Tocotrienols and Cancer: From the State of the Art to Promising Novel Patents

2019 ◽  
Vol 14 (1) ◽  
pp. 5-18 ◽  
Author(s):  
Fabrizio Fontana ◽  
Michela Raimondi ◽  
Monica Marzagalli ◽  
Roberta M. Moretti ◽  
Marina Montagnani Marelli ◽  
...  
Keyword(s):  
Cancer Prevention ◽  
State Of The Art ◽  
Synergistic Effects ◽  
The State ◽  
Therapeutic Interventions ◽  
Multiple Tumor ◽  
Anti Cancer ◽  
Important Health

Background: Tocotrienols (TTs) are vitamin E derivatives naturally occurring in several plants and vegetable oils. Like Tocopherols (TPs), they comprise four isoforms, α, β, γ and δ, but unlike TPs, they present an unsaturated isoprenoid chain. Recent studies indicate that TTs provide important health benefits, including neuroprotective, anti-inflammatory, anti-oxidant, cholesterol lowering and immunomodulatory effects. Moreover, they have been found to possess unique anti-cancer properties.Objective:The purpose of this review is to present an overview of the state of the art of TTs role in cancer prevention and treatment, as well as to describe recent patents proposing new methods for TTs isolation, chemical modification and use in cancer prevention and/or therapy.Methods:Recent literature and patents focusing on TTs anti-cancer applications have been identified and reviewed, with special regard to their scientific impact and novelty.Results:TTs have demonstrated significant anti-cancer activity in multiple tumor types, both in vitro and in vivo. Furthermore, they have shown synergistic effects when given in combination with standard anti-cancer agents or other anti-tumor natural compounds. Finally, new purification processes and transgenic sources have been designed in order to improve TTs production, and novel TTs formulations and synthetic derivatives have been developed to enhance their solubility and bioavailability.Conclusion:The promising anti-cancer effects shown by TTs in several preclinical studies may open new opportunities for therapeutic interventions in different tumors. Thus, clinical trials aimed at confirming TTs chemopreventive and tumor-suppressing activity, particularly in combination with standard therapies, are urgently needed.

Recent Patents on Anti-Cancer Potential of Helenalin

2020 ◽  
Vol 15 (2) ◽  
pp. 132-142
Author(s):  
Priyanka Kriplani ◽  
Kumar Guarve
Keyword(s):  
Synergistic Effects ◽  
Therapeutic Interventions ◽  
Active Constituent ◽  
Scientific Impact ◽  
Isolation Techniques ◽  
Anti Cancer ◽  
Prevention Of Cancer ◽  
Synthetic Derivatives

Background: Arnica montana, containing helenalin as its principal active constituent, is the most widely used plant to treat various ailments. Recent studies indicate that Arnica and helenalin provide significant health benefits, including anti-inflammatory, neuroprotective, antioxidant, cholesterol-lowering, immunomodulatory, and most important, anti-cancer properties. Objective: The objective of the present study is to overview the recent patents of Arnica and its principal constituent helenalin, including new methods of isolation, and their use in the prevention of cancer and other ailments. Methods: Current prose and patents emphasizing the anti-cancer potential of helenalin and Arnica, incorporated as anti-inflammary agents in anti-cancer preparations, have been identified and reviewed with particular emphasis on their scientific impact and novelty. Results: Helenalin has shown its anti-cancer potential to treat multiple types of tumors, both in vitro and in vivo. It has also portrayed synergistic effects when given in combination with other anti- cancer drugs or natural compounds. New purification/isolation techniques are also developing with novel helenalin formulations and its synthetic derivatives have been developed to increase its solubility and bioavailability. Conclusion: The promising anti-cancer potential of helenalin in various preclinical studies may open new avenues for therapeutic interventions in different tumors. Thus clinical trials validating its tumor suppressing and chemopreventive activities, particularly in conjunction with standard therapies, are immediately required.

scholarly journals Trypanosomatid-Caused Conditions: State of the Art of Therapeutics and Potential Applications of Lipid-Based Nanocarriers

2020 ◽  
Vol 8 ◽  
Author(s):  
Giuliana Muraca ◽  
Ignacio Rivero Berti ◽  
María L. Sbaraglini ◽  
Wagner J. Fávaro ◽  
Nelson Durán ◽  
...  
Keyword(s):  
Chagas Disease ◽  
State Of The Art ◽  
Therapeutic Interventions ◽  
Safety Issues ◽  
Routes Of Administration ◽  
Treatment Regimens ◽  
Lipid Nanocarriers ◽  
Approved Drugs

Trypanosomatid-caused conditions (African trypanosomiasis, Chagas disease, and leishmaniasis) are neglected tropical infectious diseases that mainly affect socioeconomically vulnerable populations. The available therapeutics display substantial limitations, among them limited efficacy, safety issues, drug resistance, and, in some cases, inconvenient routes of administration, which made the scenarios with insufficient health infrastructure settings inconvenient. Pharmaceutical nanocarriers may provide solutions to some of these obstacles, improving the efficacy–safety balance and tolerability to therapeutic interventions. Here, we overview the state of the art of therapeutics for trypanosomatid-caused diseases (including approved drugs and drugs undergoing clinical trials) and the literature on nanolipid pharmaceutical carriers encapsulating approved and non-approved drugs for these diseases. Numerous studies have focused on the obtention and preclinical assessment of lipid nanocarriers, particularly those addressing the two currently most challenging trypanosomatid-caused diseases, Chagas disease, and leishmaniasis. In general, in vitro and in vivo studies suggest that delivering the drugs using such type of nanocarriers could improve the efficacy–safety balance, diminishing cytotoxicity and organ toxicity, especially in leishmaniasis. This constitutes a very relevant outcome, as it opens the possibility to extended treatment regimens and improved compliance. Despite these advances, last-generation nanosystems, such as targeted nanocarriers and hybrid systems, have still not been extensively explored in the field of trypanosomatid-caused conditions and represent promising opportunities for future developments. The potential use of nanotechnology in extended, well-tolerated drug regimens is particularly interesting in the light of recent descriptions of quiescent/dormant stages of Leishmania and Trypanosoma cruzi, which have been linked to therapeutic failure.

scholarly journals Triclosan in Toothpaste, Is There Any Real Risk for the Health?

2016 ◽  
Vol 18 (2) ◽  
pp. 41
Author(s):  
Gabriela García C.D. ◽  
Alejandra Sánchez C.D., M.C. ◽  
Edith Galindo C.D., M.C., PhD. ◽  
Bernardino Cerda C.D., M.C., PhD.
Keyword(s):  
Public Opinion ◽  
State Of The Art ◽  
Endocrine System ◽  
The State ◽  
Toxic Action ◽  
Toxic Effects ◽  
Cellular Mechanisms ◽  
Real Risk

Triclosan is an antimicrobial drug that is widely used in products for human hygiene, beauty and home cleanliness. It is a common compound in toothpaste that have showed efficacy on the control and treatment of gingivitis. However, during the last decade, the triclosan has been extensively investigated because of its cytotoxicity, its ability to disturb cellular mechanisms on endocrine-system cells, and because of its cancerogenic in vitro and in vivo properties. Moreover, public opinion has paid attention to the toxic action of the triclosan. Thus, the dentist should know the state of the art about the detrimental effects of triclosan on patients’ health. This review explores the triclosan on its cytotoxicity, in vitro and in vivo cancerogenic effects, absorption in humans, and the toxic effects caused by triclosan toothpaste.

scholarly journals Anti-cancer properties of cannabidiol and Δ9-tetrahydrocannabinol and potential synergistic effects with gemcitabine, cisplatin and other cannabinoids in bladder cancer

2021 ◽  
Author(s):  
Andrea M Tomko ◽  
Erin G Whynot ◽  
Denis J Dupre
Keyword(s):  
Bladder Cancer ◽  
Cell Viability ◽  
Synergistic Effects ◽  
Transitional Cell ◽  
Chemotherapeutic Agents ◽  
Anti Cancer ◽  
Concentration Curves ◽  
Apoptotic Cascade

Introduction: With the legalization of cannabis in multiple jurisdictions throughout the world, a larger proportion of the population consumes cannabis. Several studies have demonstrated anti-tumor effects of components present in cannabis in different models. Unfortunately, little is known about the potential anti-tumoral effects of cannabinoids in bladder cancer, and how cannabinoids could potentially synergize with chemotherapeutic agents. Our study aims to identify whether a combination of cannabinoids, like cannabidiol and Δ9-tetrahydrocannabinol with agents commonly used to treat bladder cancer, such as gemcitabine and cisplatin, is able to produce desirable synergistic effects. We also evaluated whether co-treatment of different cannabinoids also generated synergistic effects. Materials and Methods: We generated concentration curves with different drugs to identify the range at which they could exert anti-tumor effects. We also evaluated the activation of the apoptotic cascade and whether cannabinoids have the ability to reduce invasion. Results: Cannabidiol, Δ9-tetrahydrocannabinol and other cannabinoids reduce cell viability of bladder cancer cell lines, and their combination with gemcitabine or cisplatin may induce differential responses: from antagonistic to additive and synergistic effects, depending on the concentrations used. Cannabidiol and Δ9-tetrahydrocannabinol were also shown to induce caspase 3 cleavage and reduce invasion in a Matrigel assay. Cannabidiol and Δ9-tetrahydrocannabinol also display synergistic properties with other cannabinoids like cannabichromene or cannabivarin. Discussion: Our results indicate that cannabinoids can reduce human bladder transitional cell carcinoma cell viability, and that they can potentially exert synergistic effects when combined with other agents. Our in vitro results will form the basis for future studies in vivo and in clinical trials for the development of new therapies that could be beneficial for the treatment of bladder cancer in the future.

Xanthohumol: A Metabolite with Promising Anti-Neoplastic Potential

2021 ◽  
Vol 21 ◽  
Author(s):  
Hardeep S. Tuli ◽  
Vaishali Aggarwal ◽  
Gaurav Parashar ◽  
Diwakar Aggarwal ◽  
Nidarshana C. Parashar ◽  
...  
Keyword(s):  
Synergistic Effects ◽  
Cancer Therapies ◽  
Cancer Subtypes ◽  
Anti Cancer ◽  
Challenges And Opportunities ◽  
In Vivo Animal Models ◽  
Different Dimensions ◽  
Made In

: The overwhelming globalburden of cancer has posed numerous challenges and opportunities for developing anti-cancer therapies. Phytochemicalshave emerged as promising synergistic compounds with potential anti-cancer effects to supplement chemo- and immune-therapeutic regimens. Anti cancer synergistic effects have been investigated in the interaction between phytocompounds derived from flavonoids such as quercetin, apigenin, kaempferol, hesperidin, emodin etc., and conventional drugs. Xanthohumol is one of the prenylatedphytoflavonoid that has demonstrated key anti-cancer activities in in vitro (anti proliferation of cancer cell lines) and in vivo(animal models of xenograft tumours)studies, and has been explored from different dimensions for targeting cancer subtypes. In the last decade, xanthohumol has been investigated how it induces the anti-cancer effects at cellular and molecular level.The different signalling cascades and targets of xanthohumolare summarized in thisreview.Overall, this reviewsummarizes the current advances made in the field of natural compounds with special reference to xanthohumol and its promising anti-cancer effectsto inhibit tumour progression.The present review hasalso touched upon the potential of xanthohumol transitioning into a lead candidate from nano-therapy viewpoint along with the challenges which need to be addressed for extensive pre-clinical and clinical anti-cancer studies.

scholarly journals Triclosan in Toothpaste, Is There Any Real Risk for the Health?

2016 ◽  
Vol 18 (2) ◽  
pp. 41
Author(s):  
Gabriela García C.D. ◽  
Alejandra Sánchez C.D., M.C. ◽  
Edith Galindo C.D., M.C., PhD. ◽  
Bernardino Cerda C.D., M.C., PhD.
Keyword(s):  
Public Opinion ◽  
State Of The Art ◽  
Endocrine System ◽  
The State ◽  
Toxic Action ◽  
Toxic Effects ◽  
Cellular Mechanisms ◽  
Real Risk

Triclosan is an antimicrobial drug that is widely used in products for human hygiene, beauty and home cleanliness. It is a common compound in toothpaste that have showed efficacy on the control and treatment of gingivitis. However, during the last decade, the triclosan has been extensively investigated because of its cytotoxicity, its ability to disturb cellular mechanisms on endocrine-system cells, and because of its cancerogenic in vitro and in vivo properties. Moreover, public opinion has paid attention to the toxic action of the triclosan. Thus, the dentist should know the state of the art about the detrimental effects of triclosan on patients’ health. This review explores the triclosan on its cytotoxicity, in vitro and in vivo cancerogenic effects, absorption in humans, and the toxic effects caused by triclosan toothpaste.

scholarly journals Cell-Penetrating CEBPB and CEBPD Leucine Zipper Decoys as Broadly Acting Anti-Cancer Agents

Cancers ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 2504
Author(s):  
Qing Zhou ◽  
Xiotian Sun ◽  
Nicolas Pasquier ◽  
Parvaneh Jefferson ◽  
Trang T. T. Nguyen ◽  
...  
Keyword(s):  
Transcription Factors ◽  
Transcriptional Activation ◽  
Leucine Zipper ◽  
Cell Penetrating Peptides ◽  
Multiple Tumor ◽  
Synthetic Cell ◽  
Anti Cancer ◽  
Cell Penetrating

Transcription factors are key players underlying cancer formation, growth, survival, metastasis and treatment resistance, yet few drugs exist to directly target them. Here, we characterized the in vitro and in vivo anti-cancer efficacy of novel synthetic cell-penetrating peptides (Bpep and Dpep) designed to interfere with the formation of active leucine-zipper-based dimers by CEBPB and CEBPD, transcription factors implicated in multiple malignancies. Both peptides similarly promoted apoptosis of multiple tumor lines of varying origins, without such effects on non-transformed cells. Combined with other treatments (radiation, Taxol, chloroquine, doxorubicin), the peptides acted additively to synergistically and were fully active on Taxol-resistant cells. The peptides suppressed expression of known direct CEBPB/CEBPD targets IL6, IL8 and asparagine synthetase (ASNS), supporting their inhibition of transcriptional activation. Mechanisms by which the peptides trigger apoptosis included depletion of pro-survival survivin and a required elevation of pro-apoptotic BMF. Bpep and Dpep significantly slowed tumor growth in mouse models without evident side effects. Dpep significantly prolonged survival in xenograft models. These findings indicate the efficacy and potential of Bpep and Dpep as novel agents to treat a variety of cancers as mono- or combination therapies.

Ethnomedicinal uses, Phytochemistry and Pharmacological Aspects of the Genus Berberis Linn: A Comprehensive Review

2020 ◽  
Vol 23 ◽  
Author(s):  
Roohi Mohi-ud-din ◽  
Reyaz Hassan Mir ◽  
Prince Ahad Mir ◽  
Saeema Farooq ◽  
Syed Naiem Raza ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Pharmacological Activities ◽  
Traditional Use ◽  
Comprehensive Review ◽  
Wide Range ◽  
Anti Cancer ◽  
Comprehensive Survey ◽  
Ethnomedicinal Uses

Background: Genus Berberis (family Berberidaceae), which contains about 650 species and 17 genera worldwide, has been used in folklore and various traditional medicine systems. Berberis Linn. is the most established group among genera with around 450-500 species across the world. This comprehensive review will not only help researchers for further evaluation but also provide substantial information for future exploitation of species to develop novel herbal formulations. Objective: The present review is focussed to summarize and collect the updated review of information of Genus Berberis species reported to date regarding their ethnomedicinal information, chemical constituents, traditional/folklore use, and reported pharmacological activities on more than 40 species of Berberis. Conclusion: A comprehensive survey of the literature reveals that various species of the genus possess various phytoconstituents mainly alkaloids, flavonoid based compounds isolated from different parts of a plant with a wide range of pharmacological activities. So far, many pharmacological activities like anti-cancer, anti-hyperlipidemic, hepatoprotective, immunomodulatory, anti-inflammatory both in vitro & in vivo and clinical study of different extracts/isolated compounds of different species of Berberis have been reported, proving their importance as a medicinal plant and claiming their traditional use.

Ferula hermonis: A Review of Current Use and Pharmacological Studies of its Sesquiterpene Ester Ferutinin

2020 ◽  
Vol 21 (5) ◽  
pp. 499-508 ◽  
Author(s):  
Rémi Safi ◽  
Marwan El-Sabban ◽  
Fadia Najjar
Keyword(s):  
Wide Spectrum ◽  
Endemic Plant ◽  
Anti Cancer ◽  
Pharmacological Studies ◽  
Sexual Impotence ◽  
Novel Applications ◽  
Anti Fungal ◽  
Sesquiterpene Ester

Ferula hermonis Boiss, is an endemic plant of Lebanon, locally known as “shilsh Elzallouh”. It has been extensively used in the traditional medicine as an aphrodisiac and for the treatment of sexual impotence. Crude extracts and isolated compounds of ferula hermonis contain phytoestrogenic substances having a wide spectrum of in vitro and in vivo pharmacological properties including anti-osteoporosis, anti-inflammatory, anti-microbial and anti-fungal, anti-cancer and as sexual activity enhancer. The aim of this mini-review is to highlight the traditional and novel applications of this plant’s extracts and its major sesquiterpene ester, ferutinin. The phytochemical constituents and the pharmacological uses of ferula hermonis crude extract and ferutinin specifically will be discussed.

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