The present study evaluated the anticancer potential of 11 plants used in Bangladeshi folk medicine. The extracts were tested for cytotoxicity using the brine shrimp lethality assay, sea urchin eggs ...assay, hemolysis assay and MTT assay using tumor cell lines. The extract of
Oroxylum indicum showed the highest toxicity on all tumor cell lines tested, with an IC
50 of 19.6
μg/ml for CEM, 14.2
μg/ml for HL-60, 17.2
μg/ml for B-16 and 32.5
μg/ml for HCT-8. On the sea urchin eggs, it inhibited the progression of cell cycle since the frist cleavage (IC
50
=
13.5
μg/ml). The extract of
Aegle marmelos exhibited toxicity on all used assays, but in a lower potency than
Oroxylum indicum. In conclusion, among all tested extracts, only the extracts of
Oroxylum indicum,
Moringa oleifera and
Aegles marmelos could be considered as potential sources of anticancer compounds. Further studies are necessary for chemical characterization of the active principles and more extensive biological evaluations.
Several 3-arylamino and 3-alkoxy-nor-β-lapachone derivatives were synthesized in moderate to high yields and found to be highly potent against cancer cells SF295 (central nervous system), HCT8 ...(colon), MDA-MB435 (melanoma), and HL60 (leukemia), with IC50 below 2 μM. The arylamino para-nitro and the 2,4-dimethoxy substituted naphthoquinones showed the best cytoxicity profile, while the ortho-nitro and the 2,4-dimethoxy substituted ones were more selective than doxorubicin and similar to the precursor lapachones, thus emerging as promising new lead compounds in anticancer drug development.
Display omitted
•An itinerary for Rocha pears biofortification with calcium was developed in two orchards.•Monitoring of photoassimilates revealed only minor changes during Ca ...biofortification.•Accumulation indexes for calcium reached 47 %–63 % and 24 %–59 %.•Accumulation of Ca prevailed in the epidermis and central region of the fruits.•Physicochemical characteristics of fresh and heat-treated fruits did not vary substantially.
Low dietary intake of Ca in humans has been epidemiologically linked to various diseases, which can have serious health consequences over time. Accordingly, the development of an agronomic itinerary for Ca biofortification of Rocha pears and the assessment of physicochemical deviations prompted this study. Two orchards with contrasting soil and water characteristics were selected, characterized through orthophotomaping and, during fruits development, leaves were sprayed twice with Ca(NO3)2 (0.1, 0.3 and 0.6 kg ha−1) or CaCl2 (0.4, 0.8 and 1.6 kg ha−1), followed by pulverization only with CaCl2 (first once with 4 kg ha−1 and then four times with 8 kg ha−1). During fruits development net photosynthesis, stomatal conductance, transpiration rates, instantaneous and water use efficiency, only showed minor deviations, which indicated that the threshold of toxicity was not surpassed. Calcium contents varied during fruits development and at harvesting the average biofortification index varied between 47 %–63 % and 24 %–59 % in each of the orchards. Besides, the equatorial region of the fruits showed for all treatments (substantially in Ca treated samples) higher Ca contents in the epidermal and in the central regions. Fresh and heat-treated fruits (in a thermomix at 90 °C, during 10 min) biofortified with Ca only revealed minor differences and the sensory acceptability did not vary markedly. It is concluded that, although prevailing a heterogeneous distribution of Ca in fruit tissues, high indexes of biofortification in Rocha pears can be prompt in the orchards, without substantial physicochemical changes. Accordingly, agronomic biofortification with Ca can be used as a strategy for benefiting consumer’s health.
Chemically sulfated xyloglucan (S_XLG) was applied to encapsulate hydrophilic quercetin sulfate (Q_SO3) into superparamagnetic nanocomposites (MNSXQ_SO3) synthesized via interfacial polyaddition ...reaction. This nanoplatform was evaluated concerning in vitro antitumor activity, drug release profile, and magnetic behavior under a magnetic field. MNSXQ_SO3 exhibited antitumor activity against four human tumor cell lines: leukemia HL-60 (IC50 = 1.58 ± 0.54 μg mL−1), glioblastoma SNB-19 (IC50 = 8.77 ± 0.36 μg mL−1), colorectal carcinoma HCT-116 (IC50 = 8.69 ± 0.21 μg mL−1) and prostate PC3 (IC50 = 17.42 ± 3.57 μg mL−1). Additionally, MNSXQ_SO3 was able to delay the release of Q_SO3 (76 %) compared to the free Q_SO3 (100 %), after 48 h of drug delivery assay, revealing a release profile compatible with the Korsmeyer-Peppas kinetic model. These results represent a relevant progress in the production of multifunctional hybrid nanocarriers, providing a versatile nanocomposite with potential for targeted drug delivery and theranostic applications.
Display omitted
•Magnetic nanocomposites are synthesized with chemically sulfated xyloglucan.•Superparamagnetic iron oxide nanoparticles are entrapment within the nanocomposites.•Hydrophilic quercetin is successfully incorporated into magnetic nanomaterial.•The hybrid nanosystem was able to modify the drug release profile of hydrophilic quercetin.•Development of a promising hybrid nanoproduct able to be applied in theranostic proposals.
The search for new anti-cancer drugs is one of the most prominent research areas of natural products. Numerous active compounds isolated from Brazilian Cerrado plant species have been studied with ...promising results.
To investigate the cytotoxic potential of 412 extracts from Brazilian Cerrado plants used in traditional medicine belonging to 21 families against tumor cell lines in culture.
Maceration of 50 plant species resulted in 412 hexane, dichloromethane, ethanol and hydroalcohol extracts. The cytotoxicity of the extracts was tested against human colon carcinoma (HCT-8), melanoma (MDA-MB-435), and brain (SF-295) tumor cell lines, using the thiazolyl blue test (MTT) assay. Bioassay-guided fractionation was performed for one active extract.
Twenty-eight of the 412 tested extracts demonstrated a substantial antiproliferative effect, at least 85% inhibition of cell proliferation at 50
μg/mL against one or more cell lines. Those extracts are obtained from different parts of Anacardiaceae, Annonaceae, Apocynaceae, Clusiaceae, Flacourtiaceae, Sapindaceae, Sapotaceae, Simaroubaceae and Zingiberaceae. Complete dose-response curves were generated and IC
50 values were calculated for these active extracts against four cell lines HCT-8, MDA-MB-435, SF-295 and HL-60 (leukemia), and their direct cytotoxic effects were determined. In summary, 14 extracts of 13 species showed toxicity in all tested tumor cell lines, with IC
50 values ranging from 0.1 to 19.1
μg/mL. The strongest cytotoxic activity was found for the hexane extract of
Casearia sylvestris var.
lingua stem bark, with an IC
50 of 0.1
μg/mL for HCT-8, 0.9
μg/mL for SF-295, 1.2
μg/mL for MDA-MB-435, and 1.3
μg/mL for HL-60, and
Simarouba versicolor root bark, with an IC
50 of 0.5
μg/mL for HCT-8, 0.7
μg/mL for SF-295, 1.5
μg/mL for MDA-MB-435, 1.1
μg/mL for HL-60. Bioassay-guided fractionation of the last extract led to the isolation of glaucarubinone, which showed pronounced activity against the four cell lines studied. Further studies of the active extracts are necessary for chemical characterization of the active compounds and more extensive biological evaluations.
The chemical composition and biological activity of a sample of yellow propolis from Mato Grosso do Sul, Brazil (EEP-Y MS), were investigated for the first time and compared with green, brown, and ...red types of Brazilian propolis and with a sample of yellow propolis from Cuba. Overall, EEP-Y MS had different qualitative chemical profiles, as well as different cytotoxic and antimicrobial activities when compared to the other types of propolis assessed in this study and it is a different chemotype of Brazilian propolis. Absence of phenolic compounds and the presence of mixtures of aliphatic compounds in yellow propolis were determined by analysing 1H-NMR spectra and fifteen terpenes were identified by GC-MS. EEP-Y MS showed cytotoxic activity against human tumour strain OVCAR-8 but was not active against Gram-negative or Gram-positive bacteria. Our results confirm the difficulty of establishing a uniform quality standard for propolis from diverse geographical origins. The most appropriate pharmacological applications of yellow types of propolis must be further investigated.
The venom of amphibians is a fascinating source of active substances. In view of their medical importance and aiming to explore the amazing Brazilian biodiversity, we conducted bioprospecting of ...antiproliferative activity in extracts of Rhinella marina and Rhaebo guttatus toads occurring in the Southern Amazon of Mato Grosso, Brazil. LC–MS and HPLC analysis of the venom extracts of R. marina revealed four bufadienolides (telocinobufagin – 1, marinobufagin – 2, bufalin – 3 and resibufogenin – 4). R. guttatus venom extracts contained only marinobufagin (2). First, R. marina and R. guttatus venom extracts were evaluated for cytotoxicity against tumor cell lines by the MTT assay. All extracts revealed cytotoxicity, where R. marina extracts were comparable to doxorubicin (IC50 values ranging from 0.01 to 0.23 μg/mL). Only extracts of R. guttatus toad venom caused membrane disruption of human erythrocytes. The extracts were investigated for selective activity by determining their effect on stimulated human peripheral blood mononuclear cells (PBMC) with the Alamar Blue™ assay. The extracts were up to 80-fold more selective against leukemia cells when compared to dividing leukocytes. Aiming to confirm these antiproliferative effects, BrdU incorporation into DNA was measured in HL-60 treated cells with R. marina venom extracts. These extracts decreased BrdU incorporation at both concentrations tested. In summary, nine extracts of R. marina and R. guttatus venom showed pronounced lethal and discriminating effects on tumor lines, especially those from R. marina, highlighting toad parotoid gland secretions as a promising source for novel lead anticancer chemicals.
•Extracts from Rhinella marina and Rhaebo guttatus displayed lethal effects on cancer lines.•The extracts from venoms reduced proliferation of HL-60 cells by BrdU labeling.•R. marina extracts were more selective against leukemia cells.•Four bufadienolides were identified in the R. marina extracts by LC–MS.•One bufadienolide were identified in the R. guttatus extracts by LC–MS.
The optimized extraction process of natural matrices such as propolis that results in extracts with significant compounds has been one of the main needs of the industry. The aim of this work was to ...analyze the content of the active components of Brazilian red propolis extracts previously treated with ultrasound, as well as to evaluate in vitro their performance regarding antioxidant capacity and against bacteria and tumor cells. The results of the chromatographic analysis showed the influence of ultrasound treatment for higher yields of formononetin and kaempferol. However, just a higher content of these two components was not enough to interfere with higher concentrations of phenolic compounds and flavonoids among the extracts. The ten extracts obtained showed activity against two bacterial strains, and eight of them showed >70% cytotoxicity against five neoplastic cell lines. These results demonstrated the influence of ultrasound technology as a pretreatment in obtaining the ethanolic extracts of propolis, increasing the possibility of the applicability of Brazilian red propolis in different areas.
Mimosa caesalpiniifolia is a native plant of the Brazilian northeast, and few studies have investigated its chemical composition and biological significance. This work describes the identification of ...the first chemical constituents in the ethanolic extract and fractions of M. caesalpiniifolia stem bark based on NMR, GC-qMS and HRMS analyses, as well as an assessment of their cytotoxic activity. GC-qMS analysis showed fatty acid derivatives, triterpenes and steroid substances and confirmed the identity of the chemical compounds isolated from the hexane fraction. Metabolite biodiversity in M. caesalpiniifolia stem bark revealed the differentiated accumulation of pentacyclic triterpenic acids, with a high content of betulinic acid and minor amounts of 3-oxo and 3β-acetoxy derivatives. Bioactive analysis based on total phenolic and flavonoid content showed a high amount of these compounds in the ethanolic extract, and ESI-(-)-LTQ-Orbitrap-MS identified caffeoyl hexose at high intensity, as well as the presence of phenolic acids and flavonoids. Furthermore, the evaluation of the ethanolic extract and fractions, including betulinic acid, against colon (HCT-116), ovarian (OVCAR-8) and glioblastoma (SF-295) tumour cell lines showed that the crude extract, hexane and dichloromethane fractions possessed moderate to high inhibitory activity, which may be related to the abundance of betulinic acid. The phytochemical and biological study of M. caesalpiniifolia stem bark thus revealed a new alternative source of antitumour compounds, possibly made effective by the presence of betulinic acid and by chemical co-synergism with other compounds.
The culture of preantral follicles as an in vitro model to evaluate the toxicity of new anticancer drug has being established. Therefore, the aim of this study was to evaluate the effect of ...quinoxaline derivative the 2 2- (XYZC 6H 3 –CH=N-NH)-quinoxaline, 1 (QX) on caprine preantral follicles. We evaluate the follicular morphology and activation, proliferation and apoptosis of granulosa cells and finally the protein (ABCB1) and genes expression (cyclin/Cdks), respectively involved in multidrug resistance and cell cycle progression. Ovarian fragments containing primordial and developing follicles were exposed (in vitro culture) to different concentrations of QX (QX1.5, QX3.0 or QX6.0 μM/mL) during 6 days. To evaluate the effect of QX, the ovarian tissue was exposed to Paclitaxel 0.1 μg/mL (PTX – negative control) or in culture media without QX (MEM). At the end of exposure time, we realized that the QX (all concentrations) increased (P < .05) the normal morphology of preantral follicles compared to control (not treated ovarian tissue) or MEM. However, QX6.0 showed a enhanced (P < .05) on follicular activation (burnout) and apoptosis than QX1.5 and QX3.0. Expression of ABCB1 was similar between QX1.5 and QX6.0 and both were lower than control, MEM and PTX. Interestingly, the apoptosis rate in QX3.0 was similar to control and MEM and lower then QX1.5; QX6.0 and PTX. We conclude that quinoxaline may be a promising chemotherapeutic agent, however, other concentrations within a defined range (2–5.5 μM) could be widely investigated.
•Quinoxaline (QX6.0) can cause follicular burnout in a more evident and intense way.•Quinoxaline at the lowest (1.5 μM) and at the highest (6.0 μM) concentration, seem to inhibit the expression of ABCB1.
PDF
