Derivatives of Gallic Acid Induce Apoptosis in Tumoral Cell Lines and Inhibit Lymphocyte Proliferation

1998 ◽  
Vol 350 (1) ◽  
pp. 49-54 ◽  
Author(s):  
Antonio Serrano ◽  
Carmen Palacios ◽  
Garbiñe Roy ◽  
Constantino Cespón ◽  
Marı́a L. Villar ◽  
...  
Keyword(s):  
Gallic Acid ◽  
Cell Lines ◽  
Lymphocyte Proliferation ◽  
Tumoral Cell ◽  
Derivatives Of

Synthesis and Cytotoxicity Assessment of Novel 7-O- and 14-O-Derivatives of Glaucocalyxin A

2020 ◽  
Vol 20 (10) ◽  
pp. 1241-1249
Author(s):  
Hong-Chuan Liu ◽  
Li-Ming Qiao ◽  
Wei Zheng ◽  
Zhao-Bao Xiang ◽  
Hai-Sheng Chen ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Folk Medicine ◽  
A549 Cells ◽  
Cancer Cell Lines ◽  
Human Cancer Cell Lines ◽  
Derivatives Of

Background: Rabdosia japonica has been historically used in China as a popular folk medicine for the treatment of cancer, hepatitis, and gastricism. Glaucocalyxin A (GLA), an ent-kaurene diterpene isolated from Rabdosia japonica, is one of the main active ingredients showing potent inhibitory effects against several types of tumor cells. To the best of our knowledge, studies regarding the structural modification and Structure- Activity Relations (SAR) of this compound have not yet been reported. Objective: The aim of this study was to discover more potent derivatives of GLA and investigate their SAR and cytotoxicity mechanisms. Methods: Novel 7-O- and 14-O-derivatives of GLA were synthesized by condensation of acids or acyl chloride. The anti-tumor activities of these derivatives against various human cancer cell lines were evaluated in vitro by MTT assays. Apoptosis assays of compound 17 (7,14-diacylation product) were performed on A549 and HL-60 cells by flow cytometry and TUNNEL. The acute toxicity of this compound was tested on mice, at the dose of 300mg per kg body weight. Results: Seventeen novel 7-O- and 14-O-derivatives of GLA (1-17) were synthesized. These compounds showed potent cytotoxicity against the tested cancer cell lines, and almost all of them were found to be more cytotoxic than GLA and oridonin. Of the synthesized derivatives, compound 17 presented the greatest cytotoxicity, with IC50 values of 0.26μM and 1.10μM in HL-60 and CCRF-CEM cells, respectively. Furthermore, this compound induced weak apoptosis of A549 cells but showed great potential in stimulating the apoptosis of HL- 60 cells. Acute toxicity assays indicated that compound 17 is relatively safer. Conclusion: The results reported herein indicate that the synthesized GLA derivatives exhibited greater cytotoxicity against leukemia cells than against other types of tumors. In particular, 7,14-diacylation product of GLA was found to be an effective anti-tumor agent. However, the cytotoxicity mechanism of this product in A549 cells is expected to be different than that in other tumor cell lines. Further research is needed to confirm this hypothesis.

scholarly journals Antioxidant Network Based on Sulfonated Polyhydroxyalkanoate and Tannic Acid Derivative

2021 ◽  
Vol 8 (1) ◽  
pp. 9
Author(s):  
Laura Brelle ◽  
Estelle Renard ◽  
Valerie Langlois
Keyword(s):  
Gallic Acid ◽  
Tannic Acid ◽  
Water Soluble ◽  
Gel Formation ◽  
Ene Reaction ◽  
Inorganic Cations ◽  
Medium Chain Length ◽  
Physically Crosslinked ◽  
The Stability ◽  
Derivatives Of

A novel generation of gels based on medium chain length poly(3-hydroxyalkanoate)s, mcl-PHAs, were developed by using ionic interactions. First, water soluble mcl-PHAs containing sulfonate groups were obtained by thiol-ene reaction in the presence of sodium-3-mercapto-1-ethanesulfonate. Anionic PHAs were physically crosslinked by divalent inorganic cations Ca2+, Ba2+, Mg2+ or by ammonium derivatives of gallic acid GA-N(CH3)3+ or tannic acid TA-N(CH3)3+. The ammonium derivatives were designed through the chemical modification of gallic acid GA or tannic acid TA with glycidyl trimethyl ammonium chloride (GTMA). The results clearly demonstrated that the formation of the networks depends on the nature of the cations. A low viscoelastic network having an elastic around 40 Pa is formed in the presence of Ca2+. Although the gel formation is not possible in the presence of GA-N(CH3)3+, the mechanical properties increased in the presence of TA-N(CH3)3+ with an elastic modulus G’ around 4200 Pa. The PHOSO3−/TA-N(CH3)3+ gels having antioxidant activity, due to the presence of tannic acid, remained stable for at least 5 months. Thus, the stability of these novel networks based on PHA encourage their use in the development of active biomaterials.

scholarly journals Fucoxanthin Holds Potential to Become a Drug Adjuvant in Breast Cancer Treatment: Evidence from 2D and 3D Cell Cultures

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4288
Author(s):  
Fernanda Malhão ◽  
Ana Catarina Macedo ◽  
Carla Costa ◽  
Eduardo Rocha ◽  
Alice Abreu Ramos
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
3D Models ◽  
Anticancer Activities ◽  
Cytotoxic Effects ◽  
3D Cultures ◽  
3D Cell Cultures ◽  
Tumoral Cell ◽  
Microscopy Techniques ◽  
2D And 3D

Fucoxanthin (Fx) is a carotenoid derived from marine organisms that exhibits anticancer activities. However, its role as a potential drug adjuvant in breast cancer (BC) treatment is still poorly explored. Firstly, this study investigated the cytotoxic effects of Fx alone and combined with doxorubicin (Dox) and cisplatin (Cis) on a panel of 2D-cultured BC cell lines (MCF7, SKBR3 and MDA-MB-231) and one non-tumoral cell line (MCF12A). Fucoxanthin induced cytotoxicity against all the cell lines and potentiated Dox cytotoxic effects towards the SKBR3 and MDA-MB-231 cells. The combination triggering the highest cytotoxicity (Fx 10 µM + Dox 1 µM in MDA-MB-231) additionally showed significant induction of cell death and genotoxic effects, relative to control. In sequence, the same combination was tested on 3D cultures using a multi-endpoint approach involving bioactivity assays and microscopy techniques. Similar to 2D cultures, the combination of Fx and Dox showed higher cytotoxic effects on 3D cultures compared to the isolated compounds. Furthermore, this combination increased the number of apoptotic cells, decreased cell proliferation, and caused structural and ultrastructural damages on the 3D models. Overall, our findings suggest Fx has potential to become an adjuvant for Dox chemotherapy regimens in BC treatment.

scholarly journals Biguanide-Based Synthesis of 1,3,5-Triazine Derivatives with Anticancer Activity and 1,3,5-Triazine Incorporated Calcium Citrate Nanoparticles

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1028
Author(s):  
Monnaya Chalermnon ◽  
Sarocha Cherdchom ◽  
Amornpun Sereemaspun ◽  
Rojrit Rojanathanes ◽  
Tanatorn Khotavivattana
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agent ◽  
Drug Loading ◽  
Calcium Citrate ◽  
Colorectal Cancer Cell Lines ◽  
Triazine Derivatives ◽  
Further Development ◽  
Derivatives Of ◽  
Potential Use

Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.

The rescue of oral development of defective-micronucleate conjugants of Paramecium tetraurelia by normal gametic nuclei

1988 ◽  
Vol 90 (2) ◽  
pp. 287-293
Author(s):  
M. F. CHAU ◽  
STEPHEN F. NG
Keyword(s):  
Sexual Reproduction ◽  
Cell Lines ◽  
Early Stage ◽  
Sexual Cycle ◽  
Paramecium Tetraurelia ◽  
Laser Microbeam ◽  
Nuclear Reorganization ◽  
Oral Development ◽  
Derivatives Of

The present study further analyses the importance of postmeiotic divisional derivatives of the micronucleus in the development of the oral apparatus of Paramecium during sexual reproduction. Cell lines possessing defective micronuclei generated by laser microbeam irradiation of the micronucleus were employed. They exhibited anomalies in nuclear reorganization and stomatogenesis in the sexual cycle. During autogamy, in some cells the micronuclear cycle terminated shortly after meiosis, resulting in the loss of all postmeiotic micronuclear derivatives. Stomatogenesis became arrested at an early stage of assembly of the oral membranelles, but the old oral apparatus was resorbed as usual, leading to the production of astomatous cells at the end of the sexual cycle. Conjugation of these cell lines with normal micronucleates rescued both nucleogenesis and stomatogenesis in the defective micronucleate conjugant, primarily as a result of transfer of the male gametic nucleus from the normal conjugant to the defective-micronucleate mate. These observations demonstrate the stomatogenic significance, in particular in the initiation of oral membranelle assembly, of the gametic nuclei during sexual reproduction. The present study also suggests the possibility of micronuclear activities in the early part of the sexual cycle affecting postzygotic nucleogenesis.

scholarly journals Comparative cytotoxic activity between kaempferol and gallic acid against various cancer cell lines

Data in Brief ◽  
2018 ◽  
Vol 21 ◽  
pp. 1033-1036 ◽  
Author(s):  
Hong Ngoc Thuy Pham ◽  
Jennette A. Sakoff ◽  
Quan V. Vuong ◽  
Michael C. Bowyer ◽  
Christopher J. Scarlett
Keyword(s):  
Cytotoxic Activity ◽  
Gallic Acid ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines

scholarly journals Quantification of rutin and quercetin by HPTLC/HPLC and in vitro immunomodulatory and anticancer activities of Capparis moonii fruits extracts

2017 ◽  
Vol 7 (1) ◽  
pp. 153
Author(s):  
Gaurav Mahesh Doshi ◽  
Manjushree Kundalik Pawar ◽  
Kajal Haribhai Chavda
Keyword(s):  
Gallic Acid ◽  
Cell Lines ◽  
Antibody Titre ◽  
High Performance ◽  
Assay Method ◽  
Total Phenolic ◽  
Flavonoid Content ◽  
Phenolic And Flavonoid ◽  
Rutin And Quercetin

Background: The current research was undertaken on dried fruits of Capparis moonii to screen its potential for immunomodulatory and cancer indications with identification of phytoconstituents by chromatographic techniques.Methods: Methanolic (MECN), hydro-methanolic (HMECN) and aqueous extracts (AQCN) of Capparis moonii were subjected to high performance thin layer chromatography (HPTLC) and high-performance liquid chromatography (HPLC) after studying the total phenolic and flavonoid content by using rutin and gallic acid as standards respectively as well as undertaking powder characteristics and preliminary phytochemical screening. Immunomodulatory activities covered were hemagglutination antibody titre and delayed-type hypersensitivity reaction with the aid of sheep red blood cells (0.5×109) as antigens.  The extracts were studied for antioxidant potential. Anticancer prospects were focusing on in vitro cell lines screening (MCF 7 and HCT 15) by Sulforhodamine B assay method and potato disc assay.Results: The total phenolic and flavonoid content of MECM, HMECM and AQCM fruits extracts were found to be 0.20, 0.11 and 0.47 mg of gallic acid/g and 78.3, 18.8 and 64.4 mg of rutin/g respectively. Rutin and quercetin were confirmed by HPTLC and HPLC showing well resolved peaks. IC50 values in antioxidant studies were found to be significant with all the extracts. Significant immunomodulatory effect was noticed at 200mg/kg in both models (high antibody titre levels and decrease paw volume after 48 h). Unsatisfactory results were observed with selected cell lines and disc assay.Conclusions: Thus, selected fruits may probably have immunomodulatory potential due to presence of flavonols (rutin and quercetin).

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