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1.
Plants (Basel) ; 12(21)2023 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-37960098

RESUMO

The effectiveness of lemon myrtle (LM) (Backhousia citriodora) essential oil (EO) was investigated to combat Penicillium digitatum by in vitro agar diffusion and vapour assay and in artificially infected oranges. The main constituent of LM EO was revealed as citral when analysed in gas chromatography-mass spectrometry. Pure citral was also included in the experiment for comparison. The in vitro fungal growth was significantly inhibited by LM EO at 1, 2, 3, 4 and 5 µL per disc while complete growth inhibition by both the pure citral and LM EO occurred at 4 and 5 µL per disc. Inoculated fruits treated by dipping in 1000 µL L-1 LM EO solutions for 5, 10, 15, 30 and 120 s showed significantly lower fungal wounds compared to control. While longer dipping times led to some rind injuries, fruits with a 5 and 10 s dip were found free from any injury. The evaluation after dipping and storage confirmed that the fruits maintained the sensory attributes and were not compromised by the incorporation of the essential oil. The results of this study indicate that LM EO can be a promising alternative to synthetic fungicides for preserving the quality of citrus fruits during storage.

2.
Int J Mol Sci ; 24(6)2023 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-36982195

RESUMO

Molecularly imprinted polymers (MIPs) for benzylpiperazine (BZP, 1), an illicit designer drug, were developed by using both self-assembly and semi-covalent approaches. From an array of potential functional monomers (FMs) and using a combination of pre-synthetic interaction studies (by molecular modelling and NMR analysis) and binding assays, the highest performing self-assembly 1-MIPs were confirmed to result from methacrylic acid (7) as FM, ethylene glycol dimethacrylate (EGDMA) or trimethylolpropane trimethacrylate (TRIM) as crosslinkers and chloroform as the porogen and rebinding solvent at template (T): FM ratios of 1:1 and 1:2, giving imprinting factors (IF) 3 to 7. The semi-covalent 1-MIPs were designed using benzylpiperazine (4-vinylphenyl) carbamate (16) as the template-monomer adduct in combination with either EDGMA or TRIM. Our comparative analysis showed the semi-covalent polymers to have a stronger affinity for 1 (significantly lower Kd values and higher IFs) and faster uptake than the self-assembly systems. Both approaches have comparable cross-reactivity: marginal to low against cocaine (17) and morphine (18) and high against ephedrine (19) and phenylpiperazine (20). They also have comparable selectivity: highly selective towards 1 against 17, moderate against 18 and non-selective against 19. EGDMA-based self-assembly MIPs displayed a greater imprinting effect (higher IFs and NIP-to-MIP Kd ratios) than TRIM-based MIPs, while the TRIM-based semi-covalent MIP outperformed its EGDMA-based equivalent. By virtue of its modest selectivity against the test illicit drugs, 1-MIPs could potentially be used as a dummy MIP for the broad-based capture and enrichment of illicit drug blends for subsequent laboratory analysis.


Assuntos
Impressão Molecular , Polímeros/química , Polímeros Molecularmente Impressos , Solventes
3.
3 Biotech ; 12(10): 257, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36068843

RESUMO

This study aimed to determine the phytochemical, antioxidant, and anticancer activities of the crude extract and its fractions of Cupaniopsis anacardioides. The results showed that total phenolic content (TPC), their secondary metabolites (flavonoids-TFC; proanthocyanidins-TPro), and antioxidant activity were significantly different between the crude extract and its fractions. The butanol fraction (F3) had the highest levels of TPC, TFC, and TPro, followed by the crude extract, aqueous fraction (F4), dichloromethyl fraction (F2), and hexane fraction (F1). High-Pressure Liquid Chromatography (HPLC) analysis revealed 14 major bioactive compounds were identified in the C. anacardioides extract. Further analysis showed F3 fraction contained the highest levels of the major bioactive compounds, while F1 fraction had the lowest. A similar pattern was observed for antioxidant activities. The crude extract, F3 and F4 fractions were further tested for cytotoxicity against 10 cancer cell lines, including HT29 (colon); U87, SJG2 (glioblastoma); MCF-7 (Breast); A2780 (ovarian); H460 (lung); A431 (skin); Du145 (prostate); BE2-C (neuroblastoma); MIA PaCa-2 (pancreas); and one non-tumour-derived normal breast cell line (MCF10A). Except for Du145 (prostate), the crude extract, F3 and F4 fractions inhibited the cancer cell lines at 100 µg/mL, with F3 possessing greater activity against these cancer cell lines. Future studies are recommended to isolate and identify the major bioactive compounds of the F3 fraction, and further tested their impact against cancer cell lines. This could identify the potential of anticancer agents from C. anacardioides.

4.
Food Chem ; 338: 128119, 2021 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-33091976

RESUMO

The inhibition of the α-amylase and α-glucosidase activity facilitates the maintenance of circulating glucose levels by decreasing the rate of blood sugar absorption. Existing enzyme inhibitors such as acarbose, miglitol, and voglibose are used for inhibiting the activity of these enzymes, however, alternative solutions are required to avoid the side-effects of using these drugs. The current study aims to review recent evidence regarding the in vitro α-amylase and α-glucosidase inhibition activities of extracts derived from selected fruit, vegetables, and mushrooms. The mechanisms of action of the extracts involved in the inhibition of both enzymes are also presented and discussed. Compounds including flavonoids, phenolic acids, anthocyanins, saponins, carotenoids, terpenes, sugars, proteins, capsaicinoids, fatty acids, alkaloids have been shown to have α-amylase and α-glucosidase inhibition activities. Harvesting period, maturity stage, sample preparation, extraction technique, and solvent type are parameters that affect the α-amylase and α-glucosidase inhibition activities of the extracts.


Assuntos
Agaricales/química , Frutas/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/farmacologia , Verduras/química , alfa-Amilases/antagonistas & inibidores , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Extratos Vegetais/isolamento & purificação
5.
Mol Biol Rep ; 47(2): 897-905, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31724126

RESUMO

Pancreatic cancer (PC) is one of the leading causes of cancer death in Western societies. The absence of specific symptoms, late diagnosis and the resistance towards chemotherapy result in significant treatment difficulties. As such, it is important to find more effective therapeutic agents for the treatment of PC. Helicteres hirsuta Lour. (H. hirsuta) has been traditionally used in many countries for the treatment of various ailments, indicating that it contains potential therapeutic agents. This study aimed to derive different fractions from the saponin-enriched extract of H. hirsuta stem using RP-HPLC and examine the in vitro anti-pancreatic cancer activity of the derived fractions (F0-F5). With the exception of F0, the five fractions (F1-F5) possessed strong inhibitory activity against PC cells at IC50 values of 3.11-17.12 µg/mL. The flow cytometry assays revealed the active fractions caused cell cycle arrest at S phase and promoted apoptosis in MIAPaCa-2 PC cells. The LC/MS analysis revealed that the isolated fractions contained bioactive compounds, such as caffeic acid, rosmarinic acid, sagerinic acid, usnic acid, cucurbitacins and absinthin. It can be concluded that the fractions isolated from H. hirsuta stem exhibit potent in vitro anti-pancreatic cancer activity and thus warrant further in vivo studies to assess their activity against PC followed by isolation of individual bioactive compounds and the evaluation of their anti-pancreatic cancer activity.


Assuntos
Malvaceae/metabolismo , Neoplasias Pancreáticas/tratamento farmacológico , Extratos Vegetais/farmacologia , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Neoplasias Pancreáticas/metabolismo , Fitoterapia/métodos , Saponinas/farmacologia
6.
J Food Sci Technol ; 56(3): 1438-1444, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30956323

RESUMO

UV-C (180-280 nm) has been shown to extend the postharvest shelf-life of many horticulture crops. In this study, Tahitian limes (Citrus latifolia) were exposed to 0, 3.4, 7.2 and 10.5 kJ m-2 UV-C then stored for 28 days in air at 10 °C and 80% RH. Weight loss, peel colour, calyx abscission, ethylene production, respiration rate, total soluble solids (TSS), titratable acidity (TA) and acceptability index were assessed. The results showed that UV-C treatment maintained lime peel green colour and retained calyx attachment after 28 days storage. UV-C treatment also affected endogenous ethylene production and respiration rate, where the highest UV-C treatment (10.5 kJ m-2) maintained low ethylene production and low respiration rates after 28 days storage with no differences between the different UV-C intensities. In terms of fruit acceptability, limes were exposed to 10.5 kJ m-2 UV-C had a 60% acceptability index after 28 days storage, while untreated control fruit retained acceptability of 39%. In general, the pre-storage UV-C treatments did not affect fruit weight loss, TSS or TA contents during storage.

7.
Mol Biol Rep ; 46(3): 3265-3273, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30945069

RESUMO

Catharanthus roseus (L.) G. Don (C. roseus) is a well-known medicinal plant for its source of alkaloids solely found in the leaves. Other parts including the root are usually discarded after the alkaloid extraction. This study sought to investigate phytochemical profiles, antioxidant, antimicrobial and cytotoxic properties of the C. roseus root extract (RE) and its two sub-fractions including saponin-enriched (SE) and aqueous (AQ) fractions. The results showed that the RE was a rich source of saponins (1744.44 mg ESE/g) and phenolics (51.27 mg GAE/g), which comprised of gallic acid (25.74 mg/g), apigenin (1.45 mg/g) and kaempferol (1.58 mg/g). The SE fraction was enriched with 31% of saponins and 63% of phenolics higher than those of the RE; whereas the concentrations of saponins and phenolics of the AQ fraction were lower than those of the RE by 40% and 74%, respectively. The content of gallic acid in the SE fraction was 1.4-fold and 1.5-fold higher than those of the RE or AQ fraction, respectively. The SE fraction demonstrated potent antioxidant capacity, which was significantly higher than the RE or AQ fraction, and also exhibited strong anti-proliferative activity against 11 cancer cell lines including A2780 (ovarian), H460 (lung), A431 (skin), MIA PaCa-2 (pancreas), Du145 (prostate), HT29 (colon), MCF-7 (breast), BE2-C (neuroblastoma), SJ-G2, U87 and SMA (glioblastoma) with low GI50 values (≤ 2.00 µg/mL). The SE fraction was also shown to effectively inhibit the growth of both bacteria (Escherichia coli, Enterobacter aerogenes and Staphylococccus lugdunensis) and fungi (Candida albicans and Aspergillus niger). These findings warrant further investigation to isolate major compounds from the SE fraction and further test their antioxidant, anticancer and antimicrobial activities.


Assuntos
Catharanthus/química , Catharanthus/metabolismo , Extratos Vegetais/farmacologia , Alcaloides/farmacologia , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Antioxidantes/metabolismo , Linhagem Celular Tumoral/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Flavonoides/farmacologia , Humanos , Fenóis , Compostos Fitoquímicos/metabolismo , Extratos Vegetais/metabolismo , Raízes de Plantas/metabolismo , Plantas Medicinais/metabolismo , Saponinas
8.
Molecules ; 24(3)2019 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-30709047

RESUMO

Pancreatic cancer (PC) is a complex, heterogeneous disease with a dismal prognosis. Current therapies have failed to improve survival outcomes, urging the need for discovery of novel targeted treatments. Bispidinone derivatives have yet to be investigated as cytotoxic agents against PC cells. The cytotoxic effect of four bispidinone derivatives (BisP1: 1,5-diphenyl-3,7-bis(2-hydroxyethyl)-3,7-diazabicyclo[3.3.1]nonan-9-one; BisP2: 3,7-bis-(2-(S)-amino-4-methylsulfanylbutyryl)-1,5-diphenyl-3,7-diazabicyclo[3.3.1]nonan-9-one dihydrochloride; BisP3: [2-{7-[2-(S)-tert-butoxycarbonylamino-3-(1H-indol-3-yl)-propionyl]-9-oxo-1,5-diphenyl-3,7-diazabicyclo[3.3.1]non-3-yl}-1-(S)-(1H-indol-3-ylmethyl)-2-oxoethyl]-carbamic acid tertbutyl ester; BisP4: 3,7-bis-[2-(S)-amino-3-(1H-indol-3-yl)-propionyl]-1,5-diphenyl-3,7-diazabicyclo[3.3.1]nonan-9-one dihydrochloride) was assessed against PC cell lines (MiaPaca-2, CFPAC-1 and BxPC-3). Cell viability was assessed using a Cell Counting Kit-8 (CCK-8) colorimetric assay, while apoptotic cell death was confirmed using fluorescence microscopy and flow cytometry. Initial viability screening revealed significant cytotoxic activity from BisP4 treatment (1 µM⁻100 µM) on all three cell lines, with IC50 values for MiaPaca-2, BxPC-3, and CFPAC-1 16.9 µM, 23.7 µM, and 36.3 µM, respectively. Cytotoxic treatment time-response (4 h, 24 h, and 48 h) revealed a 24 h treatment time was sufficient to produce a cytotoxic effect on all cell lines. Light microscopy evaluation (DAPI staining) of BisP4 treated MiaPaca-2 PC cells revealed dose-dependent characteristic apoptotic morphological changes. In addition, flow cytometry confirmed BisP4 induced apoptotic cell death induction of activated caspase-3/-7. The bispidinone derivative BisP4 induced an apoptosis-mediated cytotoxic effect on MiaPaca-2 cell lines and significant cytotoxicity on CFPAC-1 and BxPC-3 cell lines. Further investigations into the precise cellular mechanisms of action of this class of compounds are necessary for potential development into pre-clinical trials.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Compostos Bicíclicos Heterocíclicos com Pontes/química , Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia , Antineoplásicos/síntese química , Compostos Bicíclicos Heterocíclicos com Pontes/síntese química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Humanos , Estrutura Molecular , Neoplasias Pancreáticas
9.
Foods ; 8(1)2019 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-30634422

RESUMO

Calyx browning and internal quality loss are major physiological causes for the loss of quality in citrus fruit during storage. While the symptoms of calyx senescence are only superficial, it can affect the appearance and consumer acceptability of citrus fruit. In this study, continuous ethylene exposure at different storage temperatures was investigated to assess their effect on calyx senescence and internal qualities in 'Afourer' mandarin and Navel orange fruit during storage. 'Afourer' mandarin fruit were stored at ≤0.001 (equivalent to ethylene-free air), 0.01, 0.1 and 1 µL L-1 of ethylene at either 5, 10 or 20 °C, whilst in a parallel experiment, Navel oranges were exposed to ≤0.001, 0.1 and 1 µL L-1 ethylene at either 1 or 10 °C. Changes in external and internal postharvest quality parameters were assessed for up to 8 weeks for 'Afourer' mandarins and 10 weeks for Navel oranges. At all storage temperatures, high levels of ethylene were found to increase the level of calyx senescence, weight loss, loss of fruit firmness and respiration rates. Also, there were significant effects of ethylene and storage temperatures on total soluble solids (TSS) content, titratable acidity (TA), and ethanol accumulation in both citrus species. Continuous exposure to high ethylene also significantly reduced vitamin C and ferric reducing antioxidant power (FRAP) in 'Afourer' mandarins after 8 weeks of storage. Overall, ethylene treatments had a significant effect on both the external and internal qualities of the fruit during storage. The relationship between ethylene concentrations and storage temperatures demonstrate that lowering atmospheric ethylene levels at reduced storage temperatures maintain fruit quality during long term storage.

10.
Data Brief ; 21: 1033-1036, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30450396

RESUMO

This data article indicates the in vitro cytotoxicity of kaempferol and gallic acid across different cancer cell lines including A2780 (ovarian), H460 (lung), A431 (skin), MIA PaCa-2 (pancreas), Du145 (prostate), HT29 (colon), MCF-7 (breast), BE2-C (neuroblastoma), SJ-G2, U87 and SMA (glioblastoma). The dataset showed that the inhibitory activity of kaempferol was comparatively stronger than gallic acid. Thereby, kaempferol is offered as a potent anticancer agent for further investigation and beneficial as a dietary supplement. The data within this article relates to the research article entitled "Screening phytochemical content, antioxidant, antimicrobial and cytotoxic activities of Catharanthus roseus (L.) G. Don stem extract and its fractions" (Pham et al., 2018).

11.
Mol Biol Rep ; 45(6): 2125-2133, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30209740

RESUMO

Helicteres hirsuta Lour. (H. hirsuta) has been considered as a herbal medicine for the treatment of malaria and diabetes but limited studies have been conducted on its anticancer and antibacterial properties. In this study, the in vitro antibacterial and anticancer properties of the leaf and stem extracts and their two sub-fractions (aqueous and saponin-enriched butanol fractions) prepared from H. hirsuta were elucidated. MTT and CCK-8 assays were employed to assess their in vitro anticancer properties against various cancer cell lines. The antibacterial activity was assessed using the disc diffusion method and minimum inhibitory concentration (MIC) values were determined. The results revealed that the saponin-enriched fractions from H. hirsuta leaves and stems showed the highest antibacterial activity against E. coli (MIC values of 2.50 and 5.00 mg/mL, respectively) and S. lugdunensis (MIC values of 0.35 and 0.50 mg/mL, respectively). Importantly, these saponin-enriched fractions possessed strong anticancer activity in vitro towards a range of cancer cell lines including MIA PaCa-2 (pancreas); A2780 (ovarian); H460 (lung); A431 (skin); Du145 (prostate); HT29 (colon); MCF-7 (breast); SJ-G2, U87, SMA (glioblastoma) and BE2-C (neuroblastoma) at low doses (GI50 values of 0.36-11.17 µg/mL). They especially revealed potent anti-pancreatic cancer activity in vitro against MIA PaCa-2, BxPC-3 and CFPAC-1 cells with IC50 values of 1.80-6.43 µg/mL. This finding provides scientific evidence of the cytotoxic activity of the extracts prepared from H. hirsuta leaves and stems, and suggests further studies to isolate active compounds for development of new anticancer agents from these plant extracts.


Assuntos
Linhagem Celular Tumoral/efeitos dos fármacos , Malvaceae/química , Malvaceae/metabolismo , Extratos Vegetais/uso terapêutico , Antibacterianos , Anticarcinógenos , Antioxidantes , Escherichia coli/efeitos dos fármacos , Humanos , Malvaceae/genética , Testes de Sensibilidade Microbiana , Fitoterapia/métodos , Folhas de Planta , Caules de Planta , Plantas Medicinais/química , Staphylococcus lugdunensis/efeitos dos fármacos
12.
J Food Sci Technol ; 55(7): 2467-2475, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30042562

RESUMO

The green Tahitian limes (Citrus latifolia) were exposed to 7.2 kJ m-2 UV-C and 0.5 µL L-1 1-methylcyclopropene (1-MCP) treatments both separately and in combination. After treatment, fruit were stored in ethylene free (i.e. air containing < 0.005 µL L-1) or 0.1 µL L-1 ethylene at 20 °C and 100% RH. The results showed that UV-C treatment delayed skin degreening and reduced endogenous ethylene production compared to untreated control fruit, however these effects reduced over the storage time. As expected, 1-MCP inhibited ethylene production, reduced calyx abscission and retained peel greenness during the storage. Both of the combination treatments, 1-MCP + UV-C and UV-C + 1-MCP reduced endogenous ethylene production and delayed skin yellowing. In all treatments, UV-C and 1-MCP resulted in lower fruit respiration rates than untreated control fruit, however this effect diminished during 7 and 14 days storage for fruits stored in air and 0.1 µL L-1 ethylene atmosphere, respectively. There was no difference in weight loss, SSC, TA and SSC/TA ratio between the treatments and storage conditions. The results suggest that a pre-storage UV-C treatment, followed by storage at low level of ethylene improves the quality of limes, with the additional improvement when combined with 1-MCP treatment prior or after UV-C irradiation.

13.
Pancreas ; 47(6): 690-707, 2018 07.
Artigo em Inglês | MEDLINE | ID: mdl-29894418

RESUMO

Pancreatic cancer (PC) is one of the most devastating human cancers, and despite the significant advances in the current therapeutic options, the overall survival rate for PC has remained static for the past 50 years. Plant-derived bioactive compounds play a vital role in cancer therapeutics by providing new lead compounds for future drug development. Therefore, the isolation, characterization, and identification of new bioactive compounds for the prevention and treatment of cancer continue to be an important aspect of natural product research. Many in vitro and in vivo studies published in the last few decades have established strong links between the phytochemical profile of eucalypts and anticancer activity. However, only a small number of these reports have attempted to demonstrate a relationship between the biological activity of eucalypt extracts and PC. This review focuses on potential anti-PC effects of an array of bioactive compounds present in various species of eucalypts. It also highlights the necessity for further in vitro and in vivo studies to develop a complete understanding of the potential this group of plants has for the development of potent and specific chemotherapeutic drugs for PC.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Produtos Biológicos/uso terapêutico , Eucalyptus/química , Neoplasias Pancreáticas/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Austrália , Produtos Biológicos/química , Eucalyptus/classificação , Humanos , Estrutura Molecular , Fitoterapia/métodos , Especificidade da Espécie
14.
Biomed Pharmacother ; 105: 449-460, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29879629

RESUMO

New therapeutic strategies such as the development of novel drugs and combinatorial therapies with existing chemotherapeutic agents are urgently needed to improve the clinical prognosis of pancreatic cancer. We have previously reported the antiproliferative properties of aqueous crude Eucalyptus microcorys extract against pancreatic cancer cell lines. In this study, bioassay-guided fractionation of the aqueous crude E. microcorys extract using RP-HPLC and subsequent assessment of the resultant fractions (F1-F5) for their antioxidant activity and cytotoxicity against pancreatic cancer cell lines were performed. The molecular mechanisms associated with the cytotoxicity was characterised by studying the effects of the most potent fraction-1 (F1) on apoptosis and cell cycle profiles as well as its phytochemical constituents by LC-ESI/MS/MS. F1 displayed significantly greater antioxidant activity in three different assays (p < 0.05). Moreover, F1 exhibited significantly greater antiproliferative activity (IC50 = 93.11 ±â€¯3.43 µg/mL) against MIA PaCa-2 cells compared to the other four fractions (p < 0.05). F1 induced apoptosis by regulating key apoptotic proteins- Bcl-2, Bak, Bax, cleaved PARP, procaspase-3 and cleaved caspase-3 in MIA PaCa-2 cells, suggesting the involvement of intrinsic mitochondrial apoptotic pathway and arrested cells at G2/M phase. A combination of gemcitabine and F1 exerted a greater effect on apoptosis and cell cycle arrest than F1 or gemcitabine alone (p < 0.05). LC-ESI/MS/MS revealed the tentative identities of phytochemicals present in F1 and their similarities with the phenolic compounds previously reported in Eucalyptus with antipancreatic cancer activity. Our study shows that the polyphenol and antioxidant-rich fraction of E. microcorys extract is a promising candidate for developing mono or combination therapies against pancreatic cancer.


Assuntos
Apoptose , Pontos de Checagem do Ciclo Celular , Eucalyptus/química , Neoplasias Pancreáticas/patologia , Extratos Vegetais/química , Folhas de Planta/química , Antioxidantes/farmacologia , Apoptose/efeitos dos fármacos , Proteínas Reguladoras de Apoptose/metabolismo , Ciclo Celular/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Cromatografia de Fase Reversa , Humanos
15.
In Vitro Cell Dev Biol Anim ; 53(7): 604-615, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28452004

RESUMO

In spite of the recent advancements in oncology, the overall survival rate for pancreatic cancer has not improved over the last five decades. Eucalypts have been linked with cytotoxic and anticancer properties in various studies; however, there is very little scientific evidence that supports the direct role of eucalypts in the treatment of pancreatic cancer. This study assessed the anticancer properties of aqueous and ethanolic extracts of four Eucalyptus species using an MTT assay. The most promising extracts were further evaluated using a CCK-8 assay. Apoptotic studies were performed using a caspase 3/7 assay in MIA PaCa-2 cells. The aqueous extract of Eucalyptus microcorys leaf and the ethanolic extract of Eucalyptus microcorys fruit inhibited the growth of glioblastoma, neuroblastoma, lung and pancreatic cancer cells by more than 80% at 100 µg/mL. The E. microcorys and Eucalyptus saligna extracts showed lower GI50 values than the ethanolic Eucalyptus robusta extract in MIA PaCa-2 cells. Aqueous E. microcorys leaf and fruit extracts at 100 µg/mL exerted significantly higher cell growth inhibition in MIA PaCa-2 cells than other extracts (p < 0.05). Statistically similar IC50 values (p > 0.05) were observed in aqueous E. microcorys leaf (86.05 ± 4.75 µg/mL) and fruit (64.66 ± 15.97 µg/mL) and ethanolic E. microcorys leaf (79.30 ± 29.45 µg/mL) extracts in MIA PaCa-2 cells using the CCK-8 assay. Caspase 3/7-mediated apoptosis and morphological changes of cells were also witnessed in MIA PaCa-2 cells after 24 h of treatment with the extracts. This study highlighted the significance of E. microcorys as an important source of phytochemicals with efficacy against pancreatic cancer cells. Further studies are warranted to purify and structurally identify individual compounds and elucidate their mechanisms of action for the development of more potent and specific chemotherapeutic agents for pancreatic cancer.


Assuntos
Antineoplásicos/farmacologia , Eucalyptus/química , Extratos Vegetais/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Forma Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Desoxicitidina/análogos & derivados , Desoxicitidina/farmacologia , Humanos , Concentração Inibidora 50 , Gencitabina
16.
Chem Biodivers ; 14(3)2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-27935659

RESUMO

While the pharmacological and toxicological properties of eucalypts are well known in indigenous Australian medicinal practice, investigations of the bioactivity of eucalypt extracts against high mortality diseases such as pancreatic cancer in Western medicine have to date been limited, particularly amongst the genera Corymbia and Angophora. Four Angophora and Corymbia species were evaluated for their phytochemical profile and efficacy against both primary and secondary pancreatic cancer cell lines. The aqueous leaf extract of Angophora hispida exhibited statistically higher total phenolic content (107.85 ± 1.46 mg of gallic acid equiv. per g) and total flavonoid content (57.96 ± 1.93 mg rutin equiv. per g) and antioxidant capacity compared to the other tested eucalypts (P < 0.05). Both A. hispida and A. floribunda aqueous extracts showed statistically similar saponin contents. Angophora floribunda extract exerted significantly greater cell growth inhibition of 77.91 ± 4.93% followed by A. hispida with 62.04 ± 7.47% (P < 0.05) at 100 µg/ml in MIA PaCa-2 cells with IC50 values of 75.58 and 87.28 µg/ml, respectively. More studies are required to isolate and identify the bioactive compounds from these two Angophora species and to determine their mode of action against pancreatic malignancies.


Assuntos
Myrtaceae/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Austrália , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Myrtaceae/metabolismo , Neoplasias Pancreáticas/metabolismo , Neoplasias Pancreáticas/patologia , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo , Saponinas/análise
17.
Foods ; 5(3)2016 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-28231150

RESUMO

Several studies have shown that UV-C (ultraviolet C) irradiation promotes the bioactive compounds and antioxidants of fresh fruits and vegetables. The aim of this study was to apply UV irradiation in dried lemon pomace powder for enhancing its phenolic content and antioxidant properties, thus more bioactive compounds should be available for extraction and utilization. Lemon pomace dried powder was placed under a UV lamp and treated with dosages of 4, 19, 80 and 185 kJ·m-2, while untreated powder was used as a control. UV-C irradiation significantly affected the total phenolic content, total flavonoid content, proanthocyanidins, and antioxidant capacity measured by cupric reducing antioxidant capacity (CUPRAC) and ferric reducing antioxidant power (FRAP) of the lemon pomace dried powder, while it did not affect the vitamin C content. UV-C irradiation of 19 kJ·m-2 resulted in 19% higher total phenolic content than the control, while UV-C irradiation of 180 kJ·m-2 resulted in 28% higher total flavonoid content than the control. The antioxidant capacity was reduced when UV-C irradiation more than 4 kJ·m-2 was applied. The results of this study indicate that UV-C treatment has the potential to increase the extraction of bioactive compounds of dried lemon pomace at relatively high dosages.

18.
Chem Biodivers ; 12(6): 907-24, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-26080737

RESUMO

The genus Eucalyptus (Myrtaceae) is mainly native to Australia; however, some species are now distributed globally. Eucalyptus has been used in indigenous Australian medicines for the treatment of a range of aliments including colds, flu, fever, muscular aches, sores, internal pains, and inflammation. Eucalyptus oils containing volatile compounds have been widely used in the pharmaceutical and cosmetics industries for a multitude of purposes. In addition, Eucalyptus extracts containing nonvolatile compounds are also an important source of key bioactive compounds, and several studies have linked Eucalyptus extracts with anticancer properties. With the increasing research interest in Eucalyptus and its health properties, this review briefly outlines the botanical features of Eucalyptus, discusses its traditional use as medicine, and comprehensively reviews its phytochemical and anticancer properties and, finally, proposes trends for future studies.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Eucalyptus/química , Compostos Fitoquímicos/química , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Humanos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
19.
Antioxidants (Basel) ; 4(4): 647-61, 2015 Oct 08.
Artigo em Inglês | MEDLINE | ID: mdl-26783950

RESUMO

Euphorbia tirucalli is a succulent shrub or small tree that is native to the African continent, however, it is widely cultivated across the globe due to its use in traditional medicines to treat ailments, ranging from scorpion stings to HIV. Recent studies have identified compounds present in the latex of the plant, including a range of bi- and triterpenoids that exhibit bioactivity, including anticancer activity. This study aimed to optimize water extraction conditions for high-yield total phenolic content recovery, to prepare methanol and aqueous extracts from the aerial sections of the plant, and to test the phytochemical, antioxidant, and anti-cancer properties of these extracts. Water extraction of total phenolic compounds (TPC) was optimized across a range of parameters including temperature, extraction time, and plant mass-to-solvent ratio. The water extract of the E. tirucalli powder was found to contain TPC of 34.01 mg GAE (gallic acid equivalents)/g, which was approximately half that of the methanol extract (77.33 mg GAE/g). The results of antioxidant assays showed a uniform trend, with the methanol extract's antioxidant reducing activity exceeding that of water extracts, typically by a factor of 2:1. Regression analysis of the antioxidant assays showed the strongest correlation between extract TPC and antioxidant activity for the ABTS (2,2-azino-bis(3-ethyl-benzothiazoline-6-sulfonic acid) and DPPH (2,2-diphenyl-1-picrylhydrazyl) methods. The methanol extract also showed greater growth inhibition capacity towards the MiaPaCa-2 pancreatic cancer cell line. These data suggest that further investigations are required to confirm the source of activity within the E. tirucalli leaf and stems for potential use in the nutraceutical and pharmaceutical industries.

20.
Org Biomol Chem ; 12(36): 6994-7003, 2014 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-24933586

RESUMO

Six novel functional monomers: 4-(4-vinylphenyl)pyridine (M1), 4'-vinylbiphenyl-4-ol (M2), N,N-dimethyl-4'-vinylbiphenyl-3-amine (M3), (4'-vinylbiphenyl-4-yl)methanol (M4), 4'-vinylbiphenyl-4-carboxylic acid (M5) and 4-hydroxy-5-methyl-4'-vinylbiphenyl-3-carboxylic acid (M6), were examined for their ability to imprint theophylline (1). Using a molecular modelling-NMR titration approach, M2 and M6 were predicted to give rise to the most specific molecularly imprinted polymers (MIPs). Rebinding analysis suggests that no imprinting effect resulted from the polymerisation of monomers M1, M5 and M6, but modest to good levels of imprinting were evident from monomers M2, M3 and M4 with IF values ranging from 1.1 (MIPM3, 20 mg) to 45 (MIPM2, 10 mg). The selective recognition of 1 varied as a function of polymer mass used. At low polymer loadings MIPM2 gave the very high IF of 45, reducing to IF = 4.1­2.3 at 20­40 mg polymer loading. With monomer M2, microwave synthesised MIP (MW-MIPM2) was examined. The MW-MIPM2 displayed lower specific rebinding than its conventionally produced counterpart (MIPM2) with IF values ranging from 1.6­2.3 (cf., MIPM2 IF 2.3­45), but significantly higher levels of rebinding with 25­52% of 1 rebound from a 0.080 mM CH3CN solution of 1 (cf., MIPM2 5­25%). MW-MIPM2 displayed a lower BET surface area than MIPM2 (185 m(2) g(−1)vs. 240 m(2) g(−1)), and lower surface (zeta) potential (−13.1 ± 8.22 mV vs. −31.4 ± 4.84 mV). Freundlich isotherm analysis revealed that MW-MIPM2 possessed higher affinity binding sites for 1 than MIPM2 with Kd values of 1.38 and 2.31 respectively. In addition, MW-MIPM2 also exhibits a higher number of binding sites (NT) compared to MW-NIPM2 (0.72 and 0.41 mg g(−1), respectively). In specificity studies using caffeine (2), MIPM2 displayed a two-fold preference for rebinding of 1 and MW-MIPM2 a five-fold preference for 1 over 2. The quantity of 2 bound in both cases was consistent with non-specific binding events. In competitive rebinding experiments, increased discrimination in favour of 1 over 2 was observed.

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