中心组合设计-响应面分析法优选莽吉柿果皮中α-mangostin的超声提取工艺

目的:优化莽吉柿果皮中α-mangostin的提取工艺。方法:采用中心组合设计方法,研究乙醇浓度、超声时间、液固比及其交互作用对α-mangostin提取率的影响。应用SAS软件和响应面分析相结合的方法,模拟得到回归方程的预测模型和可信度,并通过岭脊分析得到最佳的提取条件。结果:最佳提取条件为:乙醇浓度67.8%、超声提取时间85.9 min、液固比24.2 mL/g。该条件下提取率为5.53%。结论:本研究为工业化提取α-mangostin提供了有效方法。

Antibiofilm activity of a-mangostin extracted from Garcinia mangostana L. against Staphylococcus aureus

Objective: To isolate a-mangostin(AMG) from the peels of mangosteen(Garcinia mangostana L.), grown in Vietnam, and to investigate antibiofilm activity of this compound against three Staphylococcus aureus(S. aureus) strains, one of which was methicillin-resistant S. aureus(MRSA) and the other two strains were methicillinsensitive S. aureus(MSSA).Methods: AMG in n-hexane fraction was isolated on a silica gel column and chemically analyzed by HPLC and NMR. The antibiofilm activity of this compound was investigated by using a 96-well plate model for the formation of biofilms. Biofilm biomass was quantified using crystal violet. The viability of cells was observed under confocal microscopy using LIVE/DEAD Bac Light stains. Biofilm composition was determined using specific chemical and enzyme tests for polysaccharide, protein and DNA. Membranedamaging activity was assayed by measuring the hemolysis of human red blood cells in presence of AMG.Results: The results indicated that the isolated AMG, with a purity that exceeded 98%,had minimal inhibitory concentrations in the range of 4.6–9.2 mmol/L for the three strains tested. Interestingly, the MSSA strains were more sensitive to AMG than the MRSA strain. Minimal bactericidal concentrations were 2-fold higher than the minimal inhibitory concentration values for the three strains, indicating that AMG was a bactericidal compound. AMG also prevented biofilm formation effectively, albeit that again the MRSA strain was the most resistant. Interestingly, biofilms of the MRSA strain contained protein as a main component of the extracellular matrix, whereas this was polysaccharide in the MSSA strains. This might relate to the resistance of the MRSA 252 strain to AMG.Assays using human red blood cells indicated that AMG caused significant membrane damage with 50% of cell lysis occurred at concentration of about 36 mmol/L.Conclusions: Our results provide evidence that the isolated AMG has inhibitory activity against biofilm formation by S. aureus, including MRSA. Thus, isolated AMG proposes a high potential to develop a novel phytopharmaceutical for the treatment of MRSA.

RP-HPLC-UVD法测定莽吉柿胶囊中alpha-mangostin的含量

建立一种测定莽吉柿胶囊中α-倒捻子素(alpha-mangostin)含量的方法。采用反相高效液相色谱-紫外检测法测定。色谱条件:DiamonsilTMCl8色谱柱(250 mm×4.6 mm,5μm),流动相为甲醇-水(83∶17),流速为1.0 mL/min,柱温:25℃,紫外检测波长:317 nm。在选定的色谱条件下,反相高效液相色谱-紫外检测法符合精密度、准确度、线性(r=0.999 5)的基本要求,加样回收率为100.9%,RSD为1.82%。该方法简便、准确、灵敏度高、重现性好,可用于莽吉柿胶囊中alpha-mangostin的含量测定。

Inhibitory Effect of Alpha‑Mangostin to Dengue Virus Replication and Cytokines Expression in Human Peripheral Blood Mononuclear Cells

Massive pro-inflammatory cytokines production has been correlated with the pathogenesis of severe dengue disease.The active compound of mangosteen fruit pericarps,α-mangostin,has been commonly used as traditional medicine and dietary supplement.We examined the effect ofα-mangostin against dengue virus(DENV)infection in human peripheral blood mononuclear cells(PBMC)by the measurement of virus titer and TNF-αand IFN-γcytokines concentration post infection.Increasing concentration ofα-mangostin inhibited virus replication and reduced inflammatory cytokines expression at 24-and 48-h post infection.Our results support the potential use ofα-mangostin as anti-antiviral and anti-inflammatory therapies in the treatment of dengue.

α-Mangostin and apigenin induced the necrotic death of BT474 breast cancer cells with autophagy and inflammation

Objective: To find new compounds in order to overcome the mainstay of metastatic breast cancer due to the adverse side effects from, and increasing resistance to, current chemotherapeutic agents. Methods: 毩-Mangostin and apigenin were reported in comparison to doxorubicin, a chemotherapeutic drug. Ductal carcinoma(BT474) cell line and nontumorigenic epithelial tissue from mammary gland(MCF-10 A) were used. Cell viability assessment was calculated by the standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide method. Cell morphology was investigated by light microscopy. By flow cytometry analysis, programmed cell death was observed using annexin observed using propidium iodide st桋 and propidium iodide staining while cell-cycle arrest wasaining. Change in transcriptional expression was evaluated by real-time quantitative reverse transcription PCR. Results: In 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, the result revealed and apigenin were more cytotoxic to BT474 cells. Longer exposure times to 毩-mangostin enin caused more floating cells and a lower density of adhered cells wi毩-mangostin and apigth more vacuoles present in the colonies in BT474 only. 毩-Mangostin and apigenin caused necrosis in BT474 cells in a 24 h exposure, but a small amount of early apoptotic cells could also be detected at 24, 48 and 72 h exposure, whereas doxorubicin caused early apoptosis to BT474 cells at 24 h. Transcript expression and activity analysis supported caspase-3 was involved in the death of BT474 cells treated by all compounds. Moreover, 毩-mangostin and apigenin arrested the cellcycle at the G1-phase, but at the G2/M-phase by doxorubicin. All three compounds induced a change in transcript expression levels of inflammation-associated, proto-oncogene, autophagyassociated and apoptosis-associated genes. Conclusions: ntial new sources of chemotherapeuti毩-Mangostin and apigenin are worth investigating as potec agents for breast cancer treatment.

RP—HPLC法测定山竹果壳中a—Mangostin的含量

建立高效液相色谱法测定山竹果壳中a—Mangostin的含量。色谱条件：色谱柱为Diamonsil C18（250mm×4．6mm，5μm）；流动相为乙腈-pH3．0磷酸水溶液（70：30）；流速1．0mL／min；检测波长240nm；柱温25℃；进样20山。线性范围内0．02—0．10mg／mL（r=0．9998），加样平均回收率为98．25％，RSD为0．74％（n=6）。本方法准确度高、重现性好，操作快速简捷，可以作为山竹果壳中a—Mangostin含量的检测方法。

<i>α</i>-Mangostin Promotes DAF-16-Mediated Thermotolerance in <i>Caenorhabditis elegans</i>

Garcinia mangostana, commonly known as mangosteen, is a tropical fruit with a reddish-purple pericarp. In Southeast Asia, the pericarp has traditionally been used as a medicine to treat various diseases, including inflammation, wounds, and bacterial infections, as well as aging. α-mangostin is an abundant xanthone in the pericarp, and is thought to play a critical role in the medicinal effects of mangosteens. Previous studies have demonstrated numerous beneficial effects of α-mangostin, such as cytotoxicity in cancer cells. However, the effects of this xanthone in in vivo have not yet been studied. In the current study, C. elegans was used to test the in vivo effects of α-mangostin using several bioassays, including fat accumulation, pharyngeal movement (pumping) and heat-stress assays. Quantitative real time PCR (qRT-PCR) was also used to examine the expression of heat shock proteins. The results revealed that α-mangostin appeared to cause an increase in fat accumulation, which correlated with an increase in pharyngeal movement. The thrashing movement of the worms after heat stress also showed a correlation with an increase in heat shock protein mRNA expression.

α-倒捻子素通过NF-κB途径抑制LPS/ATP诱导的小胶质细胞中NLRP3炎症小体的激活

目的探究α-倒捻子素(α-mangostin)在脊髓损伤后小胶质细胞炎症模型中作用及相关机制。方法体外培养小鼠小胶质细胞系BV-2细胞,利用脂多糖和三磷酸腺苷(LPS/ATP)联合诱导的方式建立BV-2炎症模型。CCK-8法检测不同浓度(0、10、20、40、80μmol/L)的α-mangostin对LPS/ATP刺激下的细胞增殖活力影响以筛选适宜的α-mangostin浓度范围;将BV-2细胞分为Ctrl组、LPS/ATP组、40μmol/Lα-mangostin组和不同浓度(10、20、40μmol/L)的α-mangostin干预组(分别记为LPS/ATP+10μmol/Lα-mangostin组、LPS/ATP+20μmol/Lα-mangostin组与LPS/ATP+40μmol/Lα-mangostin组)。ELISA实验检测各组BV-2细胞上清液中促炎因子白介素-6/1β/18(IL-6、IL-1β、IL-18)和肿瘤坏死因子(TNF-α)含量,Western blot检测各组细胞中NOD样受体蛋白3(NLRP3)炎症小体相关蛋白NLRP3、凋亡相关斑点样蛋白(ASC)、裂解型半胱氨酸蛋白酶1(cleaved caspase-1)和白介素1β(IL-1β)表达及核因子κB(NF-κB)途径中p65的磷酸化水平(p-p65/p65)和BV-2细胞核中p65的表达。结果与Ctrl组相比,LPS/ATP组细胞增殖活力明显降低(P<0.05),但低浓度(10、20、40μmol/L)的α-mangostin可显著改善LPS/ATP对小胶质细胞增殖活力的抑制作用(P<0.05),但高浓度(80μmol/L)α-mangostin可促进LPS/ATP对小胶质细胞的损伤(P<0.05)。与Ctrl组相比,40μmol/Lα-mangostin组小胶质细胞上清液中炎症因子IL-6、IL-1β、IL-18、TNF-α含量和细胞中NLRP3、ASC、cleaved caspase-1、IL-1β和p-p65/p65比值及细胞核中p65蛋白均无明显改变(P>0.05),而LPS/ATP组均显著增加(P<0.05);与LPS/ATP组相比,不同浓度α-mangostin干预组中IL-6、IL-1β、IL-18、TNF-α含量和BV-2细胞中NLRP3、ASC、cleaved caspase-1、IL-1β和p-p65/p65比值及细胞核中p65蛋白表达随α-mangostin浓度的增加而依次降低,其中以LPS/ATP+40μmol/Lα-mangostin组的降低程度最为明显(P<0.01)。结论α-mangostin可通过NF-κB途径抑制BV-2细胞中NLRP3炎性小体活化所介导的神经炎症反应。

大豆提取物-α-倒捻子素复合物的制备及其抗氧化活性

为提高难溶化合物α-倒捻子素溶解性,采用摇瓶-冷冻干燥法制备大豆提取物-α-倒捻子素复合物并对其进行结构表征和体外抗氧化活性评价。结果表明,在最佳工艺即大豆提取物质量浓度200 mg/mL、60℃、16 h、220 r/min下制得的复合物中α-倒捻子素溶解度为379.014μg/mL;复合物平均粒径为(1.21±0.015) nm,分布均一,且大豆提取物与α-倒捻子素之间可能通过氢键缔合;大豆提取物与α-倒捻子素具有协同抗氧化作用,大豆提取物-α-倒捻子素复合物对DPPH自由基和ABTS自由基清除作用强于同质量浓度的α-倒捻子素。

α-倒捻子素/甘草酸纳米胶束的制备、表征及评价

制备α-倒捻子素/甘草酸纳米胶束(α-Mangostin/glycyrrhizic Acid Nanomicelles,α-MG/GA NMs),以提高α-倒捻子素(α-Mangostin,α-MG)的溶解度和抗氧化活性。以甘草酸(Glycyrrhizic Acid,GA)为载体制备α-MG/GA NMs,并进行工艺优化,表征和体外释放度、体外抗氧化活性评价。结果表明,在最佳工艺下制得的α-MG/GA NMs中α-MG溶解度为232.65μg/mL,比水中溶解度大了近1163倍;α-MG/GA NMs粒径为123.46 nm、PDI为0.24、Zeta电位为-20.94 mV;透射电镜(TEM)和扫描电镜(SEM)显示其为类球形;冻干后在光照、高温、高湿条件下稳定性良好;傅里叶红外光谱(FT-IR)显示α-MG与GA可能发生氢键相互作用;体外释放结果表明α-MG/GA NMs能促进α-MG释放,具有缓释效果,在pH值7.4、5.0的释放介质中24 h累积释放率分别为47.03%、40.56%;与游离α-MG相比,α-MG/GA NMs的抗氧化活性更强,且GA与α-MG具有协同抗氧化作用,对DPPH自由基、ABTS+自由基清除作用的协同指数(CI值)分别为0.62、0.58。该研究制备的α-MG/GA NMs提高了α-MG的溶解度与抗氧化活性,为α-MG在食品、药品、化妆品等领域的应用提供了理论基础。

Pharmacology of mangostins and their derivatives:A comprehensive review

Mangosteen(Garcinia mangostana Linn.) is a well-known tropical tree indigenous to Southeast Asia. Its fruit's pericarp abounds with a class of isoprenylated xanthones which are referred as mangostins. Numerous in vitro and in vivo studies have shown that mangostins and their derivatives possess diverse pharmacological activities, such as antibacterial, antifungal, antimalarial, anticarcinogenic, antiatherogenic activities as well as neuroprotective properties in Alzheimer's disease(AD). This review article provides a comprehensive review of the pharmacological activities of mangostins and their derivatives to reveal their promising utilities in the treatment of certain important diseases, mainly focusing on the discussions of the underlying molecular targets/pathways, modes of action, and relevant structure-activity relationships(SARs). Meanwhile, the pharmacokinetics(PK) profile and recent toxicological studies of mangostins are also described for further druggability exploration in the future.

Synergistic effect of α-mangostin on antibacterial activity of tetracycline, erythromycin, and clindamycin against acne involved bacteria

Objective:To evaluate the synergistic effect ofα-mangostin with tetracycline,erythromycin,and clindamycin against bacteria involved in acne production.Methods:A broth microdilution method was used to determine the minimum inhibitory concentration(MIC)ofα-mangostin and a range of antibiotics.Synergistic effects on antibacterial activity were determined based on their own MIC,and then using a checkerboard method and a time-kill assay at 37°C for24 h.Results:α-Mangostin exhibited antibacterial activity against Propionibacterium acnes,Staphylococcus aureus,S.epidermidis and S.pyogenes with MIC values of 0.78,3.13,0.78,and 6.25μg/m L,respectively.The results of the checkerboard assay showed thatα-mangostin produced synergistic effects with tetracycline,erythromycin,and clindamycin against all tested bacteria,with a fractional inhibitory concentration index(FICI)between 0.09 and 0.32.Moreover,time-kill curve data indicated thatα-mangostin increased the antibacterial activity of tetracycline,erythromycin,and clindamycin.Conclusion:These findings suggested thatα-mangostin may be used to enhance the antibacterial activity of some antibiotics against bacteria involved in acne production.

鼠尾草酸、α-倒捻子素联合不同作用机制抗生素的抗金黄色葡萄球菌作用研究

目的探究植物源抗菌天然产物鼠尾草酸、α-倒捻子素分别与抗生素的联合应用效果,发现不同联合应用效果的抗菌组合物。方法分别以敏感金黄色葡萄球菌ATCC25923、耐甲氧西林金黄色葡萄球菌MRSA 01为指示菌株,采用微量肉汤稀释法,测定鼠尾草酸、α-倒捻子素和不同作用机制抗生素对指示菌株的最低抑菌浓度;再采用棋盘格法,分别测定鼠尾草酸、α-倒捻子素与不同作用机制抗生素联用对测试菌株的部分抑菌浓度指数(fractional inhibitory concentration index,FICI)。结果鼠尾草酸、α-倒捻子素联合硫酸庆大霉素对测试菌株的FICI范围分别为0.28~0.62、0.31~0.50,前者对两株测试菌株分别显示协同或无关作用,后者均显示协同作用;鼠尾草酸、α-倒捻子素分别与其他抗生素对测试菌株的FICI范围为0.52~1.12,均显示无关作用。结论靶向细胞膜的鼠尾草酸、α-倒捻子素与作用于核糖体影响细胞膜的氨基糖苷类庆大霉素联用时,主要呈现协同的联合抗菌效果,进一步证实了课题组发现的联合用药效果的相关规律;组合物鼠尾草酸/硫酸庆大霉素对金黄色葡萄球菌的不同菌株既可显示协同,又可显示无关作用,为联合用药防细菌耐药的进一步研究打下了基础。

α-倒捻子素对10种植物病原细菌的杀菌活性

α-倒捻子素(α-mangostin)是山竹果皮中一种具有生物活性多样的的氧杂蒽酮类化合物。为探明α-倒捻子素的农用杀细菌活性,对10种植物病原细菌进行室内抑菌活性初筛,并对抑制效果较好的病原细菌采用平板菌落法进行室内毒力及盆栽试验。结果表明,α-倒捻子素对水稻白叶枯病菌和甜瓜细菌性果斑病菌的抑菌活性最强,其EC50分别为35.93和27.58 mg/L,同时对甜瓜细菌性果斑病具有较强的保护和治疗作用,其中保护作用优于治疗作用。因此,α-倒捻子素对植物病原细菌具有良好的抑制效果,在农用抑菌方面具有很大的研究潜力。

α-倒捻子素通过HMGB1促炎通路诱导人黑色素瘤A375细胞的凋亡

目的研究α-倒捻子素对人黑色素瘤A375细胞增殖、迁移和凋亡的影响及HMGB1介导的炎症反应在给药过程中的作用。方法利用含有不同药物浓度(0、10、15、20μM)的DMEM培养基培养人黑色素瘤A375细胞,CCK-8试剂盒检测每组细胞活力及药物毒性,并使用光学显微镜观察用药后细胞形态变化;划痕实验检测每组用药后人黑色素瘤A375细胞的迁移能力;使用TUNEL染色检测用药后人黑色素瘤A375细胞的凋亡情况;细胞免疫荧光实验用来观察HMGB1蛋白用药前后的表达变化;免疫印迹实验检测药物处理后人黑色素瘤A375细胞内HMGB1及其相关炎症通路蛋白的表达情况。结果α-倒捻子素对A375细胞存在明显毒性,且显著抑制A375细胞的增殖及迁移,并呈现剂量依赖的效果;TUNEL染色证明,α-倒捻子素显著诱导A375细胞凋亡;细胞免疫荧光和免疫印迹实验表明,α-MG组HMGB1及炎症相关蛋白表达明显减少(P<0.01)。结论α-倒捻子素可显著抑制人黑色素瘤A375细胞的生长,激活HMGB1相关炎症通路,诱导人黑色素瘤A375细胞发生凋亡。

α-倒捻子素调节骨关节炎软骨细胞的增殖和凋亡

目的研究α-倒捻子素对骨关节炎(osteoarthritis,OA)软骨细胞增殖和凋亡的影响。方法先分离培养人原代OA软骨细胞,分别给予5、10、20μmol/L的α-倒捻子素处理后24、48、72 h运用MTT法检测细胞增殖情况;流式细胞仪检测细胞凋亡情况;Western blot法检测基质金属蛋白酶1(matrix metalloproteinase-1,MMP-1)、MMP-3、MMP-13、过氧化物酶体增殖激活物受体γ(peroxisome proliferator-activated receptorγ,PPARγ)、PPARδ、过氧化物酶增殖激活受体γ共激活子-1α(peroxisome proliferator-activated receptorγcoactivator-1α,PGC-1α)及肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)的表达;ELISA法检测细胞培养上清中的Ⅱ型胶原蛋白(collagen-Ⅱ)、蛋白多糖(proteoglycans,PG)、白细胞介素-1β(interleukin-1β,IL-1β)及IL-6含有量。结果α-倒捻子素可显著促进细胞增殖,抑制细胞凋亡;显著促进Collagen-Ⅱ和PG的产生;显著抑制MMP-1、MMP-3、MMP-13的表达;显著促进PPARγ、PPARδ、PGC-1α的表达,抑制TNF-α的表达。此外,α-倒捻子素还可显著抑制IL-1β和IL-6的产生。结论α-倒捻子素可通过增加PPARδ、PPARγ的表达,促进OA软骨细胞增殖,抑制细胞凋亡和炎性反应,从而延缓关节软骨的破坏和退变。

α-山竹黄酮的NMR研究

应用一维1H NMR、13C NMR、DEPT、二维HMBC、HSQC、1H-1H COSY、ROESY对1,3,6-三羟基-7-甲氧基-2,8双(3-甲基-2-丁烯)-9-口山酮(-αmangostin、-αMAG)的1H、13C原子进行了指认归属.

应用Alamar Blue法与试管法测定α-倒捻子素和8-甲氧基补骨脂素体外抗结核杆菌活性

选取传统中药提取单体化合物α-倒捻子素和8-甲氧基补骨脂素,通过2种药物敏感性实验方法MABA(Microdilution Alamar Blue Assay)分析与试管法分别测定了两种化合物对结核分枝杆菌H37Rv(ATCC27294)和H37Ra(ATCC25177)的体外抗菌活性,同时还测定了9种阳性抗结核药物对这两种结核菌的最低抑菌浓度(MIC),比较2种方法的检测结果。结果表明:α-倒捻子素对结核分枝杆菌H37Rv(ATCC27294)和H37Ra(ATCC25177)的最低抑菌浓度均为6.25μg/mL,而8-甲氧基补骨脂素对结核分枝杆菌H37Rv(ATCC27294)和H37Ra(ATCC25177)的最低抑菌浓度均为128μg/mL。Alamar B1ue法与试管法相比较,完全符合率是90%(9/11),具有较好的一致性。本研究结果表明Mamar B1ue法是一种快速、简便测定药物对结核分枝杆菌MIC的方法。本研究为α-倒捻子素和8-甲氧基补骨脂素的进一步开发利用和抗分枝杆菌机制研究打下了基础。

α-倒捻子素对MKN45胃癌细胞增殖、迁移、侵袭和血管生成的影响及其作用机制

目的:探讨α-倒捻子素对人胃癌细胞MKN45增殖、迁移、侵袭和血管生成的影响及其作用机制。方法:MTS法研究α-倒捻子素对人胃癌细胞MKN45增殖的影响;伤口愈合实验及Transwell实验分别用于研究α-倒捻子素对MKN45细胞体外迁移及侵袭的影响;采用大鼠动脉环实验检测α-倒捻子素对MKN45胃癌细胞血管生成的影响;ELISA实验检测α-倒捻子素对MKN45细胞分泌的血管内皮生长因子(vascular endothelial growth factor,VEGF)、肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)、转化生长因子-β(transforming growth factor-β,TGF-β)及碱性成纤维细胞生长因子(basic fibroblast growth factor,b FGF)表达的影响等;Western blot检测α-倒捻子素对基质金属蛋白酶-2(matrix metalloproteinase-2,MMP-2)、基质金属蛋白酶-9(matrix metalloproteinase-9,MMP-9)、神经-钙黏素(N-cadherin)及上皮-钙黏素(E-cadherin)蛋白表达的影响。结果:α-倒捻子素能够明显抑制人胃癌细胞MKN45的增殖,且具有剂量依赖性;α-倒捻子素能够明显抑制MKN45细胞的迁移和侵袭;动脉环实验结果显示α-倒捻子素能够抑制MKN45细胞诱导的血管生成。ELISA结果显示,α-倒捻子素能够抑制VEGF、TNF-α、TGF-β及b FGF的蛋白表达;Western blot结果显示α-倒捻子素能够下调MMP-2、MMP-9及神经-钙黏素的表达,同时上调上皮-钙黏素的表达。结论:α-倒捻子素能够抑制MKN45人胃癌细胞的增殖、迁移、侵袭和血管生成,其发挥作用可能与以下两方面机制相关:(1)抑制调控肿瘤细胞迁移及血管生成相关蛋白的表达;(2)抑制MKN45细胞的上皮间质转化。

α-倒捻子素通过加剧自噬影响胃癌细胞的增殖和凋亡

目的探讨α-倒捻子素对人胃癌细胞增殖和凋亡的影响及其分子机制。方法CCK8法检测α-倒捻子素对SGC7901细胞活力的影响,免疫荧光和流式细胞术检测α-倒捻子素对SGC7901细胞凋亡及细胞周期的影响,Western blot法检测细胞凋亡及自噬相关蛋白的表达情况。统计分析的正态性检验采用Shapir-Wilk;服从正态分布的多组间比较采用单因素方差分析;方差不齐时,采用Welch矫正检验,两两间比较采用Games-Howell检验。结果 CCK8法结果显示,不同浓度的α-倒捻子素(10、15、20、25、30μmol/L)处理后组间细胞活力的差异有统计学意义(P<0.05)。qPCR结果表明,LC3而非Caspase蛋白的mRNA水平与α-倒捻子素浓度呈正相关(r=0.976,P<0.05)。在15μmol/L而非10μmol/L的α-倒捻子素处理系统中,6-氨基-3-甲基嘌呤(3-MA,10μmol/L)、巴弗洛霉素A(10μmol/L)、LY294002(10μmol/L)等自噬抑制剂均能显著缓解α-倒捻子素对SGC7901细胞的杀伤作用(P<0.05)。结论α-倒捻子素可能主要通过诱导自噬性死亡而影响人胃癌细胞的活力。