Displaying publications 1 - 20 of 306 in total

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  1. Fulltext Typhonium divaricatum (rodent tuber): a promising local plant in the fight against cancer
    Neoh CK
    Med J Malaysia, 1992 Mar;47(1):86-8.
    PMID: 1387458
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology*
  2. An effective protein extraction method for two-dimensional electrophoresis in the anticancer herb Andrographis paniculata Nees
    Talei D, Valdiani A, Puad MA
    Biotechnol Appl Biochem, 2013 Sep-Oct;60(5):521-6.
    PMID: 23725097 DOI: 10.1002/bab.1126
    Proteomic analysis of plants relies on high yields of pure protein. In plants, protein extraction and purification present a great challenge due to accumulation of a large amount of interfering substances, including polysaccharides, polyphenols, and secondary metabolites. Therefore, it is necessary to modify the extraction protocols. A study was conducted to compare four protein extraction and precipitation methods for proteomic analysis. The results showed significant differences in protein content among the four methods. The chloroform-trichloroacetic acid-acetone method using 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES) buffer provided the best results in terms of protein content, pellets, spot resolution, and intensity of unique spots detected. An overall of 83 qualitative or quantitative significant differential spots were found among the four methods. Based on the 2-DE gel map, the method is expected to benefit the development of high-level proteomic and biochemical studies of Andrographis paniculata, which may also be applied to other recalcitrant medicinal plant tissues.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/isolation & purification*; Antineoplastic Agents, Phytogenic/chemistry
  3. 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/pharmacology*; Antineoplastic Agents, Phytogenic/chemistry*
  4. New phenantrene alkaloids from Cryptocarya crassinervia
    Awang K, Hadi AH, Saidi N, Mukhtar MR, Morita H, Litaudon M
    Fitoterapia, 2008 Jun;79(4):308-10.
    PMID: 18313862 DOI: 10.1016/j.fitote.2007.11.025
    The bark of Cryptocarya crassinervia provided two new phenantrene alkaloids, 2-hydroxyatherosperminine (1) and N-demethyl-2-methoxyatherosperminine (2).
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology; Antineoplastic Agents, Phytogenic/chemistry
  5. 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/isolation & purification; Antineoplastic Agents, Phytogenic/pharmacology; Antineoplastic Agents, Phytogenic/chemistry
  6. A Comprehensive Review on the Chemotherapeutic Potential of Piceatannol for Cancer Treatment, with Mechanistic Insights
    Seyed MA, Jantan I, Bukhari SN, Vijayaraghavan K
    J Agric Food Chem, 2016 Feb 3;64(4):725-37.
    PMID: 26758628 DOI: 10.1021/acs.jafc.5b05993
    Cancer is a diverse class of diseases characterized by uncontrolled cell growth that constitutes the greatest cause of mortality and morbidity worldwide. Despite steady progress, the treatment modalities of cancer are still insufficient. Several new concepts have emerged for therapeutic intervention in malignant diseases with the goal of identifying specific targets and overcoming resistance against current cytotoxic therapies. Many studies have reported the remarkable and significant properties of dietary plant polyphenols such as curcumin, resveratrol, flavopiridol, indirubin, magnolol, piceatannol, parthenolide, epigallocatechin gallate, and cucurbitacin as anticancer agents known for their pleiotropic effects on cancer, immune cells, and inflammation. Piceatannol, an analogue and metabolite of resveratrol, is a natural stilbene commonly found in grape skins and wine. Compared to resveratrol, this molecule exhibits superior bioactivities as an inhibitor of COX-1/2 and the CSN-associated kinase. Piceatannol is thought to be a potent natural compound with many therapeutic effects, such as the prevention of hypercholesterolemia, arrhythmia, atherosclerosis, angiogenesis, and cardiovascular diseases. It also demonstrates vasorelaxation, antioxidant, and anticancer activities. This comprehensive review summarizes the current data regarding the mechanisms of action of piceatannol, its chemopreventive properties, and its possible therapeutic potential against various types of human cancer.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/metabolism; Antineoplastic Agents, Phytogenic/pharmacology*; Antineoplastic Agents, Phytogenic/chemistry
  7. Cytotoxic prenylated depsidones from Garcinia parvifolia
    Xu YJ, Chiang PY, Lai YH, Vittal JJ, Wu XH, Tan BK, et al.
    J Nat Prod, 2000 Oct;63(10):1361-3.
    PMID: 11076552
    Leaf extracts of Garcinia parvifolia provided relatively high yields of four novel, cytotoxic prenylated depsidones. The structures were determined mainly by detailed NMR spectral analysis and X-ray crystallography.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/isolation & purification; Antineoplastic Agents, Phytogenic/pharmacology*; Antineoplastic Agents, Phytogenic/chemistry
  8. Goniolanceolatins A-H, Cytotoxic Bis-styryllactones from Goniothalamus lanceolatus
    Bihud NV, Rasol NE, Imran S, Awang K, Ahmad FB, Mai CW, et al.
    J Nat Prod, 2019 09 27;82(9):2430-2442.
    PMID: 31433181 DOI: 10.1021/acs.jnatprod.8b01067
    Eight new bis-styryllactones, goniolanceolatins A-H (1-8), possessing a rare α,β-unsaturated δ-lactone moiety with a (6S)-configuration, were isolated from the CH2Cl2 extract of the stembark and roots of Goniothalamus lanceolatus Miq., a plant endemic to Malaysia. Absolute structures were established through extensive 1D- and 2D-NMR data analysis, in combination with electronic dichroism (ECD) data. All of the isolates were evaluated for their cytotoxicity against human lung and colorectal cancer cell lines. Compounds 2 and 4 showed cytotoxicity, with IC50 values ranging from 2.3 to 4.2 μM, and were inactive toward human noncancerous lung and colorectal cells. Compounds 1, 3, 6, 7, and 8 showed moderate to weak cytotoxicity. Docking studies of compounds 2 and 4 showed that they bind with EGFR tyrosine kinase and cyclin-dependent kinase 2 through hydrogen bonding interactions with the important amino acids, including Lys721, Met769, Asn818, Arg157, Ile10, and Glu12.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/isolation & purification; Antineoplastic Agents, Phytogenic/pharmacology*; Antineoplastic Agents, Phytogenic/chemistry
  9. Schwarzinicines A-G, 1,4-Diarylbutanoid-Phenethylamine Conjugates from the Leaves of Ficus schwarzii
    Krishnan P, Lee FK, Yap VA, Low YY, Kam TS, Yong KT, et al.
    J Nat Prod, 2020 01 24;83(1):152-158.
    PMID: 31935094 DOI: 10.1021/acs.jnatprod.9b01160
    Schwarzinicines A-G (1-7), representing the first examples of 1,4-diarylbutanoid-phenethylamine conjugates, were isolated from the leaves of Ficus schwarzii. The structures of these compounds were determined by detailed analysis of their MS, 1D and 2D NMR data. Compounds 1-4 exhibited pronounced vasorelaxant effects in the rat isolated aorta (Emax 106-120%; EC50 0.96-2.10 μM). However, compounds 1 and 2 showed no cytotoxic effects against A549, MCF-7, and HCT 116 human cancer cells (IC50 > 10 μM).
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/isolation & purification; Antineoplastic Agents, Phytogenic/pharmacology; Antineoplastic Agents, Phytogenic/chemistry*
  10. Fulltext Medicinal Plants with Anti-Leukemic Effects: A Review
    Maher T, Ahmad Raus R, Daddiouaissa D, Ahmad F, Adzhar NS, Latif ES, et al.
    Molecules, 2021 May 07;26(9).
    PMID: 34066963 DOI: 10.3390/molecules26092741
    Leukemia is a leukocyte cancer that is characterized by anarchic growth of immature immune cells in the bone marrow, blood and spleen. There are many forms of leukemia, and the best course of therapy and the chance of a patient's survival depend on the type of leukemic disease. Different forms of drugs have been used to treat leukemia. Due to the adverse effects associated with such therapies and drug resistance, the search for safer and more effective drugs remains one of the most challenging areas of research. Thus, new therapeutic approaches are important to improving outcomes. Almost half of the drugs utilized nowadays in treating cancer are from natural products and their derivatives. Medicinal plants have proven to be an effective natural source of anti-leukemic drugs. The cytotoxicity and the mechanisms underlying the toxicity of these plants to leukemic cells and their isolated compounds were investigated. Effort has been made throughout this comprehensive review to highlight the recent developments and milestones achieved in leukemia therapies using plant-derived compounds and the crude extracts from various medicinal plants. Furthermore, the mechanisms of action of these plants are discussed.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology; Antineoplastic Agents, Phytogenic/therapeutic use*; Antineoplastic Agents, Phytogenic/chemistry
  11. 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/isolation & purification; Antineoplastic Agents, Phytogenic/pharmacology*; Antineoplastic Agents, Phytogenic/chemistry
  12. Fulltext Chemistry, Biosynthesis, Physicochemical and Biological Properties of Rubiadin: A Promising Natural Anthraquinone for New Drug Discovery and Development
    Watroly MN, Sekar M, Fuloria S, Gan SH, Jeyabalan S, Wu YS, et al.
    Drug Des Devel Ther, 2021;15:4527-4549.
    PMID: 34764636 DOI: 10.2147/DDDT.S338548
    Anthraquinones (AQs) are found in a variety of consumer products, including foods, nutritional supplements, drugs, and traditional medicines, and have a wide range of pharmacological actions. Rubiadin, a 1,3-dihydroxy-2-methyl anthraquinone, primarily originates from Rubia cordifolia Linn (Rubiaceae). It was first discovered in 1981 and has been reported for many biological activities. However, no review has been reported so far to create awareness about this molecule and its role in future drug discovery. Therefore, the present review aimed to provide comprehensive evidence of Rubiadin's phytochemistry, biosynthesis, physicochemical properties, biological properties and therapeutic potential. Relevant literature was gathered from numerous scientific databases including PubMed, ScienceDirect, Scopus and Google Scholar between 1981 and up-to-date. The distribution of Rubiadin in numerous medicinal plants, as well as its method of isolation, synthesis, characterisation, physiochemical properties and possible biosynthesis pathways, was extensively covered in this review. Following a rigorous screening and tabulating, a thorough description of Rubiadin's biological properties was gathered, which were based on scientific evidences. Rubiadin fits all five of Lipinski's rule for drug-likeness properties. Then, the in depth physiochemical characteristics of Rubiadin were investigated. The simple technique for Rubiadin's isolation from R. cordifolia and the procedure of synthesis was described. Rubiadin is also biosynthesized via the polyketide and chorismate/o-succinylbenzoic acid pathways. Rubiadin is a powerful molecule with anticancer, antiosteoporotic, hepatoprotective, neuroprotective, anti-inflammatory, antidiabetic, antioxidant, antibacterial, antimalarial, antifungal, and antiviral properties. The mechanism of action for the majority of the pharmacological actions reported, however, is unknown. In addition to this review, an in silico molecular docking study was performed against proteins with PDB IDs: 3AOX, 6OLX, 6OSP, and 6SDC to support the anticancer properties of Rubiadin. The toxicity profile, pharmacokinetics and possible structural modifications were also described. Rubiadin was also proven to have the highest binding affinity to the targeted proteins in an in silico study; thus, we believe it may be a potential anticancer molecule. In order to present Rubiadin as a novel candidate for future therapeutic development, advanced studies on preclinical, clinical trials, bioavailability, permeability and administration of safe doses are necessary.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/isolation & purification; Antineoplastic Agents, Phytogenic/pharmacology*; Antineoplastic Agents, Phytogenic/chemistry
  13. Fulltext Phytochemical and cytotoxic investigations of Alpinia mutica rhizomes
    Malek SN, Phang CW, Ibrahim H, Norhanom AW, Sim KS
    Molecules, 2011 Jan 14;16(1):583-9.
    PMID: 21240148 DOI: 10.3390/molecules16010583
    The methanol and fractionated extracts (hexane, ethyl acetate and water) of Alpinia mutica (Zingiberaceae) rhizomes were investigated for their cytotoxic effect against six human carcinoma cell lines, namely KB, MCF7, A549, Caski, HCT116, HT29 and non-human fibroblast cell line (MRC 5) using an in vitro cytotoxicity assay. The ethyl acetate extract possessed high inhibitory effect against KB, MCF7 and Caski cells (IC₅₀ values of 9.4, 19.7 and 19.8 µg/mL, respectively). Flavokawin B (1), 5,6-dehydrokawain (2), pinostrobin chalcone (3) and alpinetin (4), isolated from the active ethyl acetate extract were also evaluated for their cytotoxic activity. Of these, pinostrobin chalcone (3) and alpinetin (4) were isolated from this plant for the first time. Pinostrobin chalcone (3) displayed very remarkable cytotoxic activity against the tested human cancer cells, such as KB, MCF7 and Caski cells (IC₅₀ values of 6.2, 7.3 and 7.7 µg/mL, respectively). This is the first report of the cytotoxic activity of Alpinia mutica.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology*
  14. Phenolic constituents and anticancer properties of Morus alba (white mulberry) leaves
    Chan EWC, Wong SK, Tangah J, Inoue T, Chan HT
    J Integr Med, 2020 May;18(3):189-195.
    PMID: 32115383 DOI: 10.1016/j.joim.2020.02.006
    Flavonoids are by far the most dominant class of phenolic compounds isolated from Morus alba leaves (MAL). Other classes of compounds are benzofurans, phenolic acids, alkaloids, coumarins, chalcones and stilbenes. Major flavonoids are kuwanons, moracinflavans, moragrols and morkotins. Other major compounds include moracins (benzofurans), caffeoylquinic acids (phenolic acids) and morachalcones (chalcones). Research on the anticancer properties of MAL entailed in vitro and in vivo cytotoxicity of extracts or isolated compounds. Flavonoids, benzofurans, chalcones and alkaloids are classes of compounds from MAL that have been found to be cytotoxic towards human cancer cell lines. Further studies on the phytochemistry and anticancer of MAL are suggested. Sources of information were PubMed, PubMed Central, ScienceDirect, Google, Google Scholar, J-Stage, PubChem and China National Knowledge Infrastructure.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology*
  15. Apocynaceae species with antiproliferative and/or antiplasmodial properties: a review of ten genera
    Chan EW, Wong SK, Chan HT
    J Integr Med, 2016 Jul;14(4):269-84.
    PMID: 27417173 DOI: 10.1016/S2095-4964(16)60261-3
    Apocynaceae is a large family of tropical trees, shrubs and vines with most species producing white latex. Major metabolites of species are triterpenoids, iridoids, alkaloids and cardenolides, which are known for a wide range of biological and pharmacological activities such as cardioprotective, hepatoprotective, neuroprotective, anti-inflammatory, anticancer and antimalarial properties. Prompted by their anticancer and antimalarial properties, the current knowledge on ten genera (Allamanda, Alstonia, Calotropis, Catharanthus, Cerbera, Dyera, Kopsia, Nerium, Plumeria and Vallaris) is updated. Major classes of metabolites are described using some species as examples. Species with antiproliferative (APF) and/or antiplasmodial (APM) properties have been identified. With the exception of the genus Dyera, nine genera of 22 species possess APF activity. Seven genera (Alstonia, Calotropis, Catharanthus, Dyera, Kopsia, Plumeria and Vallaris) of 13 species have APM properties. Among these species, Alstonia angustiloba, Alstonia macrophylla, Calotropis gigantea, Calotropis procera, Catharanthus roseus, Plumeria alba and Vallaris glabra displayed both APF and APM properties. The chemical constituents of these seven species are compiled for assessment and further research.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology*
  16. Fulltext Anticancer activity of Cyathula prostrata (Linn) Blume against Dalton's lymphomae in mice model
    Mayakrishnan V, Kannappan P, Shanmugasundaram K, Abdullah N
    Pak J Pharm Sci, 2014 Nov;27(6):1911-7.
    PMID: 25362615
    Cyathula prostrata (Linn) Blume herbs are commonly used for the treatment of inflammatory and pain in Nigeria. The objective of the present study was to assess the antitumor and antioxidant activity of Cyathula prostrata (Linn) Blume in mice model. The treatment of Dalton's lymphoma ascites cells induced tumor by the methanolic extract of Cyathula prostrata was determined at concentration of 100 mg/ kg body weight given orally for 11 days, antitumor activity was assessed by monitoring the mean survival time, body weight, effect on hematological parameters, antioxidant enzyme levels and histopathological evidence. The results showed that the methanolic extract of Cyathula prostrata increased the survival period of animals, decreased the body weight and also altered many hematological markers and also restored the antioxidant enzymes when compared to the mice of the DLA control group. These findings indicate that the methanolic extract of C. prostrata has anti-tumor activity by preventing the lipid peroxidation and thereby promoting the antioxidant systems in Dalton's lymphoma ascites induced mice. So, these extract could be a natural anticancer agent for human health.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/therapeutic use*
  17. Fulltext Antiproliferative xanthone derivatives from Calophyllum inophyllum and Calophyllum soulattri
    Mah SH, Lian Ee GC, Teh SS, Sukari MA
    Pak J Pharm Sci, 2015 Mar;28(2):425-9.
    PMID: 25730799
    Structure-activity relationships of eleven xanthones were comparatively predicted for four cancer cell lines after the compounds were subjected to antiproliferative assay against B-lymphocyte cells (Raji), colon carcinoma cells (LS174T), human neuroblastoma cells (IMR-32) and skin carcinoma cells (SK-MEL-28). The eleven chemical constituents were obtained naturally from the stem bark of Calophyllum inophyllum and Calophyllum soulattri. Inophinnin (1) and inophinone (2) were isolated from Calophyllum inophyllum while soulattrin (3) and phylattrin (4) were found from Calophyllum soulattri. The other xanthones were from both Calophyllum sp. and they are pyranojacareubin (5), rheediaxanthone A (6), macluraxanthone (7), 4-hydroxyxanthone (8), caloxanthone C (9), brasixanthone B (10) and trapezifolixanthone (11). Compound 3 was found to be the most cytotoxic towards all the cancer cell lines with an IC50 value of 1.25μg/mL while the simplest xanthone, compound 8 was inactive.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology*
  18. Fulltext The cytotoxic effect of Baeckea frustescens extracts in eliminating hypoxic breast cancer cells
    Shahruzaman SH, Yusof FZ, Maniam S, Fakurazi S, Maniam S
    BMC Complement Med Ther, 2021 Oct 01;21(1):245.
    PMID: 34598696 DOI: 10.1186/s12906-021-03417-9
    BACKGROUND: Adaptive metabolic response towards a low oxygen environment is essential to maintain rapid tumour proliferation and progression. The vascular network that surrounds the tumour develops an intermittent hypoxic condition and stimulates hypoxia-inducing factors. Baeckea frutescens is used in traditional medicine and known to possess antibacterial and cytoprotective properties. In this study, the cytotoxic effect of B. frutescens leaves and branches extracts against hypoxic human breast cancer (MCF-7) was investigated.

    METHOD: The extracts were prepared using Soxhlet apparatus for ethanol and hexane extracts while the water extracts were freeze-dried. In vitro cytotoxic activities of B. frutescens extracts of various concentrations (20 to 160 μg/mL) at 24, 48, and 72 hours time points were studied using MTT in chemically induced hypoxic condition and in 3-dimensional in vitro cell culture system. An initial characterisation of B. frutescens extracts was carried out using Fourier-transform Infrared- Attenuated Total Reflection (FTIR-ATR) to determine the presence of functional groups.

    RESULTS: All leaf extracts except for water showed IC50 values ranging from 23 -158 μg/mL. Hexane extract showed the lowest IC50 value (23 μg/mL), indicating its potent cytotoxic activity. Among the branch extracts, only the 70% ethanolic extract (B70) showed an IC50 value. The hexane leaf extract tested on 3- dimensional cultured cells showed an IC50 value of 17.2 μg/mL. The FTIR-ATR spectroscopy analysis identified various characteristic peak values with different functional groups such as alcohol, alkenes, alkynes, carbonyl, aromatic rings, ethers, ester, and carboxylic acids. Interestingly, the FTIR-ATR spectra report a complex and unique profile of the hexane extract, which warrants further investigation.

    CONCLUSION: Adaptation of tumour cells to hypoxia significantly contributes to the aggressiveness and chemoresistance of different tumours. The identification of B. frutescens and its possible role in eliminating breast cancer cells in hypoxic conditions defines a new role of natural product that can be utilised as an effective agent that regulates metabolic reprogramming in breast cancer.

    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology*
  19. Cytotoxicity and electron microscopy of cell death induced by goniothalamin
    Ali AM, Mackeen MM, Hamid M, Aun QB, Zauyah Y, Azimahtol HL, et al.
    Planta Med, 1997 Feb;63(1):81-3.
    PMID: 9063100
    The cytotoxicity of goniothalamin was found to be strong towards both cancerous (HGC-27, MCF-7, PANC-1, HeLa), and non-cancerous (3T3) cell lines, especially in cases of dividing cells. Drug exposure studies indicated that the cytotoxic action of goniothalamin was time- and dose-dependent. At the ultrastructural level, goniothalamin-induced cytotoxicity revealed a necrotic mode of cell death towards MCF-7 cells.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology*
  20. Formulating 10-hydroxycamptothecin into nanoemulsion with functional excipient tributyrin: An innovative strategy for targeted hepatic cancer chemotherapy
    Yang S, Lin HS, Zhang L, Chi-Lui Ho P
    Int J Pharm, 2024 Apr 10;654:123945.
    PMID: 38403088 DOI: 10.1016/j.ijpharm.2024.123945
    This study aimed to develop an innovative dosage form for 10-hydroxycamptothecin (HCPT), a chemotherapeutic agent with limited aqueous solubility and stability, to enhance its parenteral delivery and targeting to hepatic cancer. We formulated HCPT into a nanoemulsion using tributyrin, a dietary component with histone deacetylase inhibitor activity. The resulting HCPT-loaded tributyrin nanoemulsion (Tri-HCPT-E) underwent extensive evaluations. Tri-HCPT-E significantly improved the aqueous solubility, stability, and anti-cancer activities in HepG2 cells. Pharmacokinetic studies confirmed the increased stability and hepatic targeting, with Tri-HCPT-E leading to a 120-fold increase in plasma exposure of intact HCPT and a 10-fold increase in hepatic exposure compared to the commercial free solution. Co-administration of 17α-ethynylestradiol, an up-regulator of low-density lipoprotein (LDL) receptor, further enhanced the distribution and metabolism of HCPT, demonstrating an association between the LDL receptor pathway and hepatic targeting. Most importantly, Tri-HCPT-E exhibited superior in vivo anti-cancer efficacy in a mouse xenograft model compared to the commercial formulation, without causing escalated hepatic or renal toxicity. In conclusion, formulating HCPT into a nanoemulsion with tributyrin has proven to be an innovative and effective strategy for targeted hepatic cancer chemotherapy while tributyrin, a pharmacologically active dietary component, has emerged as a promising functional excipient for drug delivery.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic*
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