Cytotoxic Compounds from Kibatalia gitingensis (Elm.) Woodson

Reyes, Mariquit M. De Los; Oyong, Glenn G.; Ng, Vincent Antonio S.; Shen, Chien‐Chang; Ragasa, Consolacion Y.

doi:10.5530/pj.2017.1.2

Cited by 4 publications

(4 citation statements)

References 19 publications

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“…This implies that HCT-116 cells are more responsive to the treatments used. Differences in treatment response between colon cancer cell lines were also observed in previous studies [44][45][46]. It was reported that variations in the expression profiles of genes associated with drug sensitivity in HCT-116 and HT-29 cells could be an important factor dictating how the cells respond to inhibitory compounds [47].…”

Section: Resultsmentioning

confidence: 61%

Cytotoxic Prenylflavanones from Philippine Stingless Bee (Tetragonula biroi Friese) Nests

Reyes¹,

Oyong²,

Ebajo³

et al. 2018

Asian J. Chem.

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INTRODUCTIONPropolis or "bee glue" is a resinous material collected by honeybees from tree buds, sap flows or other botanical exudates and is used for sealing and coating bee hives. For many centuries, aside from its use as food, beverage and food supplement, it has long been used extensively in traditional medicine because of its wide range of therapeutic values for the treatment of common cold, flu, upper respiratory tract infections, as dermatological preparations for wounds, burns, acne, herpes simplex, genitalis and neurodermatitis, as mouthwash and toothpaste to prevent caries and gingivitis and for cosmetic applications [1,2]. Propolis was shown to exhibit a broad spectrum of biological activities which include antimicrobial [3,4], antifungal [5,6], free radical scavenging [7,8], anti-HIV [9,10], anti-inflammatory [11,12] and anti-herpes [13,14]. A recent study reported that propolis, at a concentration of 0.01 % (w/v), exhibited antiproliferative and cytotoxic actions against human fibroblasts proliferation in cell culture, followed by mild cell necrosis [15]. The dichloromethane crude extract and compounds, glyasperin A (1), propolin E (2) and propolin A (3), obtained from Philippine stingless bee (Tetragonula biroi Friese) nests, were evaluated for their cytotoxic potentials. The anti-proliferative activities of crude extract and compounds 1-3 against human cancer cell lines, breast (MCF-7) and colon (HT-29 and HCT-116), and a normal cell line, human dermal fibroblast neonatal (HDFn), were evaluated using the PrestoBlue ® cell viability assay. The crude extract was most anti-proliferative against HCT-116 cells (IC50 = 1.410 µg/mL). Glyasperin A (1) exhibited the strongest effect on MCF-7 cells (2.378 µg/mL). Propolin E (2) was most cytotoxic against HCT-116 cells (2.279 µg/mL), while propolin A (3) was most inhibitory against MCF-7 cells (2.815 µg/mL). Comparing the colorectal cancer cell lines, HCT-116 was generally more susceptible under crude extract, 2, and 3 (IC50 = 1.410, 2.279, 3.013 µg/mL, respectively) than 5.320, 5.359). Comparing the activities of propolin E and propolin A against HCT-116 cells, 2 (IC50 = 2.279 µg/mL) was more cytotoxic than 3 (3.013). The crude extract was more cytotoxic than Zeocin against HCT-116 cells. To our best of knowledge, this is the first report on the anti-proliferative properties of crude extract and compounds from T. biroi.

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Section: Resultsmentioning

confidence: 61%

Cytotoxic Prenylflavanones from Philippine Stingless Bee (Tetragonula biroi Friese) Nests

Reyes¹,

Oyong²,

Ebajo³

et al. 2018

Asian J. Chem.

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“…Based on the results obtained from the MTT assay, the prepared compounds showed a dose-dependent cytotoxic activity against cancer cells. These results indicate that these compounds have the potential to be anti-cancer agents in view of their potent cytotoxicity and antitumor activity in the order of S3> S1> S4> S2 [17][18][19].…”

Section: Biological Activitymentioning

confidence: 85%

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2023

J. Med. Chem. Sci.

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Four new Triazole Schiff Bases were synthesized through the green condensation and were structurally confirmed by mass spectroscopy, IR, 1 H NMR, TGA, and DSC. The chief advantages of the reported technique were its working ease, very mild reaction conditions, short reaction time, and high yield. Quantum chemical calculations were applied to investigate the optimized geometry and electronic structure of the compounds, S1-S4. DFT/B3LYP/6-31+G (d), was performed to determine the chemical quantum descriptors (CQDs). An analysis of the CQDs showed that the S1 compound had a higher molecular stability. The findings of the computational research revealed that there was a close interaction between the theoretical and experimental data. The synthesized compounds were studied for their anticancer activity against two cell lines, MCF-7 and HepG2. The results revealed that the S3 and S4 compounds had a remarkable activity, with IC50 of 64.64 μg/mL and 23.52 μg/mL, respectively, thus, making them crucial components for anticancer medicines in future studies. Molecular docking tests were carried out on the S3 and S4 compounds with the receptors 5EKN and 3PP0. The results exposed that the compounds were effective in inhibiting the receptors with a good binding energy to confirm their anticancer activity.

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“…At the present time, there are a number of pieces of evidence that demonstrated anti-cancer properties of the pentacyclic triterpenoids of oleanane-, ursane, lupane, and friedelane types (including oleanolic, ursolic, betulinic, 18α-glycyrrhetinic, asiatic acids, celastrol, lupeol, among others) [231,302]. These compounds suppress tumor growth, reduce survival, and induce apoptosis of different types of cancer cells, including skin, breast, colon, prostate tumor cells, and others [290,303,304]. However, treatment with pentacyclic triterpenoids at effective anti-cancer concentrations had a toxic effect on normal cells in some cases [304].…”

Section: Effects On Age-related Diseasesmentioning

confidence: 99%

“…These compounds suppress tumor growth, reduce survival, and induce apoptosis of different types of cancer cells, including skin, breast, colon, prostate tumor cells, and others [290,303,304]. However, treatment with pentacyclic triterpenoids at effective anti-cancer concentrations had a toxic effect on normal cells in some cases [304]. A promising anti-cancer potential has triterpenoids extracted from formopsis, poria, and Reishi fungi.…”

Section: Effects On Age-related Diseasesmentioning

confidence: 99%

Terpenoids as Potential Geroprotectors

et al. 2020

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Terpenes and terpenoids are the largest groups of plant secondary metabolites. However, unlike polyphenols, they are rarely associated with geroprotective properties. Here we evaluated the conformity of the biological effects of terpenoids with the criteria of geroprotectors, including primary criteria (lifespan-extending effects in model organisms, improvement of aging biomarkers, low toxicity, minimal adverse effects, improvement of the quality of life) and secondary criteria (evolutionarily conserved mechanisms of action, reproducibility of the effects on different models, prevention of age-associated diseases, increasing of stress-resistance). The number of substances that demonstrate the greatest compliance with both primary and secondary criteria of geroprotectors were found among different classes of terpenoids. Thus, terpenoids are an underestimated source of potential geroprotectors that can effectively influence the mechanisms of aging and age-related diseases.

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Cytotoxic Compounds from Kibatalia gitingensis (Elm.) Woodson

Cited by 4 publications

References 19 publications

Cytotoxic Prenylflavanones from Philippine Stingless Bee (Tetragonula biroi Friese) Nests

Cytotoxic Prenylflavanones from Philippine Stingless Bee (Tetragonula biroi Friese) Nests

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Terpenoids as Potential Geroprotectors

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