Research progress of anti-tumor effect and mechanism of CDDO and its derivatives / 中国药房

2-cyano-3，12-dioxooleana-1，9 （11）-dien-28-oic acid （CDDO） is a compound synthesized by taking oleanolic acid， a natural triterpene， as a precursor or precursor， and transforming three modifiable functional groups in the molecule through a series of chemical structure modification. In order to improve its anti-tumor activity， CDDO derivatives are further synthesized. In this paper， the research results of anti-tumor effects and mechanisms of CDDO and its derivatives in recent years are summarized. It is found that CDDO and its derivatives have a wide range of anti-tumor effects， and can show significant anti-tumor effects on breast cancer， pancreatic cancer， lung cancer and ovarian cancer at low concentrations such as micromole or even nanomole， among which CDDO methyl ester compound （CDDO-Me） and CDDO imidazolidinone compound （CDDO-Im） have the most obvious effects. CDDO and its derivatives exert anti-tumor activity mainly by inducing tumor cell apoptosis， and regulating metabolic reprogramming and immune microenvironment. The involved pathways mainly include Janus protein tyrosine kinase （JAK）/ signal transduction and transcription activation protein 3（STAT3） signal pathway， nuclear factor E2-related factor 2 （NRF2） signal pathway， phosphatidylinositol 3 kinase （PI3K）/protein kinase B （also known as Akt）/mammalian rapamycin target protein （mTOR） signal pathway， Wnt/β-catenin signal pathway， nuclear factor κB signal pathway.

Study on the modification and anti-tumor activity of silybin derivatives for CDK4/6 targeted / 药学学报

By using computer-aided drug design, the activities group model which CDK4/6 inhibitors on the market were introduced to silybin C-7, and a series of silybin derivatives were designed and synthesized, and the structure was confirmed by MS, 13C NMR and 1H NMR. The in vitro antitumor activity evaluation of the target compound was carried out by MTT method, and the in vitro anti-tumor activity was carried out in human hepatocellular carcinoma cells (HepG-2). Experimental results show that all compounds are higher than the activity of the parent silybin, of which compound I1 has a certain inhibitory effect on human HepG-2 cells, which is worth further study.

Research progress on chemical structures and pharmacological effects of natural cytisine and its derivatives / 中国中药杂志

Cytisine derivatives are a group of alkaloids containing the structural core of cytisine, which are mainly distributed in Fabaceae plants with a wide range of pharmacological activities, such as resisting inflammation, tumors, and viruses, and affecting the central nervous system. At present, a total of 193 natural cytisine and its derivatives have been reported, all of which are derived from L-lysine. In this study, natural cytisine derivatives were classified into eight types, namely cytisine type, sparteine type, albine type, angustifoline type, camoensidine type, cytisine-like type, tsukushinamine type, and lupanacosmine type. This study reviewed the research progress on the structures, plant sources, biosynthesis, and pharmacological activities of alkaloids of various types.

Antitumor activity of aumolertinib, a third-generation EGFR tyrosine kinase inhibitor, in non-small-cell lung cancer harboring uncommon EGFR mutations

Uncommon epidermal growth factor receptor (EGFR) mutations account for 10%-20% of all EGFR mutations in non-small-cell lung cancer (NSCLC). The uncommon EGFR-mutated NSCLC is associated with poor clinical outcomes and generally achieved unsatisfactory effects to the current therapies using standard EGFR-tyrosine kinase inhibitors (TKIs), including afatinib and osimertinib. Therefore, it is necessary to develop more novel EGFR-TKIs to treat uncommon EGFR-mutated NSCLC. Aumolertinib is a third-generation EGFR-TKI approved in China for treating advanced NSCLC with common EGFR mutations. However, it remains unclear whether aumolertinib is effective in uncommon EGFR-mutated NSCLC. In this work, the in vitro anticancer activity of aumolertinib was investigated in engineered Ba/F3 cells and patient-derived cells bearing diverse uncommon EGFR mutations. Aumolertinib was shown to be more potent in inhibiting the viability of various uncommon EGFR-mutated cell lines than those with wild-type EGFR. And in vivo, aumolertinib could also significantly inhibit tumor growth in two mouse allograft models (V769-D770insASV and L861Q mutations) and a patient-derived xenografts model (H773-V774insNPH mutation). Importantly, aumolertinib exerts responses against tumors in advanced NSCLC patients with uncommon EGFR mutations. These results suggest that aumolertinib has the potential as a promising therapeutic candidate for the treatment of uncommon EGFR-mutated NSCLC.

Anti-tumor activity of yeast vesicle biomimetic nanomedicine with the ability of active tumor penetration / 药学学报

The dense extracellular matrix (ECM) of the tumor severely limits the deep penetration of nanomedicine and weakens its anti-tumor effect. Based on this, the yeast vesicle biomimetic nanomedicine with active deep penetration ability of tumor tissue was designed and developed for enhanced tumor therapy. Results of characterization showed that the yeast cell vesicles (YCV) displayed a spherical morphology with diameter of around 100 nm and was well dispersed. Then the chemotherapeutic drug doxorubicin (DOX) was selected as a model drug, and DOX was loaded into YCV to obtain YCV/DOX through electrostatic interaction, the encapsulation efficiencies of DOX were calculated as 82.5%. The drug release profile of YCV/DOX implied that DOX release showed a manner of pH-dependent, it may be that pH has affected the electrostatic effect of YCV and DOX. Compared with liposomes (Lipo), in vitro cell experiments showed that YCV from natural sources had stronger permeability in three-dimensional multicellular spheres. It is speculated that the mechanism may be good deformation capacity of YCV. A 4T1 xenograft tumor model was established to evaluate the therapeutic efficacy of YCV/DOX. The results suggested that YCV/DOX has stronger tumor tissue penetration ability and could effectively inhibit the tumor growth. All animal experiments were performed in line with national regulations and approved by the Animal Experiments Ethical Committee of Zhengzhou University. This study brings new ideas for the development of biomimetic nanomedicine to overcome the ECM of solid tumors.

Study on preparation ，safety and anti-tumor activity of apigenin silk fibroin nanoparticles / 中国药房

OBJECTIVE To prepare apigenin silk fibroin（API@SF）nanoparticles and to evaluate their safety and anti-tumor activity. METHODS API@SF nanoparticles were prepared by nanoprecipitation method ，and their morphology ，particle size ，Zeta potential，drug loading amount and in vitro release were characterized. The safety of nanoparticles was evaluated by hemolysis test and HE staining. MTT assay was adopted to evaluate inhibitory effects of API@SF nanoparticles on breast cancer 4T1 cells in mice. RESULTS The prepared API@SF nanoparticles were spherical with uniform distribution. The average particle size was 406.61 nm， the polydispersity index was 0.154，the Zeta potential was －18.4 mV，and the average drug-loading amount was 5.20％. The in vitro release results showed that the release rate of the nanoparticles was relatively fast in the release medium of pH 5.0 and relatively slow in the release medium of pH 7.4. Results of hemolysis test and HE staining showed that the nanoparticles had good biocompatibility. Results of MTT assay showed that the inhibitory effect of API@SF nanoparticles on 4T1 cells was significantly higher than that of API raw materials （P＜0.05），and its mechanism may be related to increasing the level of reactive oxygen species in cells. CONCLUSIONS API@SF nanoparticles are prepared successfully ，which possess good safety and anti-tumor activity.

Secretory phospholipase A2 responsiveness and in vitro anti-tumor activity of oxaliplatin-loaded liposomes modified with facial amphiphiles / 中国药科大学学报

@#Modulating drug release from liposomes at tumor sites are important for eliciting therapeutic effects of platinum drugs considering their low permeability through liposomal membranes, here a novel secretory phospholipase A2 (sPLA2) responsive-liposome system was constructed for oxaliplatin (L-OHP).Lipid ingredients dipalmitoyl phosphatidylcholine and distearoyl phosphoethanolamine-PEG2k, together with facial amphiphiles (FAs) including lithocholic acid (LCA) or 3-keto lithocholic acid (kLCA) were used to prepare sPLA2 responsive-liposome (LCA-Lip or kLCA-Lip) by thin-film hydration method.The physicochemical properties, sPLA2-responsive drug release and anti-tumor activity were evaluated in vitro.The results indicated L-OHP loaded liposomes modified with FAs had similar particle sizes of approximately 100 nm and narrow size distributions (PDI < 0.11).Compared with non-FAs-containing liposomes (C-Lip), LCA-Lip or kLCA-Lip has a comparable entrapment efficiency and loading efficiency.LCA-Lip or kLCA-Lip didn't show significant higher drug leakage at the presence of 10% or 50% fetal bovine serum (FBS) in media than that in media without FBS.Treated with secretory phospholipase A2 from Colo205 cells culture conditioned medium (CCM sPLA2) for 24 h, FAs modified liposomes released about 70% of carboxyfluorescein (CF), while C-Lip only released 20% of CF.Compared to L-OHP loaded C-Lip, L-OHP-loaded FAs-included formulations had much greater anti-proliferative activity against sPLA2-secreting Colo205 cells.In summary, our results shows that LCA or kLCA promotes responsiveness of liposomes to tumor-related sPLA2 and points to a new way to develop platium drugs-loaded liposomal delivery systems with better release mechanisms.

Design, synthesis and anti-cervical cancer activity of novel trifluoromethyl chalcones derivatives / 中国药科大学学报

@#Chalcones are polyphenolic flavonoid substances with various pharmacological effects and low toxicity.In this study, 15 novel trifluoromethyl chalcone derivatives (3a-3o) were designed and synthesized using the chalcone nucleus of natural licorice chalcone as the lead compound skeleton in order to find the candidate drugs with high efficiency and low toxicity against cervical cancer.The structures of the target compounds were confirmed by 1H NMR, 13C NMR and HRMS. The inhibitory activities of compounds 3a-3o, licorice chalcone, cisplatin and Nutlin3a on SiHa, HeLa and C-33A human cervical cancer cells and H8 and HaCaT normal cells were determined by MTT assay, and the structure-activity relationship was analyzed.Transwell and flow cytometry methods were used to assess the target compounds'' ability to inhibit cell migration and invasion, promote apoptosis, and arrest the cell cycle.Molecular docking technology was used to further study the binding characteristics of the target compound with MDM2 protein.The results showed that the compounds had different degrees of inhibitory activity against the three types of cervical cancer cells.Compound 3n showed the strongest activity against HeLa cells (IC50 = 11.69 μmol/L), which was superior to the lead compound, and had lower toxicity against the two normal cells.Compound 3n was found to significantly inhibit the migration and invasion of HeLa cells, induce apoptosis and arrest the cell cycle at G2/M phase.The results of molecular docking showed that the effective binding of compound 3n to MDM2 protein may be one of its anti-tumor mechanisms.This study provides an experimental basis for the screening of new anti-cervical cancer candidate drug from chalcone derivatives.

Research on anti-tumor natural product diosgenin / 中国中药杂志

Diosgenin is widely distributed in many plants, such as Polygonatum sibiricum, Paris polyphylla, Dioscorea oppositifolia, Trigonella foenum-graecum, Costus speciosus, Tacca chantrieri, which has good anti-tumor activity and preferable effects on preventing atherosclerosis, protecting the heart, treating diabetes, etc. This review combed through the anti-tumor mechanisms of diosgenin encompassing lung, breast, gallbladder, liver, oral cavity, stomach, bladder, bone marrow, etc. Besides, it was discovered that diosgenin mainly exerts its effect by inhibiting tumor cell migration, suppressing tumor cell proliferation and growth, and inducing cell apoptosis. However, problems like low yield and bioavailability frequently exist in natural diosgenin. This review introduced methods such as structural modification, dosage form optimization and combination medication to improve the yield and anti-tumor activity of diosgenin. Via the summary of this paper, it is expected to provide theoretical basis for the rational exploitation and utilization of diosgenin.

Research progress of effective components of traditional Chinese medicine in anti-aging and anti-tumor mechanism / 药学学报

Increasing research have found a high correlation between senescence and tumor. Cellular senescence can inhibit tumorigenesis while the cellular microenvironment altered by senescent cells can promote the proliferation and metastasis of tumor cells. Some cellular signaling pathways are commonly involved in aging process and carcinogenesis. The deregulation and imbalance of these pathways results into senescence and tumor development. Thus, agents that balance these pathways may effective for anti-aging and anti-tumor. Traditional Chinese medicine (TCM) has been used for the activation of multiple signaling pathways and molecular targets both associated with aging and tumor, with few side effects. Therefore, the article reviewed the cellular signalings that cross between the aging and tumors, and on this basis, summarized the current effective components of TCM with anti-aging and anti-cancer properties, as well as the potential mechanisms of these components in the cross signalings, to provide new research strategies and perspectives for effective components of TCM to treat aging and tumors.

Preparation and anti-tumor activity of a novel antibody-drug conjugate 607-LDM / 药学学报

Antibody-drug conjugates (ADCs) are one of the most important classes of anticancer therapeutics. Human epidermal growth factor receptor-2 (HER2), which is highly expressed in many types of aggressive cancers including breast and ovarian cancer, has been approved as an ideal target for ADCs. Lidamycin (LDM), developed by Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, is an enediyne-containing antibiotic with potent anti-tumor activity. LDM is a promising payload for ADCs. In the present research, using a special site-directed conjugating technology, we made a novel ADC (607-LDM) with a drug-to-antibody ratio (DAR) of 2 and composed of the anti-HER2 antibody 607 and LDM. The new ADC exhibited potent antitumor activity against human ovarian cancer SKOV3 and breast cancer BT-474 cells. It also induced apoptosis and G2/M arrest. In nude mice with SKOV3 xenografts and a tumor volume of 150-200 mm3, a single intravenous injection 607-LDM at 1 mg·kg-1 induced tumor growth inhibition of 72.4%, which was significant compared to either LDM (50.6%) or antibody (30.2%) treatment alone, or both in combination (50.1%, P < 0.05). All animal experiments were performed in accord with National Regulations and approved by the Animal Experiments Ethical Committee of College of Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences. The novel ADC designed in this study, 607-LDM, is a promising candidate for the treatment of HER2-positive cancers.

Synthesis and antitumor activities of NO-donating rhein derivatives / 中国药科大学学报

@#Seven target compounds coupled by rhein and furoxan were synthesized and their chemical structures were confirmed by 1H NMR, IR, and MS. All target compounds were evaluated for anti-proliferative activity against human hepatoma cells HepG2 and Bel-7402, human colon cancer cells HCT116, human osteosarcoma cells U2OS, drug-resistant cells Bel-7402/5-FU and normal hepatocytes cells LO2 in vitro by thiazolyl blue(MTT) colorimetry. The results indicated that all target compounds had more potent anti-proliferative activity than their parent compound rhein. Additionally, compound 4g had stronger proliferation inhibitory activity on HepG2, Bel-7402, U2OS and Bel-7402/5-FU,with little effect on the proliferation of normal cells, exhibiting selective inhibitory activity. Griess assay was used to measure the release of nitric oxide in vitro. Results showed that compound 4g could increase the releases NO in HepG2 cells, which may be associated with its antitumor effects. Furthermore, the antitumor activity of compound 4g was attenuated by NO scavenger (hemoglobin), which indicates that the antitumor activity of compound 4g may be partly related to the release of NO.

Anti-tumor activity of tigecycline: a review / 生物工程学报

Tigecycline is a novel glycylcycline antibacterial drug, which shows both antibiotic function and anti-tumor activity. This review summarizes the single and combined use of tigecycline for tumor treatment and the underpinning mechanisms. As an inhibitor for mitochondrial DNA translation, tigecycline affects the proliferation, migration, and invasion of tumor cells mainly through inhibiting mitochondrial protein synthesis and inducing mitochondrial dysfunction. Although the effect of tigecycline monotherapy is controversial, the efficacy of combined use of tigecycline is satisfactory. Therefore, it is important to explore the molecular mechanisms underpinning the anti-tumor activity of tigecycline, with the aim to use it as a cheap and effective new anti-tumor drug.

Anti-tumor activities of endophytes from Cynanchum bungei Decne / 药学实践杂志

Objective To investigate the taxonomic structure and diversity of endophytic fungi from Cynanchum bungei Decne., explore the potential microbial resources and functions and provide the theoretical basis for new antitumor endophytic fungi. Methods The diversities of endophytic fungi community in different tissues, species and habitats were analyzed with traditional endophytic bacteria separation method and 18sRNA high-throughput sequencing technology. MTT assay was used to detect the cytotoxic activity of endophytic fungi from Radix Polygoni multiflori. Results 90 strains of endophytic fungi were isolated and identified from roots, stems, and leaves of C. bungei. Among them, Fusarium and Alternaria were the dominant genera. There were 8, 9 and 13 genera from roots, stems and leaves of C. bungei respectively. Among which Alternaria and Colletotrichum were the common genera in different tissues. Further studies showed that 13 endophytic fungi of C.bungei had good anti-tumor activity in vitro, accounting for 14.4% of the total genera. Among them, A. tenuissima LTJ2 and A. alternata LTJ6 had significant anti-tumor activity. Conclusion The endophytic fungi in Cynanchum bungei Decne. have rich diversity. Some strains have significant anti-tumor activity，which can be potential resources for the development of new antitumor agents.

Preliminary study on Q-markers of anti-tumor activity extracts of Polygonum orientale / 中草药

Objective: Based on the concept of quality marker (Q-marker), the components and the quality of the ethyl acetate extract of Polygonum orientale (POEa) was analyzed and studied. Methods: Firstly, the components of POEa were identified using the UPLC-ESI-HRMS method and standard compounds. Secondly, the main active compounds were determined by HPLC. Antitumor activities of these compounds were reviewed and its Q-marker was predicted. Finally, we evaluated the effects of POEa and the compound of gallic acid, isoquercetin, valerin, vitexin, luteolin, and quercetin on proliferation, apoptosis and migration of A549 cells. Results: A new quality method for simultaneous determining these six compounds of POEa was established. The six chemical ingredients were detected in each sample and the total content was more than 10%. The number of apoptotic cells in A549 cells treated with POEa and six chemical mixtures were all substantial increased, and the migration amount were significantly decreased. Tow groups showed no significantly differeances. Conclusion: The six components are scientific and reasonable to be considered as potential Q-marker represented the anti-tumor activity of POEa. The HPLC method can be used as accurate and stable quality control strategy of POEa.

Research progress of biological activity of Ipomoea batatas and its main components in vivo / 中草药

Ipomoea batatas is a kind of both edible and medicinal plant, which provides a dietary source of vitamins, minerals, carbohydrates, proteins, anthocyanins, essential fatty acids, trace elements and other nutrients, and these active substances play a role in many pharmacological activities such as antitumor, immune regulation, hepatoprotective effect, hypoglycemic, hypolipidemic, anti-aging, intestinal regulation, anti-obesity, anti-radiation, anti-fatigue, etc, and promote health in many aspects. The Dictionary of Traditional Chinese Medicine and Chinese Materia Medica recorded that I. batatas have the characteristics of tonifying deficiency and replenishing qi, strengthening spleen and kidney. In recent years, it has become a research hotspot in multidisciplinary fields for its rich nutritional components and functional characteristics. In this paper, the research progress of biological activity of I. batatas in vivo was reviewed from aspects of basic and clinical researches, which may provide references for its further development, research and comprehensive utilization.

Research progress on anti-tumor activity of curcumol and its derivatives / 中草药

Curcumol, as an important component of Curcuma Rhizoma, has anti-virus, anti-inflammatory, anti-tumor and other pharmacological activities, which has attracted more and more attentions in anti-tumor research area. The progress on the natural source, anti-tumor mechanism, structural modification, and anti-tumor evaluation of curcumol are reviewed in this paper, which will provide a novel strategy for its further structural optimization.

pH responsive docetaxel micelles with improved therapeutic efficacy on mice xenograft tumor / 药学学报

The non-specific administration of antitumor drugs is the main cause for the side effects of chemotherapy drugs on normal tissues. The application of nanotechnology in the delivery of anti-tumor drugs is one of the important ways to improve the therapeutic effect and to reduce the side effects. The current study aimed to synthesize pH responsive poly (methoxy-ethylene glycol)-poly(lactic acid)-poly-(β-amino ester) (PBAE) triblock copolymers to deliver docetaxel (DTX) and improve the anti-tumor activity of DTX. PBAE was synthesized by ring opening polymerization and Michael addition reaction, its structure and molecular weight was characterized by 1H NMR, the dissociation constant of base (pKb) were determined by acid-base titration method. The critical micelles concentration (CMC) of copolymers was measured by pyrene fluorescence spectroscopy. DTX loaded copolymer micelles were prepared by membrane hydration method. The size and its distribution as well as the stability of micelles were determined by laser light scattering analysis. The drug loading content (DL), entrapment efficiency (EE) and cumulative drug release from micelles were evaluated by high-performance liquid chromatography (HPLC). The sizes of DTX drug-loaded micelles were in the range of 10 to 100 nm with narrow distribution. DL of DTX in PBAE1 and PBAE2 micelles was (5.3 ± 0.10) % and (4.9 ± 0.05) %, respectively, with EE was (93.8 ± 1.70) % and (87.2 ± 4.10) %, respectively. The drug-loaded micelles showed pH sensitive drug release properties under weak acidic conditions, which showed potential drug release of DTX under mild acidic tumor environment. A mouse Lewis lung carcinoma model was established to evaluate the therapeutic efficacy of micellar DTX formulations. Significant inhibitory effect of the nanodrugs was observed with DTX dosages of 10 and 20 mg·kg-1, respectively. Moreover, the pH responsive PBAE1-DTX micellar drug exhibited stronger therapeutic efficacy on mice xenograft tumor, as compared with the non pH sensitive micellar drug (PELA-DTX) and free DTX. All animal experiments were performed according to the animal ethical standards and approved by the Animal Experiments and Ethical Committee of China Academy of Chinese Medical Sciences (No. 2017090110). The in vivo anti-tumor activity studies showed that the tumor volume growth rates of mice in different drug-administered groups were: PBAE1-DTX 20 mg·kg-1 < PBAE1-DTX 10 mg·kg-1 < PELA-DTX 10 mg·kg-1 < DTX 10 mg·kg-1 < normal saline, with the PBAE1-DTX group as the most potent group for tumor inhibition. The current pH sensitive DTX nano-micelles showed high potential in further studies to promote the application of nano DTX formulations for tumor treatment.

Chemical Constituents of Benzoinum and Its Anti-tumor Activities in Vitro / 中国实验方剂学杂志

Objective::To identify the active anti-tumor constituents of Benzoinum according to observation of the anti-tumor effect of chemical constituents from Benzoinum in vitro. Method::The 95%ethanol extract of Benzoinum was systematically separated by silica gel column chromatography, medium pressure liquid preparation chromatography and preparation liquid chromatography, and their structures were identified by physicochemical property and spectral data. Anti-tumor activities of the compounds of Benzoinum were screened by in vitro cells including human hepatoma cells in vitro (HepG2), human lung cancer cells (A549), human cervical cancer cells (HeLa), human breast cancer cells (MCF-7) and human prostate cancer cells (PC-3). Result::Fifteen compounds were isolated from Benzoinum and identified as myricadiol(1), 3-keto-oleanonic acid(2), (4E)-1, 5-bis(4-hydroxyphenyl)-1-methoxy-2-(methoxy-methyl)-4-pentene(3a and 3b), (E)-p-coumaryl alcohol γ-Ο-methyl ether(4), sesamin(5), 5-(3″benzoyloxypropyl)-7-methoxy-2-(3′, 4′-methylenedioxy phenyl)-benzofuran(6), dibutyl phthalate(7), methyl 4-hydroxy-3-methoxybenzoate(8), p-hydroxybenzaldehyde(9), p-hydroxyacetophenone(10), acetovanillone(11), 3-oxo-olean-11, 13(18)-dien-28, 19β-olide(12), vanillin(13), benzoic acid(14), and siaresinolic acid(15). Compounds 1 to 11 were isolated from the resin of Styrax tonkinensis for the first time. A part of these compounds had good anti-tumor activities. Among them, compound 2, 12 showed a strongest activity. Conclusion::The chemical constituents of Benzoinum have good prospects for the development and application of anti-tumor drugs.

Anti-tumor effect of new LL-37 hybrid antimicrobial peptide on breast cancer MCF-7 cells / 中国肿瘤生物治疗杂志

@#[Abstract] Objective:To investigate the anti-tumor effect and mechanism of new LL-37 hybrid peptide on breast cancer MCF-7 cells. Methods: Human antimicrobial peptide LL-37 and human neutrophil peptide 1(HNP-1) were screened by using of Antimicrobial Peptides Database (http:// aps.unmc.edu/AP/main.php). The new LL-37 hybrid peptide was synthesized by integrating the active fragments, which were selected by bioinformatics analysis. The breast cancer MCF-7 cells and human normal breast MCF10A cells were treated with the new LL-37 hybrid peptides (0~70 μmol/L). Cell viability was monitored by CCK-8 assay and the affinity of the new LL-37 hybrid peptide with MCF-7 cells was observed using confocal laser scanning microscope (CLSM). The effects of LL-37 and caspase inhibitor on apoptosis and cell cycle of MCF-7 cells were measured by FCM (flow cytometry). Results: The new LL-37 hybrid peptide, as an amphiphilic cationic polypeptide, could selectively inhibit the proliferation of breast cancer MCF-7 cells ( P <0.05) with an IC50of 58.34 μmol/L, but exerted no significant effect on normal breast MCF10A cells. LL-37 peptide had high affinity with MCF-7 cells, which could cause S-stage stagnation and significantly increased early apoptosis ( P <0.01); however, the cell cycle block and apoptosis were significantly attenuated after the treatment of caspase inhibitor ( P <0.01). Conclusion: The new LL-37 hybrid peptide has anti-tumor activity on breast cancer MCF-7 cells, and could induce MCF-7 cells apoptosis possibly by arresting cell cycle via the caspase-dependent signaling pathway.