1 and 6 showed insulin sensitizing activity, potentiating conspicuously their glucose uptake activity at a concentration of 20 μM when treated synergistically with low-concentration insulin at 1 nM.

目的 比较橘核乙醇提取物、乙酸乙酯部位、水部位、水相用50％、85％乙醇洗脱部位的抗炎、镇痛活性.方法 采用脂多糖(LPS)诱导的小鼠巨噬细胞(RAW264.7)一氧化氮(NO)释放模型、二甲苯致小鼠耳廓肿胀及棉球肉芽肿模型,研究橘核提取物的抗炎活性.采用热板法、醋酸扭体法及电子痛压法,研究其镇痛作用.结果 与模型组相比,除50％乙醇洗脱部位外,其余各部位均显示出NO抑制活性(P＜0.05、P＜0.01);橘核的乙酸乙酯部位、50％乙醇洗脱部位的高、低剂量组能显著抑制二甲苯所致小鼠耳廓肿胀(P＜0.01),明显减少肉芽肿重量,提升血清中白细胞介素-2(IL-2)的浓度(P＜0.05、P＜0.01);85％乙醇洗脱部位的高、低剂量组也明显提升血清中IL-2浓度,抑制肉芽组织增生(P＜0.05).橘核的水相及其50％乙醇洗脱部位的高、低剂量组能明显延长热板所致小鼠的痛阈值,减少醋酸所致小鼠扭体反应次数,显著提高小鼠达到疼痛阈时的压力,与模型组比较差异有显著统计学意义(P＜0.01).结论 橘核的不同部位均具有抗炎作用,乙酸乙酯部位及水相以50％乙醇洗脱部位的体内抗炎作用较强;橘核的水部位可能为镇痛的主要活性部位,其中以50％乙醇洗脱部位发挥较强镇痛作用.

目的 研究雪上一枝蒿多糖组分XP-10 在原发性肝癌肺转移的抑制效应及其作用机理,为雪上一枝蒿多糖肿瘤免疫疗法及南药植物资源合理开发提供科学依据.方法 构建H22 肝癌肺转移小鼠动物模型,随机分为病理模型组、XP-10 低剂量给药组(250 mg/kg)和XP-10 高剂量给药组(500 mg/kg),药物干预后,计数肝癌肺内转移灶数目;MTT法检测荷瘤小鼠脾淋巴细胞的活力;流式细胞术检测脾淋巴细胞Th1(CD4+IFN-γ+)、Th17(CD4+IL-17A+)和Treg细胞(CD4+Foxp3+)表达水平.结果 XP-10 药物干预显著抑制肺转移灶数目(P＜0.01),提高荷瘤小鼠淋巴细胞的活力(P＜0.01);XP-10 低剂量(250 mg/kg)药物干预显著下调荷瘤小鼠CD4+Foxp3+调节性T细胞比例(P＜0.05),XP-10 药物干预对肝癌肺转移荷瘤小鼠淋巴细胞Th17 细胞比例和Th1 细胞无显著影响(P＞0.05).结论 雪上一枝蒿多糖组分XP-10 能够显著抑制原发性肝癌的肺转移,其抑制效应部分通过下调与机体免疫反应负性调节机制相关的Treg细胞,并促进T淋巴细胞增殖、增强抗肿瘤免疫的机制而实现.为中药雪上一枝蒿的多糖抗肿瘤免疫临床疗法提供了一定的现代科学依据.

目的 研究雪上一枝蒿多糖组分XP-10 体内外免疫调节作用及初步效应机制,为雪上一枝蒿多糖的应用和合理开发提供科学依据.方法 构建体外小鼠脾淋巴细胞模型,分别采用ConA、LPS和anti-CD3 抗体诱导脾淋巴细胞增殖,MTT法检测各组脾淋巴细胞的活力;ELISA法检测ConA诱导的脾淋巴细胞培养上清中细胞因子IFN-γ、IL-2 和IL-6 水平.构建环磷酰胺诱导的体内免疫抑制模型,测定XP-10 对模型小鼠免疫器官指数的影响;MTT法检测各组脾淋巴细胞的活力;流式细胞术检测各组脾淋巴细胞Treg细胞(CD4+Foxp3+)表达水平.结果 XP-10 具有丝裂原活性,显著促进ConA和LPS诱导淋巴细胞增殖,且呈现显著的浓度依赖性关系(P＜0.05).XP-10 在 250 μg/mL浓度下可促进anti-CD3 抗体诱导的淋巴细胞增殖.XP-10 药物干预显著促进细胞因子IFN-γ(P＜0.05)和IL-6(P＜0.05 或P＜0.01)水平,然而对IL-2 的产生无明显的影响(P＞0.01).XP-10 在 125 mg/kg剂量下能显著提高免疫抑制模型脾指数和胸腺指数(P＜0.05),提高免疫抑制模型小鼠脾淋巴细胞的增殖功能,下调Treg细胞(CD4+Foxp3+T细胞)比例(P＜0.05).结论 中药雪上一枝蒿多糖组分XP-10 在体内外均具有较好的免疫调节活性,其机制可能与促进细胞因子IFN-γ分泌和下调Treg细胞表达有关,其可能在抗肿瘤免疫辅助用药方面具有一定的应用前景.

ABSTRACTHepatocellular carcinoma (HCC) is a frequently occurring malignant gastrointestinal cancer. The 5-year survival rate of HCC is still below 8%, and thus, identifying more effective therapeutic methods is needed. Here, we evaluated the effects of Stigmast-4-en-6β-ol-3-one (S463) on the viability and colony formation of liver cancer cells. S463 treatment decreased the viability and induced apoptosis and ferroptosis in liver cancer cells, and also increased cellular malondialdehyde (MDA) and lipid peroxidation levels. In S463 treated cells, the expression level of Bax was increased, and the expression level of GPX4 was reduced, and the cleavage of PARP was improved. We also found that S463 treatment downregulated E2F1 and upregulated p53 at both the mRNA and protein levels. Importantly, rescue experiments revealed that overexpression of E2F1 partially restored S463-induced Bax and p53 upregulation and GPX4 downregulation and counteracted the S463-induced decrease in cell viability and colony formation and the S463-induced increase in MDA and lipid peroxidation levels. Our findings suggest that S463 significantly inhibits viability and colony formation and induces apoptosis and ferroptosis in liver cancer cells via E2F1.

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

目的 研究荔枝Litchchinensis核正丁醇部位的化学成分及生物活性.方法 利用硅胶、D101大孔树脂、MCI、ODS、Sephadex LH-20及半制备型高效液相等色谱技术进行分离纯化,根据理化性质和波谱数据鉴定化合物结构;采用Griess法测定化合物对脂多糖诱导的小鼠巨噬细胞RAW264.7产生一氧化氮(NO)的抑制活性;采用1,1-二苯基-2-三硝基苯肼(1,1-diphenyl-2-trinitrophenylhydrazine,DPPH)方法测定化合物的体外抗氧化活性.结果 从荔枝核正丁醇部位分离得到15个化合物,分别鉴定为柚皮素-7-O-(2",6"-二-O-α-L-鼠李糖基)-β-D-吡喃葡萄糖苷(1)、litchiosideD(2)、异鼠李素-3-O-(2",6"-二-O-α-L-鼠李糖基)-β-D-吡喃葡萄糖苷(3)、山柰酚-3-O-(6-O-啡酰基)-β-葡萄糖基-(1→3)-α-鼠李糖-7-O-α-鼠李糖苷(4)、5'-O-β-D-葡萄糖苷茉莉酮酸甲酯(5)、5'-O-β-D-葡萄糖苷茉莉酮酸丁酯(6)、5'-O-β-D-葡萄糖苷茉莉酮酸(7)、松脂素-4-O-β-D-葡萄糖苷(8)、表松脂素-4-O-β-D-葡萄糖苷(9)、pyrafortunosideA(10)、苯乙基芸香苷(11)、苯甲醇-O-β-D-吡喃葡萄糖苷(12)、methyl-1-(β-D-ribofuranosyl)-imidazolin-2-one-4-carboxylate(13)、莽草酸甲酯(14)和莽草酸(15).体外抗炎活性结果表明,化合物13能明显抑制脂多糖诱导的RAW264.7细胞NO释放,其半数抑制浓度(median inhibition concentration,IC50)为(27.9+2.8)μmol/L;化合物15具有一定的抑制活性,其IC50为(62.4+9.7)μmol/L.体外抗氧化活性结果表明,化合物4对DPPH自由基具有一定的清除活性,其IC50为(109.8+1.5)μmol/L.结论 化合物1、3～6、9～15为首次从荔枝核中分离得到.化合物13有较强体外抗炎活性,化合物15有一定的体外抗炎活性.化合物4具有一定的体外抗氧化活性.关键词:荔枝核;苷类;抗炎活性;抗氧化活性;山柰酚-3-O-(6-O-啡酰基)-β-葡萄糖基-(1→3)-α-鼠李糖-7-O-α-鼠李糖苷;表松脂素-4-O-β-D-葡萄糖苷;莽草酸

目的 对益气通络方煎煮过程中是否有新的化合物产生进行分析,并对全方的急性毒性进行研究.方法 通过高效液相色谱法(HPLC),将益气通络方混提的样品和单独煎煮的地桃花、鸡根、滇鸡血藤混合后的溶液进行对比,分析成分差异;通过LD50和最大给药量实验检查益气通络方的急性毒性.结果 1.分别提取地桃花、鸡根、滇鸡血藤3味药单独进行HPLC检测,流速1.0 mL/min,柱温30℃,分别以210 nm、254 nm、280 nm和320 nm波长进行检测,254 nm的吸收图谱最理想;2.将地桃花、鸡根、滇鸡血藤3味药水提液按比例混匀,在254 nm波长下与整方混提的HPLC吸收图谱进行比较,2个谱图的吸收峰紫外光谱对应的位置和形态基本一致,除少数吸收峰的幅度略有差异外,波形的拟合度较高;3.检测益气通络方LD50,8个浓度梯度均未见动物死亡和明显的毒性反应;4.益气通络方溶解至最大浓度,一次性给予最大灌胃量,折合给药量为246.9 g/kg,仍未见到动物死亡和明显毒性反应.结论 1.益气通络方和地桃花、鸡根、滇鸡血藤单药煎煮后混合相比,并未出现明显的成分改变;2.在急性毒性动物实验中,益气通络方未见明显的不良反应.

Thirty-five tigliane diterpenoids and two ent-kaurane diterpenoids were isolated from the leaves of Croton damayeshu, and, among them, compounds 1-10 were characterized as new tigliane diterpenoids. The structures of compounds 1-10 were determined by analysis of their HRESIMS, NMR, and ECD data and by chemical methods. The isolates were assayed for their larvicidal, antifungal, and α-glucosidase inhibitory activities, and compounds 8-10 were found to possess larvicidal activities against Plutella xylostella with LC50 values of 0.19, 0.16, and 0.26 μM, respectively, comparable to the LC50 of 0.14 μM for the positive control, flubendiamide.

Further investigation on the roots of Aconitum weixiense led to the isolation of two new bis-diterpenoid alkaloids, named as weisaconitines E and F (1-2), which were elucidated by IR, HR-ESI-MS, 1D- and 2D-NMR analyses. Their structures are characterized as denudatine-atisine-type bis-diterpenoid alkaloids.

Fifteen compounds, including five new phorbol esters (1-5) and ten known metabolites were isolated from the leaves of Croton tiglium. The structures of new compounds 1-5 were determined by comprehensive analysis of the HRESIMS, IR, 1D and 2D NMR spectral data. The isolates were assayed for their larvicidal and alpha-glucosidase inhibitory activity; results suggested the new compounds 1-4 possessed significant insecticidal activity, inhibiting the Plutella xylostella with LC50 values ranging from 0.081 to 0.114 mu g/mL, while the sesquiterpenoids 11 and 15 showed noticeable alpha-glucosidase inhibitory activity with IC50 values of 11.27 and 8.13 mu M, respectively.

目的:研究卫矛属植物大理卫矛Euonymus amygdalifolius的化学成分.方法:大理卫矛干燥地上部分用95％乙醇提取,浓缩后浸膏应用硅胶、Sephadex LH-20和半制备HPLC色谱进行分离纯化,根据化合物的理化常数和波谱数据(ESI-MS、1 H-NMR、13 C-NMR)鉴定结构.结果:从大理卫矛中分离得到12个化合物,分别鉴定为羽扇豆醇(1,lupin),十六烷酸甘油酯(2,hexadecanoic acidglyceride),十六烷酸(3,hexadecanoic acid),柚皮素(4,naringenin),木犀草素(5,luteolin),山柰酚(6,kaempferol),槲皮苷(7,quercitrin),芦丁(8,rutin),24,24-Dimethyl-reissant-7(8)-25-dien-3α-ol(9),卫矛醇(10,euonyl),1-O-β-D葡萄糖-N-正二十二碳酰基-正十六碳-4,10(E,E)-二烯鞘胺醇苷(11,1-O-β-D-glucose-N-docosanoyl-hexadecanoic-4,10(E,E)-diensphingosine glycoside),羽扇豆醇乙酸酯(12,lupeol acetate).结论:化合物结构类型涉及三萜、黄酮、酰胺等,化合物1～12均为首次从大理卫矛中分离得到,化合物11首次从卫矛属中分离得到,研究结果丰富了对大理卫矛物质基础认识.

目的 探讨哥纳香属植物的药理作用.方法 结合文献,总结国内外关于哥纳香属植物的药理作用及作用机制的研究现状.结果 哥纳香属植物具有抗氧化、抗骨质疏松、抑制血小板聚集、抗病毒、抗菌、杀虫等药理作用.结论 值得对哥纳香属植物的药用资源作进一步的研究与开发.