ABSTRACT
Artocarpus heterophyllus Lam. (Moraceae) has been traditionally used in treating various diseases such as diabetes, diarrhea, malarial fever, inflammation, wound healing and other diseases. Since various bioactive compounds have been found in this plant, this review focuses on the phytochemical and pharmacological properties of a potent bioactive compound artocarpin. Despite its various functions, a mechanistic review on this compound has not been reviewed specifically. Here, pharmacological studies in vitro and in vivo on artocarpin are discussed thoroughly stressing on anticancer, antimicrobial, anti-tyrosinase, antioxidant and antiinflammatory aspects of artocarpin. This review would be beneficial for future study to show the competency of natural products for theirtherapeutic characteristics.
ABSTRACT
Artocarpus heterophyllus Lam. (Moraceae) has been traditionally used in treating various diseases such as diabetes, diarrhea, malarial fever, inflammation, wound healing and other diseases. Since various bioactive compounds have been found in this plant, this review focuses on the phytochemical and pharmacological properties of a potent bioactive compound artocarpin. Despite its various functions, a mechanistic review on this compound has not been reviewed specifically. Here, pharmacological studies in vitro and in vivo on artocarpin are discussed thoroughly stressing on anticancer, antimicrobial, anti-tyrosinase, antioxidant and antiinflammatory aspects of artocarpin. This review would be beneficial for future study to show the competency of natural products for theirtherapeutic characteristics.
ABSTRACT
Artocarpus heterophyllus has been used as traditional medicine. This plant is one of the sources of flavonoid. Flavonoid compounds possessed a wide range of biological properties including anticancer. This study was performed to investigate the cytotoxic effect of flavonoids from A. heterophyllus on H460 and MCF-7 cell lines. The interaction of flavonoids and cisplatin against tested cancer cells was also evaluated. MTT assay was used to determine the cytotoxic effect of flavonoid. Isobologram analysis was selected to evaluate the synergistic effect between flavonoid and cisplatin, their interaction was then confirmed using AO/PI staining method. Amongst of flavonoid compounds, artocarpin exhibited strong cytotoxic effect on both MCF-7 and H460 cell lines with IC₅₀ values of 12.53 µg/mL (28.73 µM) and 9.77 µg/mL (22.40 µM), respectively. This compound enhanced anticancer activity of cisplatin against H460 and MCF-7. The combination produced a synergistic effect on H460 and MCF-7 cell lines with a combination index (CI) values of 0.2 and 0.18, respectively. The AO/PI stained demonstrated that the combination of artocarpin and cisplatin caused morphological changes that indicated apoptosis. Moreover, artocarpanone also significantly increased cytotoxic effect of cisplatin compared to its single concentration with CI below than 1. This result suggested the potency of flavonoid named artocarpin to enhance the anticancer activity of cisplatin on H460 and MCF-7 cell lines.
Subject(s)
Apoptosis , Artocarpus , Cell Line , Cisplatin , Flavonoids , MCF-7 Cells , Medicine, Traditional , Methods , PlantsABSTRACT
Objective: One appealing strategy to overcome and prevent resistant problem is the use of combined two or more antibacterial substances. Lawsone methyl ether (LME) is the naphthoquinone found in the leaves of Impatiens balsamina. The objective of this study is to determine the interaction of LME with some antibiotics (ampicillin, tetracycline, norfloxacin, and clotrimazole) and a natural compound, artocarpin against methicillin-resistant Staphylococcus aureus (MRSA), Candida albicans, and Trychophyton rubrum. Methods: A broth microdilution method was used to determine the minimum inhibition concentration (MIC). Synergistic effects were evaluated at their own MIC using the checkerboard method and time-kill assay. Results: LME showed moderate antibacterial activity against MRSA with MIC value of 15.6 µg/mL, and exhibited strong antifungal activities against T. rubrum and C. albicans with MIC values of 7.8 and 3.9 µg/mL, respectively. The interaction of LME with the natural compound artocarpin against MRSA produced a synergy with fractional inhibitory concentration index (FICI) value of 0.31, while the combination of LME and clotrimazole exhibited synergy against C. albicans and T. rubrum with FICI values of 0.38 and 0.24, respectively. The time-kill assays confirmed that the compounds in combination enhanced their antimicrobial activities against the resistant microorganisms with different degrees. Conclusion: LME in combination with clotrimazole exhibited synergy effect against C. albicans and T. rubrum. In combination with artocarpin, it showed synergy effect against MRSA.
ABSTRACT
A reversed-phase high-performance liquid chromatographic method is described for the simultaneous determination of three antibacterial flavonoids, artocarpanone, artocarpin, and cycloartocarpin in ethyl acetate extracts from Artocarpus heterophyllus heartwoods. Separation was achieved using a TSK-gel ODS-80Tm column (5 µm, 4.6 × 150 mm) at 25℃ with a gradient elution system of methanol and water as follows: 0-8 min, 60:40; 8-27 min, 80:20; 27-35 min, 60:40, v/v, at a flow rate of 1 mL/min, and a quantitative UV detection at 285 nm. The method was validated by measuring the key parameters, including specificity, linearity, sensitivity, accuracy, repeatability and reproducibility. A high degree of specificity and sensitivity was achieved. The calibration curves for all three flavonoids showed good linearity with a coefficient of determinations (R²) of ≥ 0.9995. The recoveries of the method were from 98-104%, with good reproducibility and repeatability (RSD values of less than 2%) were also achieved. Ethyl acetate was the best solvent for extraction of these three flavonoids using the heat reflux conditions for 1 h. This optimized sample preparation and HPLC method can be practically used for a routine standardization process of the extracts from the A. heterophyllus heartwoods.