The genus Abrus Adans. (Fabaceae), widely distributed in tropical and subtropical regions, includes four medicinally important species in China with significant therapeutic potential. Notably, Abrus precatorius L. has been traditionally used to treat headaches, wind-phlegm disorders, and carbuncles. Abrus cantoniensis Hance and Abrus mollis Hance are valued in ethnomedicine as hepatoprotective agents, whereas Abrus pulchellus Wall. ex Thwaites shows confirmed medicinal properties. Beyond their therapeutic applications, Abrus species are valued as nutraceutical resources, traditionally prepared as beverages, teas, or functional soups in dietotherapy. However, their widespread utilization is constrained by the presence of toxic compounds such as abrin and pulchellin. Phytochemical analyses have identified numerous bioactive constituents in these plants, including flavonoids, alkaloids, triterpenoid saponins, organic acids, amino acids, and aliphatic compounds. These compounds exhibit multifaceted pharmacological effects, including antioxidant, anti-inflammatory, antiparasitic, antimicrobial, antitumor, and hepatoprotective effects. This review systematically examines the traditional uses, nutritional value, phytochemical composition, pharmacological properties, and toxicity profiles of medicinal Abrus species in China, providing up-to-date information on their therapeutic potential.
Phenylnaphthalene-type lignans have been recognized as the major anti-inflammatory constituents in V. negundo seeds, among which vitedoamine A (VA) was the first discovered lignan alkaloid bearing a γ-lactam. However, the protective effects and specific target of VA against rheumatoid arthritis (RA) have not been explored yet. Herein, our study revealed that VA could inhibit the transcriptional activity of NF-κB, and suppress the production of NO and reduce the expressions of inflammatory cytokines (IL-1β, IL-6, and TNF-α) in several inflammatory cell models, mainly via inhibiting the phosphorylation of IKKα/β and p65, and prevented the degradation of IκBα, thus restraining NF-κB activation. Meanwhile, VA considerably down-regulated the phosphorylation of IKKα/β and p65, and inhibited the degradation of IκBα in RANKL-induced osteoclasts formation and differentiation, suggesting that VA may impede osteoclastogenesis and relieve joint damage in RA. Furthermore, VA interfered IKK/IκBα/NF-κB pathway and decreased the expressions of inflammatory cytokines in IL-1β stimulated fibroblast-like synoviocytes (FLSs), suggesting that VA possessed promising in vitro anti-RA capacity, probably by direct targeting IKKβ and inhibiting its activity (IC50 value: 39 μM). In addition, molecular docking displayed that VA could bind with residues Cys99 and Asp103 in IKKβ via hydrogen bonds, thus preventing ATP from binding with IKKβ to inhibit the activity of IKKβ. Taken together, VA directly targets IKKβ and significantly inhibits the IKK/IκBα/NF-κB pathway, thus inhibiting inflammatory responses in FLSs and mitigating joint damage related to osteoclastogenesis, displaying great potential in treating RA.
Ethnopharmacological relevance: The herb of Abrus cantoniensis Hance (AC) is an important Traditional Chinese Medicine (TCM) and is also used as an herbal tea with hepatoprotective action. Soyasaponin Bb is one of the pharmacodynamic substances of AC for the herb's effective pharmacological activity. This study aims to investigate the anti-fibrotic and hepatoprotective activities of soyasaponin Bb in vivo and in vitro experiments, mechanism by network pharmacology and quantification by HPLC. Materials and methods: High-performance liquid chromatography (HPLC) was applied to evaluate the quality of the herb and determine the contents of soyasaponin Bb from different sources and parts of the AC. In vivo experiments were conducted to induce an acute liver injury model by injecting CCl4 into mice, and an in vitro hepatic fibrosis model was established by cultivating LX-2 cells with TGF-beta(1). These models were used to explore the anti-fibrotic and hepatoprotective effects of soyasaponin Bb and its underlying mechanisms. In addition, the potential target genes corresponding to soyasaponin Bb were identified using the Swiss Target Prediction database through network pharmacology methods. Meanwhile, hepatic fibrosis targets were screened using the GeneCards, TTD, and OMIM disease databases. The STING database was used to construct the protein-protein interaction (PPI) network of soyasaponin Bb-hepatic fibrosis. The soyasaponin Bb-hepatic fibrosis disease target-pathway network was constructed using Cytoscape 3.9.1 software. Gene Ontology (GO) and the Kyoto Encyclopedia of Genes and Genomes (KEGG) analyses were performed to enrich and analyze the common targets of the drug and the disease, aiming to identify the potential targets and pathways involved in the anti-fibrotic and hepatoprotective effects of soyasaponin Bb. Results: The content of soyasaponin Bb varied across different sources, with the roots containing the highest concentration, up to 0.2480%. In vivo experiments showed that soyasaponin Bb had a protective effect against CCl4-induced acute liver injury, effectively inhibiting the increase in ALT and AST levels and slowing down the hepatocyte inflammatory damage caused by CCl4. Soyasaponin Bb also down-regulated MDA levels and up-regulated SOD levels, indicating a certain antioxidant capacity. In vitro cell experiments showed that soyasaponin Bb could effectively inhibit the proliferation of HSC-LX2 cells induced by TGF-beta(1) by regulating the TGF-beta(1)/alpha-SMA pathway, significantly down-regulate the protein expression of TGF-beta(1) and alpha-SMA, while also reducing the levels of inflammatory cytokines IL-6 and IL-1 beta. Further network pharmacology analysis suggested that soyasaponin Bb can exert anti-fibrosis activity by regulating the IBD signaling pathway, Th17 signaling pathway, Hepatitis B signaling pathway, and JAK-STAT signaling pathway. Conclusion: Soyasaponin Bb is primarily distributed in the root of AC, and it has a strong protective effect against CCl4-induced acute liver injury. It can reduce the level of inflammatory factors, relieve inflammation, and exert anti-fibrotic activity by regulating the TGF-beta(1)/alpha-SMA pathway. Its potential anti-hepatic fibrosis mechanism has been investigated through network pharmacology.
Flavonoid rutinosides, a group of bioactive compounds in Anoectochilus roxburghii, contribute greatly to the plant's beneficial effects on human health. However, the glycosylation mechanism of flavonoid rutinosides in A. roxburghii remains unclear. In this study, two efficient and selective glycosyltransferases, AUTG25 and AUTG23, involved in the biosynthesis of narcissoside, a major flavonoid rutinoside in A. roxburghii, were identified through transcriptome analysis and functional validation. AUTG25 could regioselectively catalyze 3-O-glucosylation of isorhamnetin to produce isorhamnetin 3-O-glucoside, while AUTG23 could further catalyze 6"-O-rhamnosylation to generate narcissoside. Both AUTG25 and AUTG23 exhibited high positional and sugar donor selectivities in the catalytic reaction. Homology modeling and site-directed mutagenesis showed that H20, E83, E385, and F143 in AUTG25 and E280, E89, D188, W327, D369, and Y191 in AUTG23 may be critical for their catalytic functions. Transient expression in Nicotiana benthamiana finally confirmed that AUTG25 possesses flavonol-3-O-glucosyltransferase activity and AUTG23 has flavonol-3-O-glucoside (1→6) rhamnosyltransferase activity. This study clarified and provided candidate UDP-dependent glycosyltransferase genes for narcissoside biosynthesis in A. roxburghii.
Methyleugenol is one of the main active constituents in the volatile oil of the traditional Chinese medicine Asari Radix et Rhizoma. It possesses various pharmacological effects such as analgesic, anesthetic, and anti-inflammatory properties. In biosynthesis, the initial precursor phenylalanine is finally converted into methyleugenol through a series of intermediate compounds including coniferyl acid, courmaryl acid, caffeic acid, ferulic acid/ferulic-CoA, coniferyl aldehyde, conferyl alcohol, cnfiferyl acetate, and eugenol/isoeugenol, which are produced through catalysis of a large number of enzymes. Eugenol O-methyltransferase(EOMT) is one of the key enzymes in the biosynthesis pathway, capable of methylating eugenol on the para-site hydroxyl group of the benzene ring, thereby generating methyleugenol. Here, an(iso)eugenol O-methyltransferase(IEMT) gene was cloned for the first time from Asarum siebo-ldii, holding an open reading frame that consisted of 1 113 bp and encoded a protein containing 370 amino acid residues. Bioinformatics analysis results showed that this protein was equipped with the characteristic structural domains of methyltransferases such as S-adenosylmethionine(SAM) binding sites and dimerization domains. The prokaryotic expression recombinant plasmid pET28a(+)-AsIEMT was constructed, and the candidate protein was induced and purified. In vitro enzyme assays confirmed that AsIEMT had dual functions. The enzyme could catalyze the production either of methyleugenol from eugenol or of methylisoeugenol from isoeugenol, although the latter was more prevalent. When isoeugenol was used as the substrate, the kinetics parameters K_m and V_(max) of catalytic reaction were(0.90±0.06) mmol·L~(-1) and(1.32±0.04)nmol·s~(-1)·mg~(-1), respectively. This study expanded our understandings of critical enzyme genes involved in phenylpropanoid metabolic pathways, and would facilitate the elucidation of quality formation mechanisms of the TCM Asari Radix et Rhizoma.
Chinese herbal tea is a beverage made of one or more kinds of traditional Chinese medicines or herbs, which is a branch of traditional Chinese medicine culture and a Chinese intangible cultural heritage. It has long been utilized for beneficial intentions in many national areas. Drinking herbal tea is popular in most provinces and cities in China, such as Guangdong, Guangxi, and Fujian, and it is also produced in Japan, the United States, Europe, Southeast Asia, and other regions, and gradually expand to the world. Herbal tea contains flavonoids, organic acids, alkaloids, polysaccharides and glycosides, etc., which supply herbal tea with anti-oxidation, anti-inflammatory, hypoglycemic, antiviral, antibacterial, anti-tumor, anti-aging and hepatoprotective effects. With the continuous expansion of the herbal tea market, the efficacy and safety of herbal tea has garnered great attention. This article reviews the research progress of chemical composition, pharmacological activity, and security of herbal tea in China.
目的 研究3株从紫苏中分离得到的内生真菌次生代谢产物抗肿瘤活性.方法 取处于指数生长期的5种人肿瘤细胞(人肝癌细胞株HepG2、人乳腺癌细胞株MCF-7、人肺腺癌细胞株NCI-H1975、人结肠癌细胞株HT-29、人前列腺癌细胞株DU-145),将细胞分为实验组[内生真菌发酵产物乙酸乙酯萃取部分,菌株暹罗刺盘孢菌(ZC-J4)和产黄青霉(BP-Y6)产物给药浓度为25、50、100、300和400μg·mL-1,菌株嗜线虫镰刀菌(ZP-G1)产物给药浓度为1.56、3.13、6.25、12.5、25和50 μg·mL-1)]、阴性对照组、阳性对照组(阳性药物阿霉素,给药浓度为 0.06、0.13、0.25、0.50 和 1.00 μg·mL-1).处理 48 h 后,用噻唑蓝法(MTT)法测定肿瘤细胞的增殖状况,计算内生真菌代谢产物对肿瘤细胞生长的抑制率和半数抑制浓度(IC50);并通过液相色谱-质谱联用技术(LC-MS)分析代谢产物中的主要成分.结果 3株紫苏内生真菌发酵产物对肿瘤细胞的增殖有抑制效果,且在一定浓度范围内呈剂量依赖性;不同菌株代谢产物抑制作用差异较大,ZP-G1的次生代谢产物表现出的抑制作用最强,尤其是对 HepG2 细胞和 HT-29 细胞,IC50值分别为(6.28±0.09)和(9.03±1.05)µg·mL-1;BP-Y6和ZC-J4的次生代谢产物对肿瘤细胞的毒性较弱,对NCI-H1975的IC50值均大于400 μg·mL-1.LC-MS结果分析表明,3种内生真菌的代谢产物含有部分相同成分,真菌ZP-G1中含有香紫苏二醇、杨梅素等成分,在其余2株真菌中未发现.结论 紫苏内生真菌的部分菌株具有抗肿瘤活性,菌株ZP-G1对肿瘤细胞增殖的抑制效果较好,具有进一步开发抗肿瘤天然活性成分的潜力.
Ethnopharmacological relevance: Albizia julibrissin Durazz is a well-known medicinal plant with the Chinese name Hehuan (sic). Hehuan bark and Hehuan flowers have long been recognized as traditional Chinese herbal medicine for treating anxiety, melancholy, insomnia, bruises, pulmonary abscess, fractures, carbuncle, amnesia, acute conjunctivitis, blurred vision, neonatal tetanus and stroke for thousands of years. They are recorded in Chinese Pharmacopoeia separately with different properties. Until now, new chemical constituents and phar-macological activities of Hehuan have been continuously studied and revealed. The aim of the review: This review aims to provide a comprehensive summary of traditional applications, phytochemistry, pharmacology effects, and toxicology of Hehuan bark and Hehuan flowers, and give critical assessment and point out the promising direction for further research on Hehuan. Material and methods: A literature search was undertaken on Hehuan bark and Hehuan flowers by analyzing the information from scientific databases (SciFinder, Pubmed, Elsevier, Google Scholar, Web of Science, and Baidu Scholar). We also gathered the information of Hehuan from classic herbal literatures and conference papers on ethnopharmacology. Results: According to Chinese and English documents, the medicinal history of Hehuan in China can be traced back to ad 25. Meanwhile, its medicinal history as a kind of herbal medicine can also be found in other Asian countries. So far about 140 compounds have been isolated from Hehuan bark and Hehuan flowers, including triterpenoids, flavonoids, lignans, phenolic acids, alkaloids, etc. Among them, flavonoids mainly exist in Hehuan flowers, while Hehuan bark contains lignans and saponins. The composition differences between the barks and flowers of Hehuan account for the different effects and applications. Modern pharmacological studies have indicated that crude extracts and pure compounds of Hehuan flowers and Hehuan bark have multiple phar-macological activities, such as antineoplastic, immunomodulatory, anti-inflammatory, anxiolytic, antidepres-sant, metabolic regulation, anti-insomnia, neuroprotective, hepatoprotective, sedative, and anti-osteolytic activities. Conclusions: Hehuan (Albizia julibrissin Durazz) is traditionally used to relieve depression, calm nerves, promote blood circulation and reduce swelling. Modern pharmacological studies have revealed that natural products from Hehuan bark and Hehuan flowers possess extensive pharmacological activities in treating cancer, enhancing immunity, regulating metabolism, improving mental state, etc. These properties make it great clinical application potential. Further research on natural pharmaceutical chemistry, pharmacology, toxicology, pharmacokinetics, and quality standards of Hehuan are still required to verify the efficacy and safety for future clinical applications.
A simple and sensitive liquid chromatography tandem mass spectrometry method was established and validated for the quantitative determination of abrine, hypaphorine, schaftoside and soyasaponin Bb in rat plasma. After preparation by protein precipitation with acetonitrile, the analytes and internal standard were separated on a Waters CORTECS T3 column using acetonitrile containing 0.1% formic acid and 0.1% formic acid in water as mobile phase by gradient elution in 2 min. The method showed excellent linearity over the range of 5-500 ng/ml with acceptable intra- and inter-day precision, accuracy, matrix effect and recovery. The stability assay indicated that the four analytes were stable during the analysis process. The method was applied to a pharmacokinetic study of Abrus cantoniensis Hance in rats. The result suggested that after oral administration, the four analytes were quickly absorbed into the plasma. The dose-normalized exposure of hypaphorine was the highest with a long elimination half-life (t1/2 9.83 h), followed by abrine and schaftoside with t1/2 values of 1.07 and 1.15 h. The dose normalized exposure of soyasaponin Bb was the lowest, which is possibily due to the high polarity and poor permeability. This study provides a basis for elucidating the material foundation of A. cantoniensis Hance.
目的 探究从矿区构树组织分离的2株内生真菌葡萄座腔菌(Botryos-phaeria dothidea,P-L12)和燕麦镰刀菌(Fusarium avenaceum,C-J1)的抗肿瘤活性并分析其代谢产物的化学成分.方法 体外培养指数增长期的5种肿瘤细胞,以噻唑蓝(MTT)法测定2株内生真菌次生代谢产物的抗肿瘤活性.在药物处理48 h后,测定不同条件下细胞的增殖情况,计算受试2种次生代谢产物的半抑制浓度(IC50)并进行趋势分析.用液相色谱-质谱联用(LC-MS)法分析2株内生真菌代谢产物的化学成分,明确其物质基础.结果 2株内生真菌发酵产物乙酸乙酯部位提取物对5种肿瘤细胞均具有抑制作用.作用48 h后C-J1有较强的细胞毒性作用,对人肝癌细胞HepG2的抑制作用最强,IC50 为(14.21±1.56)μg·mL-1,对其余4种肿瘤细胞也有较强的细胞毒活性.P-L12的次生代谢产物仅对人前列腺癌细胞DU-145具有较强的抑制作用,其IC50为(9.96±3.00)μg·mL-1.LC-MS 分析结果表明,C-J1 与 P-L12 次生代谢产物组成中有部分产物相同,两者的差异物质主要有杨梅素、甘松新酮和2,6-二甲氧基苯酚等.结论 2株逆境构树内生真菌P-L12和C-J1具有体外抑制肿瘤细胞活性,尤其是C-J1对肿瘤细胞的抑制作用较强,可作为潜在的抗肿瘤微生物药物资源.
NOVELTY STATEMENTPhytoremediation is an effective method for ecological remediation of heavy metal contaminated soil. Endophytic fungi such as arbuscular mycorrhizal fungi, dark septate endophytic fungi, plant growth promoting endophytic fungi can synergistically improve the adaptability to heavy metal stress. This review comprehensively summarizes the regulation mechanism of plant response to heavy metal stress mediated by endophytic fungi for the first time, and provides new insights and proposals for exploring novel hyperaccumulator for phytoremediation more effectively. Endophytic fungi exist widely in plants and play an important role in the growth and adaptation of plants. They could be used in phytoremediation techniques against heavy metal contaminated soil since beneficial microbial symbionts can endow plants with resistance to external heavy metal stresses. This review summarized the regulation mechanism of plant response to heavy metal stress mediated by endophytic fungi. Potential endophytic fungi in enhancing plant's adaption to heavy metal stresses include arbuscular mycorrhizal fungi, dark septate endophytic fungi, plant growth promoting endophytic fungi. The mechanisms involve coevolution strategy, immune regulation and detoxification transport to improve the ability of plants to adapt to heavy metal stress. They can increase the synthesis of host hormones and maintaining the balance of endogenous hormones, strengthen osmotic regulation, regulate carbon and nitrogen metabolism, and increase immune activity, antioxidant enzyme and glutathione activity. They also help to improve the detoxification transport and heavy metal emission capacity of the host by significantly producing iron carrier, metallothionein and 1-aminocyclopropane-1-carboxylic acid deaminase. The combination of endophytic fungi and hyperaccumulation plants provides a promising technology for the ecological restoration of heavy metal contaminated soil. Endophytic fungi reserves further development on enhancing host plant's adaptability to heavy metal stresses.
目的 对药食两用植物紫苏的名称、基原、形态和功效进行本草考证,以正本清源,为临床应用提供参考依据.方法 从名称、产地、原植物形态、功效、毒性与副作用等方面进行本草考证.结果 历代本草所言"紫苏""苏""白苏"均属"荏"类,为唇形科紫苏Perilla frutescens及其变种,紫苏叶紫色,茎、叶、子均入药,主下气.白苏叶绿色,治风寒.结论 紫苏与白苏在形态与功效上均有差别,应加以区分.紫苏作为药食两用中药具悠久的应用历史,白苏不宜作为食用.
BackgroundA. annua (also named Artemisia annua, sweet wormwood) is the main source of the anti-malarial drug artemisinin, which is synthesised and stored in its trichomes. Members of the basic Helix-Loop-Helix (bHLH) family of transcription factors (TFs) have been implicated in artemisinin biosynthesis in A. annua and in trichome development in other plant species.ResultsHere, we have systematically identified and characterised 226 putative bHLH TFs in A. annua. All of the proteins contain a HLH domain, 213 of which also contain the basic motif that mediates DNA binding of HLH dimers. Of these, 22 also contained a Myc domain that permits dimerisation with other families of TFs; only two proteins lacking the basic motif contained a Myc domain. Highly conserved GO annotations reflected the transcriptional regulatory role of the identified TFs, and suggested conserved roles in biological processes such as iron homeostasis, and guard cell and endosperm development. Expression analysis revealed that three genes (AabHLH80, AabHLH96, and AaMyc-bHLH3) exhibited spatiotemporal expression patterns similar to genes encoding key enzymes in artemisinin synthesis.ConclusionsThis comprehensive analysis of bHLH TFs provides a new resource to direct further analysis into key molecular mechanisms underlying and regulating artemisinin biosynthesis and trichome development, as well as other biological processes, in the key medicinal plant A. annua.
药用植物学是药学与中药学专业的一门专业基础课程,药用植物与中药不仅与人类健康密切相关,而且是人与自然及社会文化连接的纽带.为了全面提高药学人才培养质量,培育医学人文精神和职业道德,落实立德树人教育目标,在药用植物学教学中融入课程思政,利用本草文化、传统中医药文化挖掘思政元素,通过教材与课堂深化内涵,开设系列选修课程拓展外延,探索思政教育与专业课程相融合的路径.
人参是一味有着悠久应用历史的名贵中药,具有大补元气之功,治虚劳内伤第一要药.在其长期的临床应用中,历代医家根据用药要求,发明了多种炮制方法.查阅历代文献归纳总结为刮、拣、去芦、去苗、去须等净制之法;烧、焙、炒、煨、炙等火制之法;蒸、煮等水火共制之法;以及秋石拌等其他制法.研究人参炮制的历史发展过程,继承传统、开拓创新,有助于提高人参炮制技艺,优化炮制工艺,完善炮制技术,使其更好地服务于中医药临床.
目的 制定刺梨药材质量标准,用于刺梨的生产、监督、流通及使用等各环节的质量控制.方法 参照《中国药典》通用检测方法及相关指导原则分别制定刺梨的水分、总灰分、浸出物限度;采用特征图谱以及薄层色谱法控制刺梨整体质量.结果 刺梨特征图谱中应呈现6个特征峰,并应与对照药材参照物色谱峰中的5个特征峰保留时间相对应,另有1峰应与加入的异槲皮苷对照品参照物峰保留时间相对应.水分不得过14.0%,总灰分不得过5.0%,醇溶性浸出物不少于20.0%.结论 实验所建立的刺梨质量标准符合国家有关中药质量标准制定要求,能够以标准的形式对刺梨的质量进行控制.
目的 对目前市场上流通的中药材海马及其混淆品微性状鉴别研究,为海马的鉴别研究提供依据.方法 利用性状鉴别法对收集到的海马及其混淆品进行鉴别;运用中药微性状鉴定法对11种不同品种海马的鳃盖和冠应用体式显微镜拍摄,运用景深合成技术合成1张高清微性状照片进行鉴别研究.结果 不同品种海马在鳃盖的嵴纹以及头冠有较明显的区别.结论 微性状鉴别法能够有效将市场上流通的不同品种的海马进行区分,并且具有简单快捷的特点.
新型冠状病毒肺炎(COVID-19)是由新型冠状病毒(SARS-CoV-2)感染引起的以发热、乏力、干咳为主要表现的急性呼吸道传染病.此次疫情,中医药在防治新冠肺炎中起到了重要作用.本文概述了新冠肺炎的发病机制,中医药辨证论治以及抗病毒中药、抗炎中药、免疫调节中药的应用前景,尤其是一些具有双向调节作用中药的应用,以期为新冠肺炎的预防和治疗提供科学思路.
The novel coronavirus pneumonia is an acute respiratory infectious disease mainly manifested by fever, fatigue and dry cough, caused by new coronavirus 2019-nCoV infection(COVID-19). Traditional Chinese Medicine played an important role in the prevention and treatment of COVID-19 during this breakout. This article reviews the clinical treatments of SARS-CoV-2 with TCM, the pathogenesis of COVID-19, dialectical treatment with TCM, and the antiviral, anti-inflammatory, immune regulatory effects of TCM. Some TCM with dual immuno-modulatory effects draw special attention, which may shed light on the prevention and treatment of COVID-19.
目的 研究构树内生真菌次级代谢产物的抗肿瘤活性.方法 用96孔板接种培养人肝癌细胞株HepG2,人乳腺癌细胞株MCF-7,人肺腺癌细胞株NCI-H1975,人结肠癌细胞株HT-29和人前列腺癌细胞株DU-145,将细胞分为4组:实验组(内生真菌发酵提取物:1.56,3.13,6.25,12.50,50.00μg·mL-1),空白对照组(0),阴性对照组(0),阳性对照组(阿霉素:0.06,0.13,0.25,0.50,1.00μg·mL-1).用四甲基偶氮唑盐微量酶反应比色法(Methyl-thiazolyldiphenyl-tetrazolium bromide,MTT)测定癌细胞增殖情况,计算细胞生长抑制率与半数抑制浓度(50%inhibiting concentration,IC50).结果 构树内生真菌发酵提取物可抑制HepG2、MCF-7、NCI-H1975、HT-29、DU-145细胞的增殖,并在一定范围内呈明显的质量浓度依赖性,作用72 h后,Alternaria alterna-ta、Gibberella avenacea的次级代谢产物显示较强的细胞毒性,Alternaria alternata对HepG2、DU-145的IC50值分别为(1.13±0.44)和(0.99±0.36)μg·mL-1,Gibberella avenacea对HepG2、MCF7、HT-29的IC50值分别为(1.22±0.38),(0.90±0.27)和(0.56±0.14)μg·mL-1;而Alternaria tenuissima、Fusarium equi-seti的次级代谢产物显示较弱的细胞毒性,Alternaria tenuissima对HepG2、NCI-H1975和DU-145的IC50值均大于50.00μg·mL-1,Fusarium equiseti对HepG2、MCF-7、NCI-H1975和HT-29的IC50值大于50.00μg·mL-1.结论 构树内生真菌次级代谢产物具有抗肿瘤活性,尤其Alternaria alternata和Gibberella avenacea的活性较强,是潜在的抗肿瘤天然产物新资源.