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Differential effect of CHL 1, CHL 2, or the combination of both flavonoids 48 hours after treatment. Pancreatic cell lines (A) MIA Paca and (B) Panc 28 were treated with CHL 1, CHL 2, or an equal concentration of both flavonoids for 48 hours. (C) MIA Paca and Panc 28 cell lines were treated with gemcitabine hydrochloride. Cell viability was determined by MTT assays and are represented as a percent of the control absorbance at a wavelength of 570nm. All data were collected at 24 h after treatment. Data shown are from representative experiments (mean± SE, n = 3). * p<0.05, significant difference between control and other concentrations for each compound. † and ‡ p<0.05, significant difference between the combination of CHL 1 + CHL 2 and CHL2; and CHL1+CHL2 and CHL1 and CHL2, respectively.
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Over 5000 flavonoids have been identified so far and many of these are known to have antineoplastic properties. The relationships between the targeting activities by these compounds on cancer cells and the specific features that determine their molecular structures are not completely elucidated. Here we report the differential cytotoxic effects of...
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Context 1
... PaCa-2 and Panc28 cells dosed with the combination of CHL1 and CHL2, display significantly lower cell viability as compared to treatment with either individual agent. (Figure 6A and 6B). Furthermore, the effect on cell viability observed at 48 hours after treatment with the combination of CHL1 and CHL2 on pancreatic cancer MIA PaCa-2 and Panc28 cells, was significantly greater than the effect observed at 48 hours after dosing the cells with gemcitabine hydrochloride ( Figure 6C) at effective concentrations (22,24). ...
Context 2
... 6A and 6B). Furthermore, the effect on cell viability observed at 48 hours after treatment with the combination of CHL1 and CHL2 on pancreatic cancer MIA PaCa-2 and Panc28 cells, was significantly greater than the effect observed at 48 hours after dosing the cells with gemcitabine hydrochloride ( Figure 6C) at effective concentrations (22,24). The effect on cell viability of combination treatment of CHL 1and CHL 2 on lung cancer A549 and colon cancer HCT 116 and CaCo 2 cells, did not differ from the results obtained with the individual compound, and returned to control levels after 48 hours in the colon cell lines (data not shown). ...
Context 3
... differential effects of the flavone versus the flavanone are further evidenced by the results obtained 48 hours after treatment with either compound or the combination of CHL 1 and CHL 2. While there is no significant change in viability of cancer cells of the lung (A549) or colon (HCT-116, CaCo-2), 48 hours after treatment with CHL 1, CHL 2, or the combination of both compounds as compared to the results obtained after 24 hours, this is not the case in pancreatic cancer cells. MIA PaCa and Panc28 pancreatic cancer cells treated with CHL 2 showed an increase in cell viability, whereas the flavone CHL 1 failed to have a significant effect as compared to the control (Figures 6A, 6B). Thus, there is no unexpected sustained effect of the flavone after 48 hours of treatment in cells of the pancreas. ...
Context 4
... PaCa-2 and Panc28 cells dosed with the combination of CHL1 and CHL2, display significantly lower cell viability as compared to treatment with either individual agent. (Figure 6A and 6B). Furthermore, the effect on cell viability observed at 48 hours after treatment with the combination of CHL1 and CHL2 on pancreatic cancer MIA PaCa-2 and Panc28 cells, was significantly greater than the effect observed at 48 hours after dosing the cells with gemcitabine hydrochloride ( Figure 6C) at effective concentrations (22,24). ...
Context 5
... 6A and 6B). Furthermore, the effect on cell viability observed at 48 hours after treatment with the combination of CHL1 and CHL2 on pancreatic cancer MIA PaCa-2 and Panc28 cells, was significantly greater than the effect observed at 48 hours after dosing the cells with gemcitabine hydrochloride ( Figure 6C) at effective concentrations (22,24). The effect on cell viability of combination treatment of CHL 1and CHL 2 on lung cancer A549 and colon cancer HCT 116 and CaCo 2 cells, did not differ from the results obtained with the individual compound, and returned to control levels after 48 hours in the colon cell lines (data not shown). ...
Context 6
... differential effects of the flavone versus the flavanone are further evidenced by the results obtained 48 hours after treatment with either compound or the combination of CHL 1 and CHL 2. While there is no significant change in viability of cancer cells of the lung (A549) or colon (HCT-116, CaCo-2), 48 hours after treatment with CHL 1, CHL 2, or the combination of both compounds as compared to the results obtained after 24 hours, this is not the case in pancreatic cancer cells. MIA PaCa and Panc28 pancreatic cancer cells treated with CHL 2 showed an increase in cell viability, whereas the flavone CHL 1 failed to have a significant effect as compared to the control (Figures 6A, 6B). Thus, there is no unexpected sustained effect of the flavone after 48 hours of treatment in cells of the pancreas. ...
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Citations
... Evaluating the cytotoxic activity and selectivity of Tacotanina isolated from C. tacotana on BC cells, we found that it is capable of inhibiting cell viability with high selectivity for cancer cells at concentrations between 56.9 and 72.7 µM, which is higher compared to the flavanone previously isolated from C. tacotana the 5,7-dihydroxy flavanone that inhibited cell viability and proliferation of colon adenocarcinoma (HT29), prostate cancer (PC-3), adenocarcinoma human alveolar basal epithelial (A549), breast adenocarcinoma (MDA-MB-231), and cervical squamous carcinoma (SiHa) cell lines [15], and another flavanones from C. leivensis the 3,5-dihydroxy-7-methoxyflavanone that showed mild cytotoxicity against the colon cell line (CaCo-2) (EC 50 = 120.80 uM) [22] and had activity on the mitochondrial membrane at varying concentrations (25, 50 and 100 µg/mL) [23]. Cytotoxicity of Tacotanina is even better than the activity found for other flavanones considered to be the main or most studied so far, 3 ,5,7-trihydroxy-4 -methoxyflavanone (hesperetin), which previously showed an IC 50 value of 129 and 87 µM for MDA-MB-231 and MCF-7, respectively [24], and 4 ,5,7-trihydroxyflavanone (naringenin) that inhibits the viability of MDA-MB-231 cells above 146.9 ...
Chromolaena tacotana is a source of flavonoids with antiproliferative properties in human breast cancer cells, the most common neoplasm diagnosed in patients worldwide. Until now, the mechanisms of cell death related to the antiproliferative activity of its flavonoids have not been elucidated. In this study, a novel flavanone (3′,4′-dihydroxy-5,7-dimethoxy-flavanone) was isolated from the plant leaves and identified by nuclear magnetic resonance (NMR) and mass spectrometry (MS). This molecule selectively inhibited cell proliferation of triple-negative human breast cancer cell lines MDA-MB-231 and MCF-7 whit IC50 values of 25.3 μg/mL and 20.8 μg/mL, respectively, determined by MTT assays with a selectivity index greater than 3. Early and late pro-apoptotic characteristics were observed by annexin-V/7-AAD detection, accompanied by a high percentage of the Bcl-2 anti-apoptotic protein inactivated and the activation of effector Caspase-3 and/or 7 in breast cancer cells. It was verified the decreasing of XIAP more than Bcl-2 anti-apoptotic proteins expression, as well as the XIAP/Caspase-7 and Bcl-2/Bax complexes dissociation after flavanone treatment. Docking and molecular modeling analysis between the flavanone and the antiapoptotic protein XIAP suggests that the natural compound inhibits XIAP by binding to the BIR3 domain of XIAP. In this case, we demonstrate that the new flavanone isolated from leaves of Chomolaena tacotana has a promising and selective anti-breast cancer potential that includes the induction of intrinsic apoptosis by downregulation of the anti-apoptotic proteins XIAP and Bcl-2. New studies should deepen these findings to demonstrate its potential as an anticancer agent.
... These compounds have an unsubstituted ring B and their cytotoxic activities on some cancer cell lines have already been reported 3 . It is generally accepted that among flavonoids, flavanones have a lowest cytotoxic effect on cancer cells 4 , however, this recognized property of flavanones can vary depending on the types of cancers these compounds are acting upon, and the substitution patterns present on rings A and B of the molecule 5 . In this study, another flavonoid from C. leivensis (Hieron) has been isolated and identified as (2R)-5,7-dihydroxyflavanone. ...
Background: Flavonoids isolated from plants have demonstrated an important role in cancer chemoprevention and chemotherapy. The genus Cromolaena has been shown to have active principles against this disease and found in species such as C. odorata, and C. laevigata in a concentration lower than 100 mg/L, however, flavonoids from C. leivensis has not been studied completely as an alternative in cancer treatment. Materials and Methods: The (2R)-5,7-dihydroxy flavanone or (R) Pinocembrin was isolated from leaves of Chromolaena leivensis (Hieron) using chromatography methods. Its structure and relative configuration were determined by NMR spectroscopy, gas chromatography coupled to mass spectrometry and X-ray diffraction. We evaluated the (R) Pinocembrin effects on cell proliferation, morphology, DNA damage, and cell cycle progression of cancer cell lines Results: The compound showed a decreasing cell proliferation rate against HT29, PC-3, A549, MDA-MB-231, and SiHa cancer cell lines with an IC50 values between 58.9 mg/L, and 30.9 mg/L, causing alterations in the stability of the cytoskeleton and G1-phase cell cycle arrest without affecting significantly the DNA integrity. Conclusion: The (R)-Pinocembrin is a potential molecule to be used in the treatment of cancer with an action on the cytoskeleton. Our study indicate that the medium polarity fraction obtained from C. leivensis is a promising fraction which could be used as in the treatment of cancer, especially as a coadjuvant.
Ethnopharmacological relevance
Chromolaena species, of the Asteraceae family, are distributed across the tropical and the temperate regions of Africa, the Americas, southern Asia, and Australia. Despite “falling out of favour” among the people because of their “weedy” nature, Chromolaena species have indisputable long medicinal history in the treatment of malaria, nasal congestion, inflammation, eye disorders, asthma, cough, flu, headache, and cold.
Aim of the review
The aim of this review is to systematically summarize the current knowledge on ethnopharmacology, phytochemistry, pharmacology, toxicology, and real-time scientific applications of the genus Chromolaena after re-classification from genus Eupatorium, as well as to proffer integrated approaches in maximizing their therapeutic values despite their “weedy” nature.
Materials and methods
First, the current species in the genus were verified by “The Plant List” (http://www.theplantlist.org) and “Royal Botanic Gardens/Kew/Missouri Botanical Garden” (http://mpns.kew.org/mpns-portal/). Second, the relevant information on each of the identified species was gathered from following databases: Google Scholar, Online Wiley library, ScienceDirect, SciFinder, Scopus, PubMed. Scientific literature was searched from inception till August 2021.
Results
More than 190 phytochemicals have been isolated and identified from 27 species of the genus, including flavonoids, alkaloids, triterpenoids, diterpenoids, sesquiterpenoids, steroids, fatty acids, and coumarins among others. Pharmacological investigations, both in vitro and in vivo, have shown that the extracts and the compounds have antimicrobial, anticancer, antioxidant, insecticidal, anti-inflammatory, and anti-diabetic activities among others.
Conclusions
Many species of genus have potential therapeutic values, and hence they are more than “wandering” weeds. In addition, there is growing interest in the real-time scientific applications of the genus in the production of pharmacological polyherbal products, and this should serve as a stimulus to strategically develop integrated control approaches for preserving these species, with a view of maximizing their therapeutic values and reducing their cost of eradication.
