Displaying publications 21 - 40 of 129 in total

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  1. Antitumour activity of Sargassum wightii (Greville) extracts against Dalton's ascites lymphoma
    Rajan DS, Rajkumar M, Srinivasan R, Harikumar RP, Suresh S, Kumar S
    Pak J Biol Sci, 2013 Nov 01;16(21):1336-41.
    PMID: 24511743
    Seaweeds have been used by mankind as medicine and food for more than 13,000 years. Marine algae are considered to produce a valuable phytoconstituents characterized by a broad spectrum of antitumor activities. The aim of the present study was to explore the effect of different solvent extracts of Sargassum wightii, Greville against Dalton's Ascitic Lymphoma (DAL) in Swiss male albino mice. DAL cells were injected intraperitoneally 1 x10(6) cell to the mice. Two days after cells injection the animals were treated with different solvent extracts of Sargassum wightii at dose of 200 mg kg(-1) for 14 days. 5-fluorouracil (20 mg kg(-1)) was used as reference drug. On day 11, cancer cell number, packed cell volume, decrease in tumour weight of the mice, increase in life span and hematological parameters were evaluated and compared with the same parameters in control. A significant increase in the life span and a decrease in the cancer cell number and tumour weight were noted in the tumour-induced mice after treatment with the extract. The haematological parameters were also normalized by the ethanolic and chloroform extracts in tumour-induced mice. These observations are suggestive of the protective effect of ethanolic extract of Sargassum wightii is comparatively better than other two tested extracts against Dalton's Ascitic Lymphoma (DAL).
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry*
  2. Leucophyllidine, a cytotoxic bisindole alkaloid constituted from the union of an eburnan and a new vinylquinoline alkaloid
    Gan CY, Robinson WT, Etoh T, Hayashi M, Komiyama K, Kam TS
    Org. Lett., 2009 Sep 3;11(17):3962-5.
    PMID: 19708704 DOI: 10.1021/ol9016172
    A cytotoxic bisindole alkaloid possessing an unprecedented structure constituted from the union of an eburnan half and a novel vinylquinoline alkaloid has been isolated from Leuconotis griffithii. The structure was established by analysis of the spectroscopic data and confirmed by X-ray diffraction analysis. A possible biogenetic pathway to the novel quinolinic coupling partner is presented from an Aspidosperma precursor.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  3. A new chromanone acid from the stem bark of Calophyllum teysmannii
    Lim CK, Subramaniam H, Say YH, Jong VY, Khaledi H, Chee CF
    Nat Prod Res, 2015;29(21):1970-7.
    PMID: 25716662 DOI: 10.1080/14786419.2015.1015020
    A new chromanone acid, namely caloteysmannic acid (1), along with three known compounds, calolongic acid (2), isocalolongic acid (3) and stigmasterol (4) were isolated from the stem bark of Calophyllum teysmannii. All these compounds were evaluated for their cytotoxic and antioxidant activities in the MTT and DPPH assays, respectively. The structure of compound 1 was determined by means of spectroscopic methods including 1D and 2D NMR experiments as well as HR-EIMS spectrometry. The stereochemical assignment of compound 1 was done based on the NMR results and X-ray crystallographic analysis. The preliminary assay results revealed that all the test compounds displayed potent inhibitory activity against HeLa cancer cell line, in particular with compound 1 which exhibited the highest cytotoxic activity comparable to the positive control used, cisplatin. However, no significant antioxidant activity was observed for all the test compounds in the DPPH radical scavenging capacity assay.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry*
  4. Calophyllum inophyllum and Calophyllum soulattri source of anti-proliferative xanthones and their structure-activity relationships
    Mah SH, Ee GC, Teh SS, Sukari MA
    Nat Prod Res, 2015;29(1):98-101.
    PMID: 25229947 DOI: 10.1080/14786419.2014.959949
    Extensive chromatographic isolation and purification of the extracts of the stem bark of Calophyllum inophyllum and Calophyllum soulattri have resulted in 11 xanthones. C. inophyllum gave inophinnin (1), inophinone (2), pyranojacareubin (5), rheediaxanthone A (6), macluraxanthone (7) and 4-hydroxyxanthone (8), while C. soulattri afforded soulattrin (3), phylattrin (4), caloxanthone C (9), brasixanthone B (10) and trapezifolixanthone (11). The structures of these compounds were determined on the basis of spectroscopic analyses such as 1D and 2D NMR, GC-MS, IR and UV. Cytotoxicity screening (MTT assay) carried out in vitro on all the xanthones using five human cancer cell lines indicated good activities for some of these xanthones. The structure-activity relationship study revealed that the inhibitory activities exhibited by these xanthone derivatives to be closely related to the existence and nature of the pyrano and the prenyl substituent groups on their skeleton.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry*
  5. A new triterpenoid from Sapium baccatum (Euphorbiaceae)
    Al Muqarrabun LM, Ahmat N, Aris SR, Norizan N, Shamsulrijal N, Yusof FZ, et al.
    Nat Prod Res, 2014;28(13):1003-9.
    PMID: 24697194 DOI: 10.1080/14786419.2014.903396
    A new triterpene, malaytaraxerate (1), and four known compounds, taraxerol (2), taraxerone (3), docosyl isoferulate (4) and docosanoic acid 2',3'-dihydroxypropyl ester (5), were isolated from the acetone extract of Sapium baccatum stem bark. The structures of the isolated compounds were determined using several spectroscopic methods, including UV-Vis, FT-IR, 1D and 2D NMR, and mass spectrometry. Major isolated compounds were assayed for cytotoxicity. The chemotaxonomic significance of this plant was also studied.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  6. A new sesquiterpenoid from Scaphium macropodum (Miq.) Beumee
    Al Muqarrabun LM, Ahmat N, Aris SR, Shamsulrijal N, Baharum SN, Ahmad R, et al.
    Nat Prod Res, 2014;28(9):597-605.
    PMID: 24568340 DOI: 10.1080/14786419.2014.886211
    A new sesquiterpenoid, malayscaphiol (1), and three known compounds, lupeol (2), lupenone (3) and stigmasterol (4), were isolated from the methanolic extract of the stem bark of Scaphium macropodum. The structures of the isolated compounds were determined using several spectroscopic methods, including UV-vis, FT-IR, 1D and 2D NMR, and mass spectrometer. Major isolated compounds were assayed for cytotoxicity and anti-acetylcholinesterase activities. The chemotaxonomy significance of this plant was also discussed.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  7. Bioactive sesquiterpenes from Curcuma ochrorhiza and Curcuma heyneana
    Aspollah Sukari M, Wah TS, Saad SM, Rashid NY, Rahmani M, Lajis NH, et al.
    Nat Prod Res, 2010 May;24(9):838-45.
    PMID: 20461629 DOI: 10.1080/14786410903052951
    Curcuma ochrorhiza ('temu putih') and C. heyneana ('temu giring') are two Zingiberaceous species which are commonly used in traditional medicine in Malaysia and Indonesia. Phytochemical investigations on these Curcuma species have resulted in the isolation of six sesquiterpenes, namely zerumbone (1), furanodienone (2), zederone (3), oxycurcumenol epoxide (4), curcumenol (5) and isocurcumenol (6), along with phytosterols stigmasterol and alpha-sitosterol. Compounds 1 and 2 were obtained for the first time for C. ochrorhiza while 4 was new to C. heyneana. The hexane extract of C. ochrorhiza and sesquiterpenes 1 and 3 showed very strong cytotoxicity activity against T-acute lymphoblastic leukaemia cells (CEM-SS), with IC(50) values of 6.0, 0.6 and 1.6 microg mL(-1), respectively. Meanwhile, constituents from C. heyneana (4-6) demonstrated moderate inhibition against CEM-SS in cytotoxic assay, with IC(50) values of 11.9, 12.6 and 13.3 microg mL(-1), respectively. The crude extracts and sesquiterpenes isolated were moderately active against certain bacteria tested in antimicrobial screening.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry*
  8. Furoquinoline alkaloids from Melicope bonwickii (F.Muell.) T.Hartley
    Komala I, Rahmani M, Sukari MA, Mohd Ismail HB, Cheng Lian GE, Rahmat A
    Nat Prod Res, 2006 Apr;20(4):355-60.
    PMID: 16644530
    Investigation on the leaves of Melicope bonwickii (F.Muell.) T.Hartley (Rutaceae) afforded a new 7-(2'-hydroxy-3'-chloroprenyloxy)-4-methoxyfuroquinoline (1) together with the known 7-(2',3'-epoxyprenyloxy)-4-methoxyfuroquinoline (2), evellerine (3) kokusaginine (4) and an amide aurantiamide acetate (5). Compounds 1 and 2 showed significant activity against cervical cell lines (Hela).
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  9. A new cycloartane triterpene bisdesmoside from the rhizomes of Actaea vaginata
    Zhang M, Yang Q, Zhang X, Wu H
    Nat Prod Res, 2021 Oct;35(20):3426-3431.
    PMID: 31821060 DOI: 10.1080/14786419.2019.1700509
    A new cycloartane triterpene bisdesmoside, soulieoside T (1), and one known compound, oleanolic acid (2), were isolated from the ethanolic extract of the rhizomes of Actaea vaginata. Their structures were elucidated by spectroscopic methods and by comparison with data reported in the literature. Compound 1 was evaluated for cytotoxic activities against three human cancer cell lines.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  10. Essential oil composition, cytotoxic and antibacterial activities of five Etlingera species from Borneo
    Vairappan CS, Nagappan T, Palaniveloo K
    Nat Prod Commun, 2012 Feb;7(2):239-42.
    PMID: 22474969
    Essential oils obtained by hydrodistillation from the rhizomes of Etlingera pyramidosphaera (K. Schum.) R. M. Sm, E. megalocheilos (Griff.) A.D. Poulsen, comb. nov., E. coccinea (Blume) S. Sakai & Nagam, E. elatior (Jack) R. M. Sm, and E. brevilabrum (Valeton) R. M. Sm were analyzed by GCMS. The highest oil yield was obtained from E. pyramidosphaera (0.45%), followed by E. elatior (0.38%), E. coccinea (0.30%), E. brevilabrum (0.28%) and E. megalocheilos (0.25%). The major constituents of the essential oils were oxygenated monoterpenes, followed by sesquiterpenes, oxygenated sesquiterpenes, oxygenated diterpenes and diterpenes. The essential oils from E. pyramidosphaera and E. brevilabrum exhibited the best cytotoxicity against MCF 7 (LC50: 7.5 +/- 0.5 mg mL(-1)) and HL 60 (LC50: 5.0 mg mL(-1)), respectively. Strong inhibition was also observed for the essential oils of E. coccinea and E. megalocheilos against Staphylococcus aureus (MIC: 8.0 +/- 0.5 mg mL(-1), and 5.0 +/- 0.5 mg mL(-1)) and Streptococcus pyrogenes (MIC: 6.0 +/- 0.5 mg mL(-1) and 8.0 +/- 0.5 mg mL(-1)).
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  11. Two new naphthoquinone derivatives from the stem bark of Callicarpa maingayi
    Asiri SM, Shaari K, Abas F, Al-Mekhlafi NA, Lajis NH
    Nat Prod Commun, 2012 Oct;7(10):1333-6.
    PMID: 23157003
    Two new naphthoquinones designated as 3alpha-hydroxy-2-(2-hydroxypropan-2-yI)-9alpha-methoxy-2,3,3alpha,9alpha-tetra-hydronaphtho[2,3-b]furan-4,9-dione (callicarpa-quinone A, 1) and 5-hydroxy-2-(2-hydroxypropan-2-yl)naphtho[2,3-b]furan-4,9-dione (callicarpaquinone B, 2) were isolated from the chloroform fraction of Callicarpa maingayi. Three other known compounds, identified as avicequinone-C (3), wodeshiol (4) and paulownin (5), were reported for the first time from this species. The structure elucidation of compounds was established by comprehensive 1D and 2D NMR spectroscopic analyses as well as EIMS, UV and IR spectral data. Compounds 1 and 2 were tested in vitro for their cytotoxic activity against human breast cancer MCF-7cells. Compound 2 exhibited strong cytotoxic activity with an IC50 value of 1.9 +/- 0.2 microM, while 1 showed moderate activity with an IC50 value of 25.0 +/- 4.3 microM.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry*
  12. Cytotoxic Aporphines from Artabotrys crassifolius
    Kwan TK, Shipton F, Azman NS, Hossan S, Jin KT, Wiart C
    Nat Prod Commun, 2016 Mar;11(3):389-92.
    PMID: 27169188
    Artabotrys crassifolius Hook. f. & Thomson is a medicinal plant used in Malaysia. The cytotoxic effects of the hexane, chloroform and ethanol extracts of the leaves and bark were examined in vitro against MCF-7, MDA-468 and HCT-116 cells. The chloroform extract of the bark inhibited the growth of all cell lines with GI₅₀ values ranging from 4.2 µg/mL to 9.4 µg/mL. Silica gel column chromatography of this extract yielded artabotrine, liridine, atherospermidine and lysicamine. Artabotrine and lysicamine inhibited the growth of HCT-116 and MCF-7 cells with GI₅₀ values ranging from 3.3 µM to 3.9 µM. These alkaloids were not toxic to human embryonic kidney cells (HEK297) up to a concentration of 50 µg/mL.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry*
  13. Papain grafted into the silica coated iron-based magnetic nanoparticles 'IONPs@SiO2-PPN' as a new delivery vehicle to the HeLa cells
    Nasiri R, Dabagh S, Meamar R, Idris A, Muhammad I, Irfan M, et al.
    Nanotechnology, 2020 May 08;31(19):195603.
    PMID: 31978907 DOI: 10.1088/1361-6528/ab6fd4
    The present study aims at engineering, fabrication, characterization, and qualifications of papain (PPN) conjugated SiO2-coated iron oxide nanoparticles 'IONPs@SiO2-PPN'. Initially fabricated iron oxide nanoparticles (IONPs) were coated with silica (SiO2) using sol-gel method to hinder the aggregation and to enhance biocompatibility. Next, PPN was loaded as an anticancer agent into the silica coated IONPs (IONPs@SiO2) for the delivery of papain to the HeLa cancer cells. This fabricated silica-coated based magnetic nanoparticle is introduced as a new physiologically-compatible and stable drug delivery vehicle for delivering of PPN to the HeLa cancer cell line. The IONPs@SiO2-PPN were characterized using FT-IR, AAS, FESEM, XRD, DLS, and VSM equipment. Silica was amended on the surface of iron oxide nanoparticles (IONPs, γ-Fe2O3) to modify its biocompatibility and stability. The solvent evaporation method was used to activate PPN vectorization. The following tests were performed to highlight the compatibility of our proposed delivery vehicle: in vitro toxicity assay, in vivo acute systemic toxicity test, and the histology examination. The results demonstrated that IONPs@SiO2-PPN successfully reduced the IC50 values compared with the native PPN. Also, the structural alternations of HeLa cells exposed to IONPs@SiO2-PPN exhibited higher typical hallmarks of apoptosis compared to the cells treated with the native PPN. The in vivo acute toxicity test indicated no clinical signs of distress/discomfort or weight loss in Balb/C mice a week after the intravenous injection of IONPs@SiO2 (10 mg kg-1). Besides, the tissues architectures were not affected and the pathological inflammatory alternations detection failed. In conclusion, IONPs@SiO2-PPN can be chosen as a potent candidate for further medical applications in the future, for instance as a drug delivery vehicle or hyperthermia agent.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  14. Fulltext Kingianic acids A-G, Endiandric acid analogues from Endiandra kingiana
    Azmi MN, Gény C, Leverrier A, Litaudon M, Dumontet V, Birlirakis N, et al.
    Molecules, 2014;19(2):1732-47.
    PMID: 24492595 DOI: 10.3390/molecules19021732
    A phytochemical investigation of the methanolic extract of the bark of Endiandra kingiana led to the isolation of seven new tetracyclic endiandric acid analogues, kingianic acids A-G (1-7), together with endiandric acid M (8), tsangibeilin B (9) and endiandric acid (10). Their structures were determined by 1D- and 2D-NMR analysis in combination with HRMS experiments. The structure of compounds 9 and 10 were confirmed by single-crystal X-ray diffraction analysis. These compounds were screened for Bcl-xL and Mcl-1 binding affinities and cytotoxic activity on various cancer cell lines. Compound 5 showed moderate cytotoxic activity against human colorectal adeno-carcinoma (HT-29) and lung adenocarcinoma epithelial (A549) cell lines, with IC50 values in the range 15-17 µM, and compounds 3, 6 and 9 exhibited weak binding affinity for the anti-apoptotic protein Mcl-1.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  15. Fulltext Phytochemical and cytotoxic investigations of Curcuma mangga rhizomes
    Malek SN, Lee GS, Hong SL, Yaacob H, Wahab NA, Faizal Weber JF, et al.
    Molecules, 2011 May 31;16(6):4539-48.
    PMID: 21629182 DOI: 10.3390/molecules16064539
    Investigations on the cytotoxic effects of the crude methanol and fractionated extracts (hexane, ethyl acetate) C. mangga against six human cancer cell lines, namely the hormone-dependent breast cell line (MCF-7), nasopharyngeal epidermoid cell line (KB), lung cell line (A549), cervical cell line (Ca Ski), colon cell lines (HCT 116 and HT-29), and one non-cancer human fibroblast cell line (MRC-5) were conducted using an in-vitro neutral red cytotoxicity assay. The crude methanol and fractionated extracts (hexane and ethyl acetate) displayed good cytotoxic effects against MCF-7, KB, A549, Ca Ski and HT-29 cell lines, but exerted no damage on the MRC-5 line. Chemical investigation from the hexane and ethyl acetate fractions resulted in the isolation of seven pure compounds, namely (E)-labda-8(17),12-dien-15,16-dial (1), (E)-15,16-bisnor-labda-8(17),11-dien-13-on (2), zerumin A (3), β-sitosterol, curcumin, demethoxycurcumin and bis-demethoxycurcumin. Compounds 1 and 3 exhibited high cytotoxic effects against all six selected cancer cell lines, while compounds 2 showed no anti-proliferative activity on the tested cell lines. Compound 1 also demonstrated strong cytotoxicity against the normal cell line MRC-5. This paper reports for the first time the cytotoxic activities of C. mangga extracts on KB, A549, Ca Ski, HT-29 and MRC-5, and the occurrence of compound 2 and 3 in C. mangga.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry*
  16. Fulltext Assessment of antioxidant capacity and cytotoxicity of selected Malaysian plants
    Ling LT, Radhakrishnan AK, Subramaniam T, Cheng HM, Palanisamy UD
    Molecules, 2010 Apr;15(4):2139-51.
    PMID: 20428033 DOI: 10.3390/molecules15042139
    Thirteen Malaysian plants; Artocarpus champeden, Azadirachta indica, Fragaria x ananassa, Garcinia mangostana, Lawsonia inermis, Mangifera indica, Nephelium lappaceum, Nephelium mutobile, Peltophorum pterocarpum, Psidium guajava and Syzygium aqueum, selected for their use in traditional medicine, were subjected to a variety of assays. Antioxidant capability, total phenolic content, elemental composition, as well as it cytotoxity to several cell lines of the aqueous and ethanolic extracts from different parts of these selected Malaysian plants were determined. In general, the ethanolic extracts were better free radical scavengers than the aqueous extracts and some of the tested extracts were even more potent than a commercial grape seed preparation. Similar results were seen in the lipid peroxidation inhibition studies. Our findings also showed a strong correlation of antioxidant activity with the total phenolic content. These extracts when tested for its heavy metals content, were found to be below permissible value for nutraceutical application. In addition, most of the extracts were found not cytotoxic to 3T3 and 4T1 cells at concentrations as high as 100 microg/mL. We conclude that although traditionally these plants are used in the aqueous form, its commercial preparation could be achieved using ethanol since a high total phenolic content and antioxidant activity is associated with this method of preparation.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  17. Fulltext Deoxyelephantopin from Elephantopus scaber Inhibits HCT116 Human Colorectal Carcinoma Cell Growth through Apoptosis and Cell Cycle Arrest
    Chan CK, Chan G, Awang K, Abdul Kadir H
    Molecules, 2016 Mar 21;21(3):385.
    PMID: 27007366 DOI: 10.3390/molecules21030385
    Deoxyelephantopin (DET), one of the major sesquiterpene lactones derived from Elephantopus scaber was reported to possess numerous pharmacological functions. This study aimed to assess the apoptosis inducing effects and cell cycle arrest by DET followed by elucidation of the mechanisms underlying cell death in HCT116 cells. The anticancer activity of DET was evaluated by a MTT assay. Morphological and biochemical changes were detected by Hoescht 33342/PI and Annexin V/PI staining. The results revealed that DET and isodeoxyelephantopin (isoDET) could be isolated from the ethyl acetate fraction of E. scaber leaves via a bioassay-guided approach. DET induced significant dose- and time-dependent growth inhibition of HCT116 cells. Characteristics of apoptosis including nuclear morphological changes and externalization of phosphatidylserine were observed. DET also significantly resulted in the activation of caspase-3 and PARP cleavage. Additionally, DET induced cell cycle arrest at the S phase along with dose-dependent upregulation of p21 and phosphorylated p53 protein expression. DET dose-dependently downregulated cyclin D1, A2, B1, E2, CDK4 and CDK2 protein expression. In conclusion, our data showed that DET induced apoptosis and cell cycle arrest in HCT116 colorectal carcinoma, suggesting that DET has potential as an anticancer agent for colorectal carcinoma.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  18. Fulltext Alpinia zerumbet (Pers.): Food and Medicinal Plant with Potential In Vitro and In Vivo Anti-Cancer Activities
    Zahra MH, Salem TAR, El-Aarag B, Yosri N, El-Ghlban S, Zaki K, et al.
    Molecules, 2019 Jul 08;24(13).
    PMID: 31288458 DOI: 10.3390/molecules24132495
    BACKGROUND/AIM: Plants play an important role in anti-cancer drug discovery, therefore, the current study aimed to evaluate the biological activity of Alpinia zerumbet (A. zerumbet) flowers.

    METHODS: The phytochemical and biological criteria of A. zerumbet were in vitro investigated as well as in mouse xenograft model.

    RESULTS: A. zerumbet extracts, specially CH2Cl2 and MeOH extracts, exhibited the highest potent anti-tumor activity against Ehrlich ascites carcinoma (EAC) cells. The most active CH2Cl2 extract was subjected to bioassay-guided fractionation leading to isolatation of the naturally occurring 5,6-dehydrokawain (DK) which was characterized by IR, MS, 1H-NMR and 13C-NMR. A. zerumbet extracts, specially MeOH and CH2Cl2 extracts, exhibited significant inhibitory activity towards tumor volume (TV). Furthermore, A. zerumbet extracts declined the high level of malonaldehyde (MDA) as well as elevated the levels of superoxide dismutase (SOD) and catalase (CAT) in liver tissue homogenate. Moreover, DK showed anti-proliferative action on different human cancer cell lines. The recorded IC50 values against breast carcinoma (MCF-7), liver carcinoma (Hep-G2) and larynx carcinoma cells (HEP-2) were 3.08, 6.8, and 8.7 µg/mL, respectively.

    CONCLUSION: Taken together, these findings open the door for further investigations in order to explore the potential medicinal properties of A. zerumbet.

    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry*
  19. Fulltext Ampelopsin E Reduces the Invasiveness of the Triple Negative Breast Cancer Cell Line, MDA-MB-231
    Tieng FYF, Latifah SY, Md Hashim NF, Khaza'ai H, Ahmat N, Gopalsamy B, et al.
    Molecules, 2019 Jul 18;24(14).
    PMID: 31323836 DOI: 10.3390/molecules24142619
    Breast cancer is the most common and the second leading cause of cancer-related deaths in women. It has two distinctive hallmarks: rapid abnormal growth and the ability to invade and metastasize. During metastasis, cancer cells are thought to form actin-rich protrusions, called invadopodia, which degrade the extracellular matrix. Current breast cancer treatments, particularly chemotherapy, comes with adverse effects like immunosuppression, resistance development and secondary tumour formation. Hence, naturally-occurring molecules claimed to be less toxic are being studied as new drug candidates. Ampelopsin E, a natural oligostilbene extracted from Dryobalanops species, has exhibited various pharmacological properties, including anticancer and anti-inflammatory activities. However, there is yet no scientific evidence of the effects of ampelopsin E towards metastasis. Scratch assay, transwell migration and invasion assays, invadopodia and gelatin degradation assays, and ELISA were used to determine the effects of ampelopsin E towards the invasiveness of MDA-MB-231 cells. Strikingly in this study, ampelopsin E was able to halt migration, transmigration and invasion in MDA-MB-231 cells by reducing formation of invadopodia and its degradation capability through significant reduction (p < 0.05) in expression levels of PDGF, MMP2, MMP9 and MMP14. In conclusion, ampelopsin E reduced the invasiveness of MDA-MB-231 cells and was proven to be a potential alternative in treating TNBC.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry
  20. Fulltext Bioguided Fractionation of Local Plants against Matrix Metalloproteinase9 and Its Cytotoxicity against Breast Cancer Cell Models: In Silico and In Vitro Study
    Hariono M, Rollando R, Karamoy J, Hariyono P, Atmono M, Djohan M, et al.
    Molecules, 2020 Oct 14;25(20).
    PMID: 33066411 DOI: 10.3390/molecules25204691
    Matrix metalloproteinase9 (MMP9) is known to be highly expressed during metastatic cancer where most known potential inhibitors failed in the clinical trials. This study aims to select local plants in our state, as anti-breast cancer agent with hemopexin-like domain of MMP9 (PEX9) as the selective protein target. In silico screening for PEX9 inhibitors was performed from our in house-natural compound database to identify the plants. The selected plants were extracted using methanol and then a step-by-step in vitro screening against MMP9 was performed from its crude extract, partitions until fractions using FRET-based assay. The partitions were obtained by performing liquid-liquid extraction on the methanol extract using n-hexane, ethylacetate, n-butanol, and water representing nonpolar to polar solvents. The fractions were made from the selected partition, which demonstrated the best inhibition percentage toward MMP9, using column chromatography. Of the 200 compounds screened, 20 compounds that scored the binding affinity -11.2 to -8.1 kcal/mol toward PEX9 were selected as top hits. The binding of these hits were thoroughly investigated and linked to the plants which they were reported to be isolated from. Six of the eight crude extracts demonstrated inhibition toward MMP9 with the IC50 24 to 823 µg/mL. The partitions (1 mg/mL) of Ageratum conyzoides aerial parts and Ixora coccinea leaves showed inhibition 94% and 96%, whereas their fractions showed IC50 43 and 116 µg/mL, respectively toward MMP9. Using MTT assay, the crude extract of Ageratum exhibited IC50 22 and 229 µg/mL against 4T1 and T47D cell proliferations, respectively with a high safety index concluding its potential anti-breast cancer from herbal.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/chemistry*
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