赤芝道地药材形成源流考

目的 对赤芝道地药材形成进行本草考证和历史文献考实。方法 查阅历代本草文献结合现代研究,从基原、产地变迁、产地加工、质量评价等方面对赤芝道地药材形成进行考证。结果 古代赤芝以野生品为主,到南宋时期已有栽培品的记载,浙江、安徽及周边地区赤芝的栽培历史悠久,所产赤芝品质优良。结论 浙江、安徽为赤芝的道地产区,赤芝道地药材的形成与载培、采收、加工等技术的进步密切相关。     

基于CiteSpace的灵芝孢子粉研究知识图谱分析

目的 对灵芝孢子相关研究进行文献计量、可视化分析，探讨并综述其研究热点及发展趋势。方法 在中国知网、Pubmed和Web of Science数据库检索灵芝孢子粉相关的文献，并根据文献语言的不同分为中文与英文2个部分，应用CiteSpace对文献中的国家、机构、关键词和主题词、被引情况进行共现分析，绘制对应知识图谱、时间线视图，进而推断灵芝孢子粉的研究热点及趋势。对灵芝孢子主要研究热点、趋势、临床研究及物质基础等方面的研究进行总结。结果 共获得相关文献1 477篇，包括989篇中文文献、488篇英文文献，发文量均呈增涨趋势，且国家及机构共现分析表明发文的主要是中国与中国机构，研究热点领域为药理药效方面，主要以抗肿瘤、免疫调节、抗癫痫等药效研究为主。近5年新兴的灵芝孢子粉的研究集中在免疫检查点、肠道菌群等前沿领域。结论 灵芝孢子粉在抗肿瘤、免疫调节、抗癫痫等方面的药理作用研究广泛，具有良好的应用前景，但物质基础和质量控制研究较为薄弱，有待进一步深化。     

Ganoderin A,a novel 9,11-secosterol from Ganoderma lucidum spores oil

In this study, four sterols were isolated from the Ganoderma lucidum spores oil obtained via supercritical CO₂ extraction. Four chemical constituents were ganoderin A (1), chaxine B (2), ergosterol, (3) and stellasterol (4). All the separated ingredients were characterized using spectral data interpretation and by comparing with reported data. Noticeably, stellasterol and chaxine B were both firstly isolated from Ganoderma lucidum spores oil and ganoderin A was shown to bear an unprecedented skeleton.     

女贞子提取工艺的研究

目的 优化女贞子的最佳提取条件。方法 采用正交试验法设计实验,考察乙醇浓度、加醇量、提取时间和提取次数,通过齐墩果酸、特女贞苷含量测定及浸膏得率来确定最佳乙醇提取工艺;考察粉碎度对女贞子提取工艺的影响,比较女贞子提取液趁热过滤浓缩与静置24 h后过滤浓缩的结果差异,并比较女贞子醇提工艺和水提工艺的各项指标。结果 女贞子最佳提取工艺为加10倍量的70%乙醇,提取3次,每次1 h,提取液趁热过滤浓缩。结论 该优化提取工艺合理可行,更适合生产。     

灵芝三萜成分分析灵芝三萜成分分析

目的建立灵芝子实体、孢子粉、发酵菌丝体三萜成分的HPLC含量测定方法。方法以赤芝孢子酸A(ganosporeric acid A,1),赤芝酸A(lucidenic acid A,2),灵芝酸B(ganoderic acid B,3)和灵芝酸C(ganoderic acid C,4)为对照品;色谱柱:反相C₁₈;流动相:乙腈-水(37∶63);流速:1.0 mL·min^-1;检测波长:UV 254 nm。结果进样量在0.2～1 μg有良好的线性关系,(1),(2),(3)和(4)的加样回收率分别为100.9%,101.2%,101.3%和101.7%。结论本法快速、简便、灵敏和分离度好,适用于灵芝子实体、孢子粉、发酵菌丝体及相关制剂的三萜类物质检查和含量测定。     

In vivo antitumor effects of bitter principles from the antlered form of fruiting bodies of Ganoderma lucidum

Two triterpene fractions and a single ganoderma alcohol obtained from an antlered form of the fruiting bodies of Ganoderma lucidum were examined for their antitumor effects on the growth of inoculated mouse Lewis lung carcinoma in mice by intraperitoneal administration. The ganoderma alcohol fraction significantly suppressed the tumor growth at doses of 50 and 100 mg/kg in the treatment period, and even after the administration, showing antitumor activity with a T/C value of 70.6% at a dose of 100 mg/kg. On the other hand, no obvious activity was shown at each dose in the ganoderma-acid-fraction-treated groups. Furthermore, ganoderiol F, which exhibited the strongest cytotoxicity against four tumor cell lines among five ganoderma alcohols examined, remarkably inhibited the tumor growth, accounting for 63.7% and 78.7% of control group at a dose of 5 mg/kg, 54.1% and 63.0% at a dose of 10 mg/kg, and 47.7% and 53.9% at a dose of 20 mg/kg in and after the administration period, respectively, in a dose-dependent manner. These results suggest that the antitumor effects of bitter principles in G. lucidum are mainly due to ganoderma alcohols.     

灵芝孢子油对大鼠肝纤维化的干预作用

目的 探讨灵芝孢子油对大鼠肝纤维化的影响。方法 选择40% CCl₄皮下注射诱导SD大鼠肝纤维化形成,造模同时用低、中、高剂量（0.33,0.67,2.00 g·kg^-1）灵芝孢子油灌胃干预（每组10只）,观察血浆谷草转氨酶（AST）、谷丙转氨酶（ALT）、丙二醛（MDA）、透明质酸（HA）和肝组织MDA、羟脯氨酸（HyP）等的变化,肝组织HE和Masson染色观察病理变化。结果 灵芝孢子油能显著降低CCl₄所致的肝纤维化大鼠血浆AST、ALT、MDA、HA水平（P<0.05）,降低肝组织HyP、MDA含量（P<0.05）,肝脏病理显示纤维化程度明显减轻（P<0.05）。结论 灵芝孢子油对CCl₄诱导的大鼠肝纤维化具有保护作用。     

灵芝孢子油、破壁灵芝孢子粉及灵芝孢子提取物对小鼠急性胃溃疡的保护作用

目的 探讨灵芝孢子油、破壁灵芝孢子粉及灵芝孢子提取物对小鼠急性胃溃疡的影响。方法 雄性ICR小鼠随机分为12组：对照组,模型组,奥美拉唑（阳性药,4 mg·kg^-1）组,灵芝孢子提取物低、中、高剂量（0.2、0.4、0.8 g·kg^-1）组,破壁灵芝孢子粉低、中、高剂量（0.6、1.2、2.4 g·kg^-1）组,灵芝孢子油低、中、高剂量（0.2、0.4、0.8 g·kg^-1）组,每组20只。ig给药,每天1次,对照组和模型组给予等体积的生理盐水。连续给药7 d后,禁食12 h,除对照组外,每组随机选取10只小鼠ig无水乙醇（10 mL·kg^-1）建立急性胃溃疡模型,1.5 h后取材;每组余下10只小鼠ig吲哚美辛（40 mg·kg^-1）建立急性胃溃疡模型,3 h后取材。观察小鼠的一般状况、胃出血和溃疡情况,进行胃损伤评分,计算损伤抑制率和损伤发生率。结果 各组小鼠给药过程中无异常。小鼠给予无水乙醇后,模型组和奥美拉唑组10 min后开始出现行动变缓,肢体活动不协调,呼吸加深、频率减慢等症状,而给予灵芝孢子提取物、破壁灵芝孢子粉和灵芝孢子油的小鼠在30 min后才陆续出现症状;给予吲哚美辛的小鼠自主活动减少,各组之间无差别;对照组小鼠行为活动如常。与对照组比较,小鼠经无水乙醇、吲哚美辛ig导致非常明显的胃溃疡,胃损伤评分显著升高（P<0.01）,损伤发生率为100%;与模型组比较,预防性给予灵芝孢子提取物、破壁灵芝孢子粉、灵芝孢子油可明显降低胃出血或溃疡等胃黏膜损伤,其中灵芝孢子提取物高剂量组、破壁灵芝孢子粉组、灵芝孢子油组的胃损伤评分显著降低（P<0.01）,损伤抑制率显著提高（P<0.01）,损伤发生率明显降低。结论 灵芝孢子油、破壁灵芝孢子粉及灵芝孢子提取物能有效抑制小鼠急性胃溃疡的发生,灵芝孢子油效果最佳,破壁灵芝孢子粉次之,并且对于无水乙醇导致的急性胃溃疡抑制作用尤为显著。     

基于结肠癌HCT116细胞三维培养模型的灵芝组分抗肿瘤活性研究

目的 基于结肠癌HCT116细胞的二维(2D)和三维(3D)培养模型研究灵芝组分(Ganoderma components,Gc)的抗肿瘤作用。方法 采用UPLC-Q-TOF-MS鉴定3种Gc的化学组成;以Matrigel基质胶为基质材料建立体外HCT116细胞3D培养模型,评价Gc1、Gc2、Gc3和5-氟尿嘧啶(5-fluorouracil,5-FU)对2D和3D培养的HCT116细胞增殖的影响,并在HCT116细胞3D培养模型中分析Gc3对周期、凋亡、耐药、脂代谢及5-FU抗肿瘤活性的影响;采用CCK-8法检测细胞活力;Real-time PCR检测细胞mRNA表达水平;Western blotting检测细胞蛋白表达水平;采用HPLC检测细胞内5-FU含量。结果 从Gc1、Gc2和Gc3中分别鉴定出76,69和17个化合物;与2D培养相比,3D培养的HCT116细胞增殖率更低,周期促进蛋白CDK2、CDK4、CDK6及脂肪酸合成蛋白FASN、SREBP1的表达显著下调,周期抑制蛋白p21和p27、脂滴分解蛋白ATGL及药物抵抗基因ITGB1、CDH1、ABCB1、ABCC1 m...     

Preparation,characterisation and anti‐tumour activity of Ganoderma lucidum polysaccharide nanoparticles

Objectives The aim was to prepare novel Ganoderma lucidum polysaccharide nanoparticles and to evaluate the physicochemical properties and anti‐tumour activity in in‐vitro cytotoxicity studies using HepG2, HeLa and A549 cancer cell lines, and growth promotion effects on mouse spleen cells. Methods Chitosan nanoparticles loaded with G. lucidum polysaccharide were prepared using the ion‐revulsion method. The diameter distribution of the particles and the surface charge were measured using a zetasizer analyser. The entrapment efficiency and drug loading capacity were examined by the diethylaminoethanol weak anion exchange method. The cytotoxic effects of nanoparticles on tumour cells and the growth promotion effects on mouse spleen cells were tested using the MTT assay. Key findings Nanoparticles loaded with G. lucidum polysaccharide at 6 μg/ml and chitosan/sodium tripolyphosphate (mass) ratio of 5.5 had significantly greater cytotoxic effects on tumour cells and growth promotion effects on mouse spleen cells than empty nanoparticles. Conclusions G. lucidum polysaccharide nanoparticles showed significant anti‐tumour efficacy, having both cytotoxic effects on tumour cells and growth promotion effects on spleen cells, making it a promising candidate in the clinical setting.     

中药女贞子水溶性化学成分的研究

中药女贞子水溶性化学成分的研究石力夫，王鹏，陈海生，董建萍（上海第二军医大学附属长海医院２００４３３）女贞子（ＬｇｕｓｔｒｕｍｌｕｃｉｄｕｍＡｉｔ）为常用中药，有扶正固本、滋补肝肾、明目乌发之功效［１］。临床主要用于强腰膝、壮筋骨、乌须发、治阴虚内热...     

茅莓提取物及有效部位的药理作用研究进展

茅莓Rubus parvifolius为蔷薇科悬钩子属落叶小灌木,其提取物及有效部位具有抗肿瘤、保护神经、保护肝损伤等药理作用。抗肿瘤是其研究热点,在体内外实验中,茅莓提取物对人恶性黑色素瘤、白血病、肝癌均表现出明显的抗肿瘤作用,可显著抑制肿瘤细胞生长、侵袭和迁移,以及诱导细胞凋亡,其抗肿瘤的主要有效部位为茅莓总皂苷。茅莓提取物对脑缺血-再灌注损伤也有神经保护作用,作用机制为增加Bcl-2表达和降低Bax表达,主要有效部位为茅莓总皂苷。茅莓提取物的抗氧化能力与清除羟自由基、超氧负离子、有机自由基及抑制丙二醛等有关,主要有效部位为茅莓总黄酮。茅莓提取物对肝脏损伤也有保护作用,与清除自由基活性相关,主要有效部位为酚类化合物。茅莓提取物及有效部位的其他药理作用还有抗炎、抗骨吸收、抗菌、抗疲劳等。综述了茅莓提取物及有效部位的药理作用及研究现状,以期为茅莓的进一步研究及新药开发提供参考。     

Regulation of osteoclastogenesis by ganoderic acid DM isolated from Ganoderma lucidum

The preventative effects of the ethanol extracts of Ganoderma lucidum against the ovariectomized (Ovx)-induced deterioration of bone density in 11-week-old female Sprague Dawley (SD) rats were investigated. The results showed that the G. lucidum-treated Ovx rats showed improved bone density compared with the Ovx rats. We studied the effects of G. lucidum on osteoclastic differentiation using bone marrow cells and RAW 264 cell D-clone (RAW-D). Differentiation, in response to receptor activator of NF-κB ligand (RANKL) and a tumor necrosis factor α (TNF-α), was inhibited by the ethanol extracts of G. lucidum and ganoderic acid DM which was isolated as one of the active compounds by bioassay-guided fractionation. Ganoderic acid DM especially suppresses the expression of c-Fos and nuclear factor of activated T cells c1 (NFATc1). This suppression leads to the inhibition of dendritic cell-specific transmembrane protein (DC-STAMP) expression and reduces osteoclast fusion.     

冬凌草的化学成分研究

目的 研究冬凌草的化学成分。方法 利用硅胶柱色谱、中压液相色谱、高效液相色谱等色谱技术对冬凌草甲醇提取物进行分离纯化,通过波谱数据分析,鉴定了化合物的结构,利用噻唑蓝(MTT)法测试化合物抗肿瘤活性。结果 从冬凌草中共分离鉴定6个化合物,分别为：rabdosianin A（1）、parvifoline G（2）、rabdoternin C（3）、betulin（4）、betulinic acid（5）、古柯二醇（6）。结论 化合物6为首次从香茶菜属中分离得到,化合物1、2、4、5为首次从冬凌草中分离得到。化合物5对人白血病细胞K562有较强的抑制作用,IC₅₀值为1.45 µmol·L^-1。     

The beneficial effects of Ganoderma lucidum on cardiovascular and metabolic disease risk

ContextVarious herbal medicines are thought to be useful in the management of cardiometabolic disease and its risk factors. Ganoderma lucidum (Curtis) P. Karst. (Ganodermataceae), also known as Lingzhi, has received considerable attention for various indications, including some related to the prevention and treatment of cardiovascular and metabolic disease by ameliorating major cardiovascular risk factors.ObjectiveThis review focuses on the major studies of the whole plant, plant extract, and specific active compounds isolated from G. lucidum in relation to the main risk factors for cardiometabolic disease.MethodsReferences from major databases including PubMed, Web of Science, and Google Scholar were compiled. The search terms used were Ganoderma lucidum, Lingzhi, Reishi, cardiovascular, hypoglycaemic, diabetes, dyslipidaemia, antihypertensive, and anti-inflammatory.ResultsA number of in vitro studies and in vivo animal models have found that G. lucidum possesses antioxidative, antihypertensive, hypoglycaemic, lipid-lowering, and anti-inflammatory properties, but the health benefits in clinical trials are inconsistent. Among these potential health benefits, the most compelling evidence thus far is its hypoglycaemic effects in patients with type 2 diabetes or hyperglycaemia.ConclusionsThe inconsistent evidence about the potential health benefits of G. lucidum is possibly because of the use of different Ganoderma formulations and different study populations. Further large controlled clinical studies are therefore needed to clarify the potential benefits of G. lucidum preparations standardised by known active components in the prevention and treatment of cardiometabolic disease.     

基于网络药理学和分子对接探讨冬虫夏草抗肿瘤的作用机制

目的 基于网络药理学方法和分子对接技术探究冬虫夏草抗肿瘤的作用机制。方法 利用TCMSP、CNKI、PubMed、Drugbank、Stitch和Swiss target prediction等平台检索冬虫夏草的化学成分和作用靶点;通过GeneCards、OMIM等数据库筛选肿瘤相关基因,运用Cytoscape 3.7.2构建冬虫夏草活性成分-靶点网络,通过String数据库对关键靶点构建网络互作(PPI)网络,并进行基因本体(GO)基因和京都基因和基因组百科全书(KEGG)通路富集分析,最后利用AutoDock Vina软件和Pymol软件对药物有效活性成分和关键靶点进行分子对接验证。结果 共得到冬虫夏草22个化合物,86个抗肿瘤共同靶点,主要包括环加氧酶(PTGS)2、丝裂原活化蛋白激酶3(MAPK3)、过氧化物酶体增生激活受体γ(PPARG)、胱天蛋白酶3(CASP3)、JUN基因等关键靶点。GO分析与KEGG通路结果显示,冬虫夏草抗肿瘤涉及到多种生物学过程以及PPAR、花生四烯代谢、5-羟色胺信号通路等多种信号通路。将关键化合物和靶点进行分子对接,提示冬虫夏草抗肿瘤可能的前5个主要活性成分11,14-二十碳二烯酸、花生四烯酸、黄豆黄素、胆甾醇和豆甾醇与关键靶点PTGS2、PTGS1、PGR、HMGCR和CNR1均能自发结合。结论 初步探讨了冬虫夏草抗肿瘤的主要活性成分、相关靶点及相关通路,发现冬虫夏草可以通过多成分、多靶点、多通路抗肿瘤,为后期实验验证提供了参考依据。     

畲药白山毛桃根抗肿瘤作用及活性成分研究进展

目的 综述畲药白山毛桃根抗肿瘤作用及活性成分研究进展,为白山毛桃根的临床应用和进一步开发提供参考依据。方法 检索1980—2018年以来国内外有关白山毛桃根的抗肿瘤作用及活性成分的研究论文,总结分析其抗肿瘤作用、抗肿瘤机制及活性成分。结果 白山毛桃根具有治疗胃癌、肝癌、黑色素瘤等多种抗肿瘤作用,其作用机制包括诱导细胞凋亡和坏死、免疫调节、阻滞细胞周期等,其抗肿瘤活性成分主要为乌苏酸类化合物。结论 白山毛桃根具有良好的抗肿瘤作用,临床应用价值较高,尚需加强其循证医学数据、抗肿瘤活性成分和质量标准的深入研究。     

Chemical studies on monoterpenoid indole alkaloids from medicinal plant resources <Emphasis Type="Italic">Gelsemium</Emphasis> and <Emphasis Type="Italic">Ophiorrhiza</Emphasis>

We have proved that the plant of origin of “Yakatsu”, one of the ancient medicines stored in Shosoin Repository, is Gelsemium elegans (Loganiaceae). Exhaustive investigation of the alkaloids in this plant as well as its closely related plant, G. sempervirens, resulted in the isolation of more than 50 compounds, including new gelsedine-, sarpagine-, and yohimbane-type alkaloids. Pharmacological study of representative and new Gelsemium alkaloids revealed that the gelsedine-type alkaloids exhibit potent cytotoxic activity against the A431 human epidermoid carcinoma cell line. It was found that Ophiorrhiza pumila (Rubiaceae) produces a remarkable anti-tumor alkaloid, camptothecin, and its related alkaloids, including new compounds that might be the biogenetic precursors of camptothecin. Chemical investigation of callus cultures, regenerated plants, and hairy roots of O. pumila revealed that the regenerated plants and the hairy roots produce almost the same alkaloids, including camptothecin, as do the wild-type plants.     

女贞子及其活性成分促生长增体质作用的研究进展

女贞子及其活性成分齐墩果酸、熊果酸、红景天苷具有促进骨、肌肉生长和体质量增长,提高机体防御功能的作用。其促生长、增体质机制可能与胰岛素样作用、雌激素样作用以及促进细胞分化有关,对于儿童生长缓慢和消耗性疾病具有开发潜力。临床上可以考虑将女贞子及其活性成分试用于促进儿童生长发育、重症患者和手术患者康复期以及消耗性疾病患者的体质恢复。     

枸杞子及其有效成分的药理作用研究进展

枸杞子Lycium barbarum是食药同源中药材,具有滋阴兴阳、止消渴、补劳伤的功效,富含枸杞多糖、枸杞总黄酮、类胡萝卜素和氨基酸等多种有效成分。现代药理学的研究显示,枸杞子及其活性成分具有抗肿瘤、调节血糖血脂、保护视力、抗抑郁与焦虑、防治神经系统疾病、抗炎抑菌、抗氧化、保护肝肺肾等作用。对枸杞子及其有效成分的药理作用进行总结和归纳,以期为其进一步应用开发及新药研究提供依据。