Anti-Cancer, Anti-Oxidant and Anti-Inflammatory Effects of Herbacetin and Its Molecular Mechanisms

Rhodiola rosea,a perennial herb of the genus Rhodiola in the Crassulaceae family,is commonly used to treat depression,fatigue,cancer and cardiovascular diseases.Herbacetin is a natural flavonol compound extracted from R.rosea plant,with many pharmacological effects such as anti-cancer effect,anti-oxidant effect and anti-inflammatory effect.In this paper,the pharmacological effects and molecular mechanisms of herbacetin were summarized by consulting domestic and foreign literature,in order to provide a theoretical basis for the development and utilization of herbacetin.

Anti-Cancer Agents Associated Diarrhea:Current Status and Prospects

Cancer stands as one of the major threats to human life.Ensuring the safety of drugs is paramount,and the impact of adverse reactions on patients’quality of life and prognosis should not be underestimated.Diarrhea is a common clinical adverse event,and despite the absence of specific anti-diarrhea drugs,there is a pressing need for improvement.This article aims to provide a valuable reference for researchers in clinical drug use and scientific tumor treatment.It summarizes recent advancements in drug mechanisms and adverse reactions,whether in preclinical research or clinical diagnosis and therapy.

Anti-inflammatory and anti-cancer potential of pterostilbene:A review

Pterostilbene is a natural compound that can be found in various food plants such as blueberries,grapes,and peanuts.It has also been reported to be extracted from Pterocarpus indicus,a tree species native to India and Southeast Asia.Pterostilbene exhibits various pharmacological activities such as antioxidants,anti-proliferation,anti-microbial,and anti-inflammatory activities with favorable pharmacokinetic properties,such as high oral bioavailability and longer half-life.The anti-inflammatory effect of pterostilbene has been reported to contribute to its therapeutic effects in many chronic inflammatory diseases.Besides,pterostilbene has anti-cancer activity on various types of cancers due to its ability to induce cell cycle arrest and apoptosis.Hence,in this review,we discuss the anti-inflammatory and anti-cancer activities of pterostilbene in preclinical studies.

Exploring the anti-cancer effect of taraxasterol using network pharmacology, molecular docking and in vitro experimental validation

Taraxasterol(TS)is a naturally occurring pentacyclic triterpenoid extracted from the traditional Chinese herb Taraxacum mongolicum.Previous studies have highlighted its significant roles in exhibiting anti-inflammatory,anti-oxidant,and liver protective effects.In the present study,the anti-cancer potential of TS against cervical cancer was investigated,employing network pharmacology techniques,molecular docking,and in vitro experimental validation.TS exhibits its anticancer properties by modulating multiple targets,pathways,and biological processes.In vitro experiments demonstrated the potent inhibitory effects of TS on cancer cell growth and migration,while no significant impact on apoptosis was observed.The primary objective was to elucidate the anti-cancer potential of TS,which is a crucial lead compound in the treatment of cervical cancer.The findings may serve as a basis for the development of novel anticancer therapeutics and medicine-based interventions for cervical cancer.

Potential Anti-cancer Activity of Furanodiene

Objective： To study the isolated from the essential oil VIVO anti-tumor activities of furanodiene of the rhizome of Curcuma wenyujin （C15H200）, a primary sesquiterpene compound YH Chen et C. Ling（Wen Ezhu）, in vitro and in Methods： In vitro MTT assay was used to further study the effects of time and dosage on anti-proliferation of furanodiene against the sensitive Hela, Hep-2, HL-60, U251 cells, based on the cytotoxic effects of furanodiene on 12 human malignant tumor cell lines with the essential oil of Wen Ezhn as control., and the half-inhibitory concentration （IC50） was observed. In vivo uterine cervix （U14） tumor cell was selected and the conventional assay method of anti-tumor activity was employed. Furanodiene liposome was administered intraperitoneally, and tumor-inhibitory rate, thymus and spleen indexes were observed. Results： The inhibitive effects on cell proliferation were shown in all of the twelve cell lines and the cytotoxic effects of furanodiene against Hela, Hep-2, HL-60, U251 cells were observed after 12 h of administration, the effect could last for at least 48 h in a dose dependent manner, and the IC50 values were 0.6, 1.7, 1.8, 7.0μg/ml, respectively. Furanodiene was also found to show inhibitive effects on the proliferation of uterine cervix （U14） tumor induced in mice. The tumor inhibition rates were 36.09% （40 mg/kg）, 41.55% （60 mg/kg）, 58.29% （80 mg/kg）, respectively. Conclusion： Furanodiene is one of primary anti-cancer active components in the essential oil of Wen Ezhu, and also a very effective agent against uterine cervix cancer, and has protection effect on the immune function.

Anti-cancer effect of ethylacetate fraction from Orostachys japonicus on HT-29 human colon cancer cells by induction of apoptosis through caspase-dependent signaling pathway

Objective: To investigate the anti-colon cancer effects of ethylacetate fraction from Orostachys japonicus(0. japonicus) on HT-29 cancer cells. Methods: The viability of HT-29 cells was assayed by the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2 H-tetrazolium(MTS) method. Apoptosis induction and cell cycle inhibition were confirmed by fluorescein isothiocyanate and propidium iodide staining using flow cytometry.Morphological changes in the nucleus were observed, using a fluorescence microscope with4',6-diamidino-2-phenylindole(DAPI) nuclear staining. The expression levels of the upstream and downstream proteins involved in the anti-cancer mechanism were confirmed by Western blotting. Results: After treating HT-29 cells with different concentrations of ethylacetate fraction from O. japonicus, the viability of cells decreased in a concentration-dependent manner,while apoptosis induction and apoptotic body formation increased. Cell cycle analysis showed that the arrest occurred at the sub-G_1 and S phase. Among the upstream and downstream proteins involved in anti-cancer activity, the level of B cell lymphoma-2 decreased, and the bcl-2-associated x protein increased. The level of pro-caspase-3, pro-caspase-8, and pro-caspase-9 decreased, while the level of cleaved-caspase-3, cleaved-caspase-8, and cleaved-caspase-9 increased. Moreover, the phosphorylation, that is, activation of extracellular signal regulated kinase 1/2, Jun-N-terminal kinase, and p38 increased. Conclusions: Combining the above results, it is thought that the survival of HT-29 cells is suppressed by ethylacetate fraction from0. japonicus through mitochondrial regulation-induced caspase cascade activation, induction of apoptosis and cell cycle arrest.

Efficacy of Yiqi Jianpi anti-cancer prescription combined with chemotherapy in patients with colorectal cancer after operation

BACKGROUND At present,colorectal cancer is routinely treated with adjuvant radiotherapy and chemotherapy postoperatively.The adverse effects(AEs)of chemotherapy usually interrupt the treatment of chemotherapy.Traditional Chinese medicine(TCM)has demonstrated great potential in improving patients'clinical symptoms,regulating the immune function,improving the life quality,and reducing the AEs of chemotherapy.AIM To observe the clinical efficacy of Yiqi Jianpi anti-cancer prescription combined with chemotherapy in patients with colorectal cancer after operation.METHODS Data from patients diagnosed with colorectal cancer between January 2019 and February 2021 were collected from Liaoning Cancer Hospital and Institute and the Second Affiliated Hospital of Liaoning University of Traditional Chinese Medicine.Patients receiving the chemotherapy regimen of capecitabine plus oxaliplatin(CAPOX)after radical resection of colorectal cancer were prospectively collected and randomly divided into an experimental group and a control group.The experimental group was given Yiqi Jianpi anti-cancer prescription combined with the CAPOX regimen,while the control group was given the CAPOX regimen alone.After six cycles of chemotherapy,the scores of TCM symptoms,Karnofsky performance scale(KPS)score,levels of T-cell subsets,and AEs after chemo therapy of the two groups were compared.RESULTS A total of 70 patients were randomly divided into either an experimental group(n=35,no dropout)or a control group(n=33,with 2 dropouts).Compared with the control group,the experimental group improved significantly(P<0.05)in scores of TCM symptoms,KPS score,levels of T-cell subsets,and AEs of chemotherapy.CONCLUSION Yiqi Jianpi anti-cancer prescription can effectively improve spleen deficiency,regulate the immune function,and alleviate the AEs of chemotherapy,so as to improve the life quality of patients with good therapeutic effects and application prospect in clinical practice.

Quantitative Structure Anti-Cancer Activity Relationship (QSAR) of a Series of Ruthenium Complex Azopyridine by the Density Functional Theory (DFT) Method

A series of ruthenium azopyridine complexes have recently been investigated due to their potential cytotoxic activities against renal cancer (A498), lung cancer (H226), ovarian cancer (IGROV), breast cancer (MCF-7) and colon cancer (WIDR). Thus, in order to predict the cytotoxic potentials of these compounds, quantitative structure-activity relationship studies were carried out using the methods of quantum chemistry. Five Quantitative Structure Activity Relationship (QSAR) models were obtained from the determined quantum descriptors and the different activities. The models present the following statistical indicators: regression correlation coefficient R2 = 0.986 - 0.905, standard deviation S = 0.516 - 0.153, Fischer test F = 106.718 - 14.220, correlation coefficient of cross-validation = 0.985- 0.895 and = 0.010 - 0.001. The statistical characteristics of the established QSAR models satisfy the acceptance and external validation criteria, thereby accrediting their good performance. The models developed show that the variation of the free enthalpy of reaction , the dipole moment μ and the charge of the ligand in the complex Ql, are the explanatory and predictive quantum descriptors correlated with the values of the anti-cancer activity of the studied complexes. Moreover, the charge of the ligand is the priority descriptor for the prediction of the cytotoxicity of the compounds studied. Furthermore, QSAR models developed are statistically significant and predictive, and could be used for the design and synthesis of new anti-cancer molecules.

Sesamum indicum(sesame) enhances NK anti-cancer activity, modulates Th1/Th2 balance, and suppresses macrophage inflammatory response

Objective:To evaluate the potential immunomodulatory effects of an aqueous extract of Sesamum indicum seeds with regard to splenocyte proliferation,Th1/Th2 balance,macrophage function,and the cytotoxic activity of natural killer(NK)cells.Methods:Splenocyte proliferation was measured by[~3H]-thymidine incorporation.Griess assay was performed to evaluate the production of nitric oxide by macrophages.The levels of cytokines secreted by splenocytes and macrophages were measured by ELISA.JAM assay was performed to examine the cytotoxic activity of NK cells against YAC-1 tumor cells.Results:Sesamum indicum significantly enhanced splenocyte proliferation in a dose-dependent manner.Sesamum indicum also increased and suppressed the secretion of Th1 and Th2 cytokines,respectively,by splenocytes.The secretion of key pro-inflammatory mediators(IL-6,TNFα,and nitric oxide)by primary macrophages was significantly inhibited by Sesamum indicum.Moreover,Sesamum indicum increased the cytotoxic activity of NK cells against YAC-1 tumor cells.Conclusions:Sesamum indicum shows potent immunomodulatory,anti-inflammatory,and anti-cancer effects.Constituents of Sesamum indicum may be used as effective therapeutic agents in regulating immune reactions implicated in various infectious and noninfectious conditions including cancer.

Anti-cancer activity of an ethyl-acetate extract of the fruits of Terminalia bellerica(Gaertn.)Roxb.through an apoptotic signaling pathway in vitro

Objective:To investigate the biochemical constituents of the fruits of Terminalia bellerica(Gaertn.)Roxb.(hereafter termed T.bellerica)and estimate the anti-cancer activity of different polar extracts.Methods:To rapidly screen and identify the biochemical constituents of ethyl acetate(EA)extracts of T.bellerica,ultra performance liquid chromatography-electrospray ionization/mass spectrometry(UPLC-ESI-MSn)was done.The CellTiter-BlueTM cell-viability assay was used to ascertain the anti-cancer activity of different polar extracts in 10 human cancer cell lines.Results:Forty polyphenols of the EA extract of T.bellerica were characterized tentatively.The EA extract exhibited significant anti-cancer activity against ZR-75-1 cells(half-maximal inhibitory concentration=27.33(0.98)μg/mL)and Colo-205 cells(39.65(2.99)μg/mL)in vitro.Treatment of ZR-75-1 cells with 20 and 60μg/mL of the EA extract elicited dosedependent apoptosis percentages at an early stage of 17.58(0.74)%and at a late stage of 29.20(1.22)%;Colo-205 cells at the same concentration of EA extract had values of 21.33(1.03)%and 40.55(0.34)%,respectively.Western blotting suggested that ZR-75-1 and Colo205 cells treated with the EA extract showed a similar increasing tendency for expression of cleaved anti-poly adenosine diphosphate ribose polymerase I.Conclusion:We identified a total of 40 chemical constituents,of which 11 were first obtained from the Terminalia Linn.genus using UPLC-ESI-MSn.Meanwhile,we observe that the EA extract of T.bellerica possesses anti-cancer activity,especially against breast and colon cancers.

In vitro antioxidant and anti-cancer activities and phytochemical analysis of Commelina benghalensis L. root extracts

Objective:To explore antioxidant potential,anti-cancer activity,and phytochemicals of Commelina benghalensis L.Methods:The roots of Commelina benghalensis were extracted in different solvents(methanol,ethanol,benzene,chloroform,n-hexane)with a range of polarity.Antioxidant activity was evaluated by reducing power assay,DPPH radical scavenging activity and phosphomolybdenum method,cytotoxicity by MTT assay,apoptotic and cell cycle analysis by flow cytometry,migratory and invasive potential by wound scratch assay and invasion assay,respectively,functional groups analysis by FT-IR spectroscopy and phytochemicals by aluminum chloride colorimetric and FolinCiocalteu methods.Results:The extracts showed worthy antioxidant potential.The chloroform extract demonstrated the most significant cytotoxic effect on MDA-MB-231(breast cancer)cell line,induced apoptosis and reduced migratory and invasive potential of MDA-MB-231 cells.Methanol and ethanol extracts presented good yield of total phenolic and total flavonoid contents.The FTIR spectroscopic studies revealed different characteristic peak values with various functional compounds such as alkenes,alkanes,aliphatic amines,aromatics,alkyl halides,carboxylic acid,alcohols,ester,aldehydes and ketones.Conclusions:The results demonstrate the potential use of Commelina benghalensis as a good antioxidant with significant anticancer effect.

Machine Learning Prediction for 50 Anti-Cancer Food Molecules from 968 Anti-Cancer Drugs

Cancer-beating molecules (CBMs) are abundant in many types of food and potentially anti-cancer therapeutic agents. In the previous work, researchers introduced a network-based machine learning platform to identify the cancer-beating molecules, for example,?comparing the similarities in the molecular network between approved anticancer drug and food molecules. Herein, we aim to build on this work to enhance the accuracy of predicting food molecules. In this project, we improve supervised learning approaches by applying Soft Voting algorithm to seven machine learning algorithms: Support Vector Machine with Radial Basis Function (SVM with RBF kernel), multilayer perceptron neural network?(MLP), Random forest, Decision trees,?Gaussian Naive Bayes, Adaboosting, and Bagging. As a result, the accuracy in the dataset of 50 food molecules utilized increased from 82% to 87%, achieving a significant improvement in the precision of?predicting anti-cancer molecules.

Microfluidics:Emerging prospects for anti-cancer drug screening

Cancer constitutes a heterogenic cellular system with a high level of spatio-temporal complexity.Recent discoveries by systems biologists have provided emerging evidence that cellular responses to anti-cancer modalities are stochastic in nature.To uncover the intricacies of cell-to-cell variability and its relevance to cancer therapy,new analytical screening technologies are needed.The last decade has brought forth spectacular innovations in the field of cytometry and single cell cytomics,opening new avenues for systems oncology and high-throughput real-time drug screening routines.The up-and-coming microfluidic Lab-on-a-Chip(LOC)technology and micrototal analysis systems(μTAS)are arguably the most promising platforms to address the inherent complexity of cellular systems with massive experimental parallelization and 4D analysis on a single cell level.The vast miniaturization of LOC systems and multiplexing enables innovative strategies to reduce drug screening expenditures while increasing throughput and content of information from a given sample.Small cell numbers and operational reagent volumes are sufficient for microfluidic analyzers and,as such,they enable next generation high-throughput and high-content screening of anticancer drugs on patient-derived specimens.Herein we highlight the selected advancements in this emerging field of bioengineering,and provide a snapshot of developments with relevance to anti-cancer drug screening routines.

HPLC Method Research of Picoplatin-a New Platinum Anti-cancer Drug and Its Impurities

Purpose: To establish a HPLC testing method of the content of bulk picoplatin and its impurities. Method: the separation was perform on a C18 column(4.6 mm×250 mm, 5 m) with potassium dihydrogen phosphate-aceton-itrile as the mobile phase at a flow rate of 1.0 mL/min. The detecting wavelength was set at 210 nm, and the column temperature was set at 30℃. Result: in the method validation, the linear relationship modulus of picoplatin is 0.9999, the systemic precision is 0.44%, the method precision is 0.74%, the average recovery rate is 99.62%, the LOD and LOQ of picoplatin is 0.2 ng and 1.0 ng. The average resolution of picoplatin and its impurities is more than 2. Conclusion: The established method is good specificity, high sensitivity, and good repeatability which could provide scientific evidence for the quality control of picoplatin and its impurities.

Anti-hemolytic, antibacterial and anti-cancer activities of methanolic extracts from leaves and stems of Polygonum odoratum

Objective: To investigate anti-hemolytic, antibacterial and anti-cancer activities of leaf and stem extracts from Polygonum odoratum. Methods: Leaves and stems of Polygonum odoratum were extracted using methanol and their anti-hemolytic activity was assessed using 2, 2′-Azobis(2-methylpropionamidine) dihydrochloride which is known to generate free radical damage on cell membranes of red blood cells. This damage, represented by hemolysis, was measured using spectrophotometry. Antibacterial activity was tested by using a broth microdilution method to find minimal inhibitory concentrations against eight bacterial strains. Anti-cancer activity of the extracts was evaluated against a human promyelocytic leukemic cell line(HL-60) by using MTT assay for cell viability and flow cytometry for apoptosis induction and cell cycle analysis. Results: Both leaf and stem extracts have anti-hemolytic activity. The results showed a significantly increased percentage of inhibition in a concentration-dependent manner. Interestingly, the leaf extract showed anti-hemolytic activity to a greater extent than the stem extract. Antibacterial activity of the extracts, as indicated by their minimal inhibitory concentration, using 12.5, 50, 25, 25 μg/mL, was measured against Staphylococcus epidermidis, Enterococcus faecium, Enterococcus faecalis and Staphylococcus aureus. The leaf extracts also exhibited anti-cancer activity, demonstrated by significantly decreased cell viability of human promyelocytic cells(HL-60), with an IC_(50) of(350.00±1.85) μg/mL for 48 h and(38.00±0.92) μg/mL for 72 h. Additionally, HL-60 became apoptotic and accumulated in G_1-phase after 48 hours of treatment. Conclusions: The extracts of Polygonum odoratum exhibit potential antihemolytic activity. They also have antibacterial activity by inhibiting growth of Gram-positive bacteria. The leaf extract shows anti-cancer activity against HL-60 to a greater extent than the stem extract, causing decreased viability, increased G_1-phase accumulation and apoptosis induction.

Chinese Anti-Cancer Association as a non-governmental organization undertakes systematic cancer prevention work in China

Cancer has become the first leading cause of death in the world, particularly in low- and middle-income countries. Facing the increasing trend of cancer incidence and mortality, China issued and implemented ＂three-early（early prevention, early diagnosis and early treatment）＂ national cancer prevention plan. As the main body and dependence of social governance, non-governmental organizations（NGOs） take over the role of government in the field of cancer prevention and treatment. American Cancer Society（ACS） made a research on cancer NGOs and civil society in cancer control and found that cancer NGOs in developing countries mobilize civil society to work together and advocate governments in their countries to develop policies to address the growing cancer burden. Union for International Cancer Control（UICC）, Cancer Council Australia（CCA）, and Malaysian cancer NGOs are the representatives of cancer NGOs in promoting cancer control. Selecting Chinese Anti-Cancer Association（CACA） as an example in China, this article is to investigate how NGOs undertake systematic cancer prevention work in China. By conducting real case study, we found that, as a NGO, CACA plays a significant role in intensifying the leading role of government in cancer control, optimizing cancer outcomes, decreasing cancer incidence and mortality rates and improving public health.

Advances in Research on Anti-cancer Mechanism of 18β Glycyrrhetinic Acid

Glycyrrhiza uralensis Fisch has been used to treat the symptoms of organ fever, food poisoning, typhoid fever, sore throat, cough due to lung heat, children's diseases and so on since the ancient times. It is a solid Chinese herbal medicine which is good for the health. In recent years, it has been found that licorice extract also has excellent anti-cancer effect. The 18β glycyrrhetinic acid, obtained by hydrolysis of precursor glycyrrhizic acid, is a relatively efficient anti-cancer ingredient. 18β glycyrrhetinic acid can exert anti-cancer effects by inhibiting cancer cell proliferation, inducing apoptosis of cancer cells, inhibiting invasion and metastasis of cancer cells, preventing oxidation, inhibiting neovascularization, inhibiting lymphangiogenesis, and regulating hormone secretion. This paper reviewed the advances in research of the anticancer mechanism of 18β glycyrrhetinic acid, to provide a theoretical basis for future research.

EXPERIMENTAL RESEARCH ON THE ANTI-CANCER IMMUNOMODULA-TIVE EFFECT OF THE POLYSOCOHARIBE-PEPTIDE OF CORIOLUS VERSICOLOR

Polysocoharibe-peptide of Coriolus Versicolor (PSP) is a new anti-cancer immunomodulative drug. The present paper reports on the experimental research done with this drug. It was found that PSP had the ability to recover hemolysin HC50, to increase the weight of the thymus, and increase the alexin of serum C3 and the IgG content of tumor bearing mice. FSP also significantly raised the pha-gocytic activity of macrophages in normal mice. PSP had a significant inhibitory effect on P38S and S180 cells. At the concentration of 1 mg/ml, PSP inhibited the proliferating activity of some human tumor call lines, such as SGC 7901, SPC, SLY and Mei. It had a direct toxic effect on SPC cells. PSP significantly inhibited the synthesis of nucleic acids of Ehrlich ascites carcinoma cells. In addition, PSP was antagonistic to the side effects of chemotherapy and radiotherapy.

The anti-cancer effect of Huaier aqueous extract with rh-Endostatin and DDP

Objective: The aim of our study was to explore the inhibition and apoptosis-inducing effect of the combination of Huaier aqueous extract with recombinant human Endostatin and DDP in human lung adenocarcinoma A549 cells. We also investigated the reversal effect of Huaier aqueous extract in reversing cisplatin resistance in human lung adenocarcinoma A549/DDP cells. Methods: We treated A549 cells with Huaier aqueous extract and the combination of Huaier aqueous extract and DDP or rh-Endostatin for 24 h, 36 h and 48 h. And then we calculated the inhibition rate through MTT approach and detected the apoptosis rate by flow cytometry. We also treated A549 and A549/DDP cells with DDP, Huaier aqueous extract, DDP and Huaier aqueous extract for 72 h, respectively. Results: Huaier aqueous extract can inhibit the growth of A549 cells and the inhibition rate improved with the increase of the concentration. The inhibition rate of the combination of rh-Endostatin and 4 mg/mL of Huaier aqueous extract in three time points and the combination of rh-Endostatin and 2 mg/mL of Huaier aqueous extract in the time point of 48 h on the growth of A549 cells all improved(P < 0.005). The inhibition rate of the combination of DDP and Huaier aqueous extract with the concentration of 2 mg/mL or 4 mg/mL on the growth of A549 cells all improved(P < 0.005). The combination of Huaier aqueous extract and DDP and the combination of Huaier aqueous extract with rh-Endostatin and DDP can improve the inhibition on the growth of A549 cells(P < 0.005). Conclusion: Huaier aqueous extract has the inhibition and apoptosis-inducing effects on the A549 cells. And the combination of Huaier aqueous extract and rh-Endostatin or DDP has the synergistic effects on the inhibition of A549 cells. The combination of Huaier aqueous extract with rh-Endostatin and DDP has the synergistic effects on the inhibition of A549 cells. Huaier aqueous extract can reverse the cisplatin resistance in human lung adenocarcinoma A549/DDP cells.