scholarly journals An Update on the Anticancer Activity of Xanthone Derivatives: A Review

2021 ◽  
Vol 14 (11) ◽  
pp. 1144
Author(s):  
Yehezkiel Steven Kurniawan ◽  
Krisfian Tata Aneka Priyangga ◽  
Jumina ◽  
Harno Dwi Pranowo ◽  
Eti Nurwening Sholikhah ◽  
...  

The annual number of cancer deaths continues increasing every day; thus, it is urgent to search for and find active, selective, and efficient anticancer drugs as soon as possible. Among the available anticancer drugs, almost all of them contain heterocyclic moiety in their chemical structure. Xanthone is a heterocyclic compound with a dibenzo-γ-pyrone framework and well-known to have “privileged structures” for anticancer activities against several cancer cell lines. The wide anticancer activity of xanthones is produced by caspase activation, RNA binding, DNA cross-linking, as well as P-gp, kinase, aromatase, and topoisomerase inhibition. This anticancer activity depends on the type, number, and position of the attached functional groups in the xanthone skeleton. This review discusses the recent advances in the anticancer activity of xanthone derivatives, both from natural products isolation and synthesis methods, as the anticancer agent through in vitro, in vivo, and clinical assays.

2020 ◽  
Vol 9 (6) ◽  
pp. 175-181
Author(s):  
Chandekar Deepali Boudhadas ◽  
Pawade Uday Venkatrao ◽  
Nikam Ashwin Vithalrao ◽  
Anjankar Meghsham Pramodrao

Cancer is one amongst the dreadful diseases of present century. The incidence of cancer is increasing worldwide. Every year about 8,00,000 new cancer patients get registered with the national cancer registry program in India. Ayurveda an ancient Indian medicine science describes many useful herbal drugs for such types of advanced diseases. Upavisha the plant poisons of low potency are mentioned in Agadtantra. Arka (Calotropis procera/ Calotropis gigantea) is one among these Upavisha is emerging as an effective anticancer drug. It shows various pharmacological activities such as Anticancer, Antimicrobial, Antiimplantation etc. Different parts of Arka are used to treat cancer. In current scenario number of synthetic anticancer drugs are used to treat cancer. These synthetic anticancer drugs are expensive and shows harmful adverse effects. Upavisha like Arka which is natural derivative may be cost effective & less harmful as Anticancer drug. Anticancer activity of Calotropis procera/Calotropis gigantea is reported in scientific journals. This review summarizes various In Vitro and In Vivo studies of anticancer activity of Upavisha Arka.


2020 ◽  
Vol 27 (6) ◽  
pp. 983-996 ◽  
Author(s):  
Md. Asaduzzaman Khan ◽  
Mousumi Tania

Background: Cordycepin is a nucleotide analogue from Cordyceps mushrooms, which occupies a notable place in traditional medicine. Objective: In this review article, we have discussed the recent findings on the molecular aspects of cordycepin interactions with its recognized cellular targets, and possible mechanisms of its anticancer activity. Methods: We have explored databases like pubmed, google scholar, scopus and web of science for the update information on cordycepin and mechanisms of its anticancer activity, and reviewed in this study. Results: Cordycepin has been widely recognized for its therapeutic potential against many types of cancers by various mechanisms. More specifically, cordycepin can induce apoptosis, resist cell cycle and cause DNA damage in cancer cells, and thus kill or control cancer cell growth. Also cordycepin can induce autophagy and modulate immune system. Furthermore, cordycepin also inhibits tumor metastasis. Although many success stories of cordycepin in anticancer research in vitro and in animal model, and there is no successful clinical trial yet. Conclusion: Ongoing research studies have reported highly potential anticancer activities of cordycepin with numerous molecular mechanisms. The in vitro and in vivo success of cordycepin in anticancer research might influence the clinical trials of cordycepin, and this molecule might be used for development of future cancer drug.


2020 ◽  
Vol 10 (4) ◽  
pp. 395-399
Author(s):  
Ajay M. Chowdari ◽  
D. Giles

Background: Ziziphus jujuba mill was commonly used for its anti-inflammatory activity in traditional system of medicine. Objective: The purpose of this study was to examine the isolates of methanolic extract from the fruits of Ziziphus jujuba Mill for its antiulcer, anti-inflammatory, and anticancer activity. Methods: Methanolic extracts of Ziziphus jujuba Mill were subjected to chromatography and eluted using ethyl acetate: methanol mixture and investigated for its structural features using IR, 1H NMR, 13C NMR and mass spectral data. The isolated compound was evaluated for its in vitro COX-2 inhibition studies, cytotoxicity studies, in vivo anti-inflammatory, antiulcer and anticancer activity. Results: The spectral data revealed that the backbone of the isolate was 3-O-α-L-rhamnopyranosyl- (1→6)-β-D-glucopyranosyl jujubogenin-20-O-(2,3,4-O-triacetyl)-α-L-rhamnopyranoside. The isolated compound showed a significant reduction in inflammation and edema. Moderate anticancer activity was also observed for the isolate. Conclusion: It was concluded that the isolated saponin possesses moderate antiulcer, antiinflammatory, and anticancer activity which could help in the identification of leads for the treatment of cancer-related inflammation.


2013 ◽  
Vol 2013 ◽  
pp. 1-13 ◽  
Author(s):  
El-Sayed S. Abdel-Hameed ◽  
Salih A. Bazaid ◽  
Mahmood S. Salman

Ward Taifi (Taif rose) is considered one of the most important economic products of Taif, Saudi Arabia. In this study both fresh and dry Taif rose were biologically and phytochemically investigated. The 80% methanol extracts andn-butanol fractions of dry and fresh Taif rose had high radical scavenging activity toward artificial 1,1-diphenyl picrylhydrazyl (DPPH)•radical with SC50values range 5.86−12.24 µg/ml whereas the aqueous fractions showed weak activity. All samples hadin vitroanticancer activity toward HepG2 with IC50< 20 µg/ml which fall within the criteria of the American Cancer Institute. High positive correlation appeared between the antioxidant activity and total phenolics whereas there is no correlation between total phenolics and anticancer activity. The LC-ESI(− ve)-MS analysis of all extracts indicate the presence of phenolic compounds belonging to hydrolysable tannins and flavonol glycosides. In conclusion, the presence of this is considered to be the first phytochemical report that identifies the major compounds in dry and fresh roses using HPLC-ESI-MS. The methanol extracts and itsn-butanol and aqueous fractions for both fresh and dry Taif rose could be used as preventive and therapeutic effective natural agents for diseases in which free radicals involved after morein vitroandin vivostudies.


2018 ◽  
Vol 25 (4) ◽  
pp. 506-524 ◽  
Author(s):  
Maricela Viola-Rhenals ◽  
Kush R. Patel ◽  
Laura Jaimes-Santamaria ◽  
Guojun Wu ◽  
Jinbao Liu ◽  
...  

Background: Considerable evidence demonstrates the importance of dithiocarbamates especially disulfiram as anticancer drugs. However there are no systematic reviews outlining how their metal-binding ability is related to their anticancer activity. This review aims to summarize chemical features and metal-binding activity of disulfiram and its metabolite DEDTC, and discuss different mechanisms of action of disulfiram and their contributions to the drug's anticancer activity. Methods: We undertook a disulfiram-related search on bibliographic databases of peerreviewed research literature, including many historic papers and in vitro, in vivo, preclinical and clinical studies. The selected papers were carefully reviewed and summarized. Results: More than five hundreds of papers were obtained in the initial search and one hundred eighteen (118) papers were included in the review, most of which deal with chemical and biological aspects of Disulfiram and the relationship of its chemical and biological properties. Eighty one (81) papers outline biological aspects of dithiocarbamates, and fifty seven (57) papers report biological activity of Disulfiram as an inhibitor of proteasomes or inhibitor of aldehyde dehydrogenase enzymes, interaction with other anticancer drugs, or mechanism of action related to reactive oxygen species. Other papers reviewed focus on chemical aspects of dithiocarbamates. Conclusion: This review confirms the importance of chemical features of compounds such as Disulfiram to their biological activities, and supports repurposing DSF as a potential anticancer agent.


Toxics ◽  
2021 ◽  
Vol 9 (2) ◽  
pp. 24
Author(s):  
Fernanda Malhão ◽  
Alice Abreu Ramos ◽  
Ana Catarina Macedo ◽  
Eduardo Rocha

Seaweed bioactive compounds have shown anticancer activities in in vitro and in vivo studies. However, tests remain limited, with conflicting results, and effects in combination with anticancer drugs are even scarcer. Here, the cytotoxic effects of five seaweed compounds (astaxanthin, fucoidan, fucosterol, laminarin, and phloroglucinol) were tested alone and in combination with anticancer drugs (cisplatin—Cis; and doxorubicin—Dox), in breast cell lines (three breast cancer (BC) subtypes and one non-tumoral). The combinations revealed situations where seaweed compounds presented potentiation or inhibition of the drugs’ cytotoxicity, without a specific pattern, varying according to the cell line, concentration used for the combination, and drug. Fucosterol was the most promising compound, since: (i) it alone had the highest cytotoxicity at low concentrations against the BC lines without affecting the non-tumoral line; and (ii) in combination (at non-cytotoxic concentration), it potentiated Dox cytotoxicity in the triple-negative BC cell line. Using a comparative approach, monolayer versus 3D cultures, further investigation assessed effects on cell viability and proliferation, morphology, and immunocytochemistry targets. The cytotoxic and antiproliferative effects in monolayer were not observed in 3D, corroborating that cells in 3D culture are more resistant to treatments, and reinforcing the use of more complex models for drug screening and a multi-approach that should include histological and ICC analysis.


2015 ◽  
Vol 44 (25) ◽  
pp. 11408-11419 ◽  
Author(s):  
Jian-Hua Wei ◽  
Zhen-Feng Chen ◽  
Jiao-Lan Qin ◽  
Yan-Cheng Liu ◽  
Zhu-Quan Li ◽  
...  

The complexes exhibited considerable in vitro and in vivo anticancer activity, and higher safety than ciplatin.


2021 ◽  
Vol 12 ◽  
Author(s):  
Zhaowu Ma ◽  
Clariis Yi-Ning Woon ◽  
Chen-Guang Liu ◽  
Jun-Ting Cheng ◽  
Mingliang You ◽  
...  

Cancer has become a global health problem, accounting for one out of six deaths. Despite the recent advances in cancer therapy, there is still an ever-growing need for readily accessible new therapies. The process of drug discovery and development is arduous and takes many years, and while it is ongoing, the time for the current lead compounds to reach clinical trial phase is very long. Drug repurposing has recently gained significant attention as it expedites the process of discovering new entities for anticancer therapy. One such potential candidate is the antimalarial drug, artemisinin that has shown anticancer activities in vitro and in vivo. In this review, major molecular and cellular mechanisms underlying the anticancer effect of artemisinin and its derivatives are summarised. Furthermore, major mechanisms of action and some key signaling pathways of this group of compounds have been reviewed to explore potential targets that contribute to the proliferation and metastasis of tumor cells. Despite its established profile in malaria treatment, pharmacokinetic properties, anticancer potency, and current formulations that hinder the clinical translation of artemisinin as an anticancer agent, have been discussed. Finally, potential solutions or new strategies are identified to overcome the bottlenecks in repurposing artemisinin-type compounds as anticancer drugs.


Cancers ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 360 ◽  
Author(s):  
Vivek Kaushik ◽  
Juan Yakisich ◽  
Anil Kumar ◽  
Neelam Azad ◽  
Anand Iyer

Ion homeostasis is extremely important for the survival of both normal as well as neoplastic cells. The altered ion homeostasis found in cancer cells prompted the investigation of several ionophores as potential anticancer agents. Few ionophores, such as Salinomycin, Nigericin and Obatoclax, have demonstrated potent anticancer activities against cancer stem-like cells that are considered highly resistant to chemotherapy and responsible for tumor relapse. The preclinical success of these compounds in in vitro and in vivo models have not been translated into clinical trials. At present, phase I/II clinical trials demonstrated limited benefit of Obatoclax alone or in combination with other anticancer drugs. However, future development in targeted drug delivery may be useful to improve the efficacy of these compounds. Alternatively, these compounds may be used as leading molecules for the development of less toxic derivatives.


Author(s):  
R Khalil ◽  
Q Ali ◽  
MM Hafeez ◽  
A Malik

Due to the versatile application of plants the utilization of plants and their inferred substances builds up day by day for the revelation of new curative agents. Conocarpus erectus has placed in the family Combretaceae, in one of the two species of Conocarpus genus and ordinarily exists in tropical and subtropical regions of the world. In some countries it is used as folk medicine for fever, anemia, diabetes, catarrh, diarrhea and conjunctivitis. The current study was carried out to investigate the antibacterial and anticancer properties of the plant. The four defatted methanol extracts of C. erectus different parts (leaves, stems, fruits and bark) showed high antibacterial and anticancer activity even with small quantity of dose. Antimicrobial assay was used to check out the antibacterial activity against 6 bacterial strains Escherichia coli, Staphylococcus Aureus and Klebstella Pneumoniae.  The results show that gram positive bacteria show more sensitivity and zone of inhibition as compared to gram negative bacteria. For anticancer activity, MTT assay was performed on HepG2 cells for this purpose. Plant extorts show anticancer activity with a minute quantity. For phytochemical screening defatted methanol extract of Conocarpus erectus was subjected to the silica gel glass column go behind by (RP-HPLC–UV–ESI-MS). It contains phenol such as tannin and flavinoid as major component. Plant contain Ellagic acid; di-hexahydroxy diphenyl, Vascalgin isomer as foremost tannin component. Gallic Acid, Kaempferol on the base of mass spectra and time of retention. The extract of Conocarpus erectus (leaves, shoot, bark & fruit) parts shows high antibacterial, antioxidant and hepta-protective activities due to phenolic content. Tannin has high antibacterial activity than other compound. C.erectus is notable for its folkloristic curative potential. More in vivo and in vitro phytochemical studies are needed to use the plant for prevention and treatment of many diseases.


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