scholarly journals Nanotechnology-Based Celastrol Formulations and Their Therapeutic Applications

2021 ◽  
Vol 12 ◽  
Author(s):  
Pushkaraj Rajendra Wagh ◽  
Preshita Desai ◽  
Sunil Prabhu ◽  
Jeffrey Wang
Keyword(s):  
Unmet Need ◽  
Aqueous Solubility ◽  
Clinical Translation ◽  
Quinone Methide ◽  
Root Extract ◽  
Therapeutic Applications ◽  
The Past ◽  
Anti Cancer ◽  
Anti Oxidant

Celastrol (also called tripterine) is a quinone methide triterpene isolated from the root extract of Tripterygium wilfordii (thunder god vine in traditional Chinese medicine). Over the past two decades, celastrol has gained wide attention as a potent anti-inflammatory, anti-autoimmune, anti-cancer, anti-oxidant, and neuroprotective agent. However, its clinical translation is very challenging due to its lower aqueous solubility, poor oral bioavailability, and high organ toxicity. To deal with these issues, various formulation strategies have been investigated to augment the overall celastrol efficacy in vivo by attempting to increase the bioavailability and/or reduce the toxicity. Among these, nanotechnology-based celastrol formulations are most widely explored by pharmaceutical scientists worldwide. Based on the survey of literature over the past 15 years, this mini-review is aimed at summarizing a multitude of celastrol nanoformulations that have been developed and tested for various therapeutic applications. In addition, the review highlights the unmet need in the clinical translation of celastrol nanoformulations and the path forward.

Novel Findings of Anti-cancer Property of Propofol

2018 ◽  
Vol 18 (2) ◽  
pp. 156-165 ◽  
Author(s):  
Jiaqiang Wang ◽  
Chien-shan Cheng ◽  
Yan Lu ◽  
Xiaowei Ding ◽  
Minmin Zhu ◽  
...  
Keyword(s):  
General Anesthesia ◽  
Cancer Progression ◽  
Molecular Mechanisms ◽  
Intravenous Anesthetic ◽  
The Past ◽  
Anti Cancer ◽  
Underlying Mechanisms ◽  
Recent Attention

Background: Propofol, a widely used intravenous anesthetic agent, is traditionally applied for sedation and general anesthesia. Explanation: Recent attention has been drawn to explore the effect and mechanisms of propofol against cancer progression in vitro and in vivo. Specifically, the proliferation-inhibiting and apoptosis-inducing properties of propofol in cancer have been studied. However, the underlying mechanisms remain unclear. Conclusion: This review focused on the findings within the past ten years and aimed to provide a general overview of propofol's malignance-modulating properties and the potential molecular mechanisms.

scholarly journals Economic Value of Agarwood and Its Prospects of Cultivation

2021 ◽  
Vol 9 (1) ◽  
pp. 23-31
Author(s):  
Suraj Raj Adhikari ◽  
Kusum Pokhrel ◽  
Sunil Dutta Baral
Keyword(s):  
New Technology ◽  
Economic Value ◽  
Traditional Medicines ◽  
Hill Country ◽  
The Past ◽  
Northern India ◽  
Anti Cancer ◽  
Pharmacological Studies ◽  
Anti Oxidant ◽  
The Hill

Aquilaria are genera of tropical trees that produces a valuable resinous wood called agarwood. Agarwood plant have been widely used as traditional medicines and Ayurvedic medicine. They are used for the treatment of arthritis, asthma, diarrhoea etc effects. It contains bioactive phytochemical sesquiterpenoids, 2 (-2-phenylethyl)-4H-chromen-4-one derivatives, genkwanins, mangiferins, cucurbitacins, other terpenoids and phenolic acids. Many pharmacological studies have been performed on anti-allergic, anti-cancer, anti-inflammatory, anti-microbial, anti-diabetic, anti-oxidant, etc. The aromatic properties of agarwood when burned or distilled are extraordinary and there is high demand for the resinous wood to make incense, perfume and as traditional medicine. Aquilaria are native to northern India but over harvesting of this tree as well as other forest trees in the past has ravaged the hill country. With new technology that has been developed to induce agarwood in trees, it is now possible to produce a sustainable high valued agarwood in young plantation trees. The growing of Aquilaria in the hill agro-ecosystems of Nepal and cultivation of agarwood as a crop using new technology could provide a new economy for the region. Int. J. Appl. Sci. Biotechnol. Vol 9(1): 23-31

IN VIVO AND IN VITRO EVALUATION OF ANTI-CANCER ACTIVITY OF NEWLY SYNTHESIZED COBALT COMPLEX OF COUMARIN SCHIFF BASES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (04) ◽  
pp. 61-69
Author(s):  
A. Rayaji ◽  
A. H. M. Viswanatha Swamy ◽  
Keyword(s):  
Nitric Oxide ◽  
Hepg2 Cell ◽  
Cobalt Complex ◽  
Reducing Ability ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Hepg2 Cell Lines ◽  
Cancer Activity

Hepatocarcinogenesis is a multistep process involving different genetic alterations that ultimately lead to malignant transformation of the hepatocytes. Modern treatment of cancer includes chemotherapy, hormone therapy, radiotherapy and surgery but they are associated with several adverse effects such as alopecia, fatigue and general weakening of the body’s immune system due to bone marrow suppression. However, there is a continual need to look out for newer drugs to overcome the menace of cancer. In view of this we synthesized the new Coumarin-Cobalt complex derivatives. Structures of all the newly synthesized metal complexes are supported by Spectral data such as IR, NMR, and mass spectrometry. Coumarin-Cobalt complex of vanillin exhibited significant anti-cancer activity by in vivo anticancer activity (BrdU estimation). Immunohistochemical analysis has been done by BrdU and the synthesized compounds were screened for anti-oxidant activity and in vitro HepG2 cell lines. The IC50 values of the HepG2 cell lines as compared with that of standard Cisplatin and compounds IIIb, IIId, IIIe, IIIh and IIIj showed appreciable activity at a concentration less than 10 μG. Coumarin-Cobalt complex of vanillin exhibited significant anti-cancer activity. Anti-oxidant activity performed by Nitric oxide reducing ability, Superoxide dismutase and reducing activity:Compounds IIIc, IIIe and IIIg showed appreciable activity at 400μg/mL and 800 μg/mL screened by nitric oxide reducing ability, superoxide anion was effectively scavenged by compound IIIg at 400μg/mL and 800 μg/mL and reducing power of compounds IIIc and IIIj is comparable with standard ascorbic acid at concentrations 400μg/mL and 800 μg/mL.

scholarly journals Pharmacological Utilization of Bergamottin, Derived from Grapefruits, in Cancer Prevention and Therapy

2018 ◽  
Vol 19 (12) ◽  
pp. 4048 ◽  
Author(s):  
Jeong-Hyeon Ko ◽  
Frank Arfuso ◽  
Gautam Sethi ◽  
Kwang Ahn
Keyword(s):  
Causes Of Death ◽  
Treatment Options ◽  
Unmet Need ◽  
Molecular Targets ◽  
Pharmacological Agents ◽  
Natural Agents ◽  
Anti Cancer ◽  
Prevention And Therapy

Cancer still remains one of the leading causes of death worldwide. In spite of significant advances in treatment options and the advent of novel targeted therapies, there still remains an unmet need for the identification of novel pharmacological agents for cancer therapy. This has led to several studies evaluating the possible application of natural agents found in vegetables, fruits, or plant-derived products that may be useful for cancer treatment. Bergamottin is a furanocoumarin derived from grapefruits and is also a well-known cytochrome P450 inhibitor. Recent studies have demonstrated potent anti-oxidative, anti-inflammatory, and anti-cancer properties of grapefruit furanocoumarin both in vitro and in vivo. The present review focuses on the potential anti-neoplastic effects of bergamottin in different tumor models and briefly describes the molecular targets affected by this agent.

scholarly journals IgE Antibodies: From Structure to Function and Clinical Translation

Antibodies ◽  
2019 ◽  
Vol 8 (1) ◽  
pp. 19 ◽  
Author(s):  
Brian Sutton ◽  
Anna Davies ◽  
Heather Bax ◽  
Sophia Karagiannis
Keyword(s):  
Conformational Changes ◽  
Immunoglobulin E ◽  
Fc Receptors ◽  
Solid Tumours ◽  
Clinical Translation ◽  
Therapeutic Modality ◽  
Ige Antibodies ◽  
Effector Functions ◽  
Anti Cancer

Immunoglobulin E (IgE) antibodies are well known for their role in mediating allergic reactions, and their powerful effector functions activated through binding to Fc receptors FcεRI and FcεRII/CD23. Structural studies of IgE-Fc alone, and when bound to these receptors, surprisingly revealed not only an acutely bent Fc conformation, but also subtle allosteric communication between the two distant receptor-binding sites. The ability of IgE-Fc to undergo more extreme conformational changes emerged from structures of complexes with anti-IgE antibodies, including omalizumab, in clinical use for allergic disease; flexibility is clearly critical for IgE function, but may also be exploited by allosteric interference to inhibit IgE activity for therapeutic benefit. In contrast, the power of IgE may be harnessed to target cancer. Efforts to improve the effector functions of therapeutic antibodies for cancer have almost exclusively focussed on IgG1 and IgG4 subclasses, but IgE offers an extremely high affinity for FcεRI receptors on immune effector cells known to infiltrate solid tumours. Furthermore, while tumour-resident inhibitory Fc receptors can modulate the effector functions of IgG antibodies, no inhibitory IgE Fc receptors are known to exist. The development of tumour antigen-specific IgE antibodies may therefore provide an improved immune functional profile and enhanced anti-cancer efficacy. We describe proof-of-concept studies of IgE immunotherapies against solid tumours, including a range of in vitro and in vivo evaluations of efficacy and mechanisms of action, as well as ex vivo and in vivo safety studies. The first anti-cancer IgE antibody, MOv18, the clinical translation of which we discuss herein, has now reached clinical testing, offering great potential to direct this novel therapeutic modality against many other tumour-specific antigens. This review highlights how our understanding of IgE structure and function underpins these exciting clinical developments.

scholarly journals Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel

Polymers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 577 ◽  
Author(s):  
Wafaa E. Soliman ◽  
Tamer M. Shehata ◽  
Maged E. Mohamed ◽  
Nancy S. Younis ◽  
Heba S. Elsewedy
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Delivery Methods ◽  
Anti Cancer ◽  
Permeation Studies ◽  
Anti Inflammatory

Background: Curcumin (Cur) possesses a variety of beneficial pharmacological properties including antioxidant, antimicrobial, anti-cancer and anti-inflammatory activities. Nevertheless, the low aqueous solubility and subsequent poor bioavailability greatly limits its effectiveness. Besides, the role of myrrh oil as an essential oil in treating inflammatory disorders has been recently demonstrated. The objective of the current investigation is to enhance Cur efficacy via developing Cur nanoemulgel, which helps to improve its solubility and permeability, for transdermal delivery. Methods: The formulated preparations (Cur gel, emulgel and nanoemulgel) were evaluated for their physical appearance, spreadability, viscosity, particle size, in vitro release and ex vivo drug permeation studies. The in vivo anti-inflammatory activity was estimated using the carrageenan-induced rat hind paw edema method. Results: The formulated Cur-loaded preparations exhibited good physical characteristics that were in the acceptable range of transdermal preparations. The release of Cur from gel, emulgel and nanoemulgel after 12 h was 72.17 ± 3.76, 51.93 ± 3.81 and 62.0 ± 3.9%, respectively. Skin permeation of Cur was significantly (p < 0.05) improved when formulated into nanoemulgel since it showed the best steady state transdermal flux (SSTF) value (108.6 ± 3.8 µg/cm2·h) with the highest enhancement ratio (ER) (7.1 ± 0.2). In vivo anti-inflammatory studies proved that Cur-loaded nanoemulgel displayed the lowest percent of swelling (26.6% after 12 h). Conclusions: The obtained data confirmed the potential of the nanoemulgel dosage form and established the synergism of myrrh oil and Cur as an advanced anti-inflammatory drug.

scholarly journals Anti-Oxidant and Hepatoprotective Effects of Senecio biafrae on CCl4-induced Liver Damage in Rats

2019 ◽  
Vol 13 (2) ◽  
pp. 31-35
Author(s):  
Israel Oghenevwodoko Okoro ◽  
◽  
Helen Ejiro Kadiri ◽  
Keyword(s):  
Negative Control Group ◽  
Positive Control ◽  
Negative Control ◽  
Control Group ◽  
Albino Rats ◽  
Root Extract ◽  
Distilled Water ◽  
Standard Drug ◽  
Anti Oxidant

Background: The present study was performed to explore whether the aqueous extract of Senecio biafrae (S. biafrae) roots provide any in vivo protective activity against carbon tetrachloride (CCl4)-induced hepatotoxicity in male albino rats. Methods: Rats (150-200 grams) were grouped into five groups (A-E) of six rats each and were treated orally for twelve days with 72 hourly administration of CCl4 (1 mL/kg) as follows: Group A received distilled water only (negative control), Group B was administered distilled water plus CCl4 (positive control), Group C was administered 400 mg/kg extract and CCl4, Group D received 200 mg/extract and CCl4, while Group E was administered standard drug (Silymarin 25mg/kg, PO). Results: Pre-treatment with the extract of S. biafrae (200 or 400mg/kg) or Silymarin (25mg/kg) caused significant restoration in the biomarkers as evaluated by reducing the levels of malondialdehyde, transaminases and elevating the levels of superoxide dismutase, catalase and glutathione peroxidase activities, which were altered by CCl4 toxicity. The extract at a dose of 400mg/kg demonstrated similar activities comparable to the standard drug (Silymarin). Conclusion: The results of this study indicate that the root extract of S. biafrae possesses hepatoprotective and anti-oxidant properties which may be due to the presence of phytochemicals in it.

A Review of Various Pharmacological Effects of Quercetin with its Barriers and Approaches for Solubility and Permeability Enhancement

2021 ◽  
Vol 11 ◽  
Author(s):  
Rakesh Mishra ◽  
Shweta Kulkarni
Keyword(s):  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Pharmacological Effects ◽  
Pharmacological Activities ◽  
Human Diet ◽  
Permeability Enhancement ◽  
Current Review ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Novel Approaches

Background: Quercetin, one of the most beneficial flavonoids, has been included in the human diet due to its therapeutic effect on health. Recently, Quercetin is gaining scientific attraction for its multifarious activities, including anti-oxidant, anti-inflammatory, antiviral, anti-diabetic, anti-cancer, anti-arthritic, as well as function to ease some cardiovascular diseases. However, these applications of quercetin in the pharmaceutical field are limited due to its poor aqueous solubility and poor permeability. Objective: The present review summarizes various pharmacological activities of quercetin, analyses the barriers like solubility and permeability, which restrict the therapeutic efficiency of quercetin, and also discusses novel approaches to enhance aqueous solubility and permeability of quercetin for its effective clinical use. Methods: The current review information sources were peer-reviewed relevant scientific articles of recognized journals from scientific engines and databases (Scopus, Web of Science, PubMed, Science Direct, Google Scholar) using different key words related to quercetin pharmacological effects, mechanism, solubility, permeability, absorption barriers, and formulation approaches. Results: Various novel approaches, including solid dispersions, inclusion complex, pro-drugs, nanoemulsion, micelles, liposomes, SNEEDS, and microspheres, have been developed to overcome the solubility and permeability barriers for efficient quercetin delivery. Conclusion: This review revealed that the multifaceted pharmacological activities of quercetin for management of various disease are enormously dependent on the development of novel and safe drug delivery systems of quercetin.

scholarly journals In vivo Anti-Cancer Activity of N-halamines

2016 ◽  
Vol 9 (1) ◽  
pp. 20
Author(s):  
Faten Zahran ◽  
Akaber T. Keshta ◽  
Abd El-Shafey I. Ahmed
Keyword(s):  
Ehrlich Ascites Carcinoma ◽  
Positive Control ◽  
Positive Control Group ◽  
Control Group ◽  
In Vivo Antitumor Activity ◽  
Ehrlich Ascites ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Copolymer 1

Purpose: N-halamines were known for their antimicrobial action due to the presence of halogen in their structure. In our search for new anti-cancer agents, we have evaluated the anti-cancer and anti-oxidant properties of some synthetic N-Halamines with high and low molecular weight in comparison with their non-halogenated forms. Urea epichlorohydrin copolymer (1), 4(1H, 3H-2, 6-dioxo-1, 3, 5-trizenyl)-O-iminomethylpolyethylene (3) and cynuric acid (5) in addition to their halogenated forms 2, 4 and 6 were selected for this study. Methodology: the toxicity for the synthesized compounds was determined. The anti-cancer and anti-oxidant activities were studied by evaluation the viability of tumor cells, life span prolongation, and estimation of antioxidants, and effects of these compounds on liver histology. Findings: Doses up to 2000 mg/kg indicated good safety in all investigated compounds. In Vivo antitumor activity results against Ehrlich ascites carcinoma (EAC) cells for the investigated compounds revealed that, the volume of ascites was significantly decreased in compounds 1, 2, 3, 4, 5 and 6 treated groups. EAC cell count was significantly reduced for similar groups, respectively, compared to the positive control group. Malonadildehyde, and nitric oxide showed a significant reduction in their levels in the treated groups, while catalase showed a significant elevation in its activity in the same groups compared to positive control group. Conclusion: Halogenated compounds showed good anti-oxidant behavior while compound 6 showed the best anti-tumor effect.

scholarly journals The Genus Eriosema (Fabaceae): From the Ethnopharmacology to an Evidence-Based Phytotherapeutic Perspective?

2021 ◽  
Vol 12 ◽  
Author(s):  
Sylvin Benjamin Ateba ◽  
Dieudonné Njamen ◽  
Liselotte Krenn
Keyword(s):  
Therapeutic Potential ◽  
Food Supplement ◽  
Iucn Red List ◽  
Convincing Evidence ◽  
Benzoic Acid Derivatives ◽  
Iucn Red List Categories ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Ethnobotanical Uses

The genus Eriosema (Fabaceae) includes approximately 150 species widely distributed across tropical and subtropical regions of the world (Africa, Neotropics, Asia and Australia). Throughout these regions, several species are used since centuries in different traditional medicinal systems, while others are used as food or food supplement. The present review attempts to critically summarize current information concerning the uses, phytochemistry and pharmacology of the Eriosema genus and to evaluate the therapeutic potential. The information published in English and French (up to September 2020) on ethnopharmacology or traditional uses, chemistry, pharmacology and toxicology of Eriosema genus was collected from electronic databases [SciFinder, PubMed, Google, Google Scholar, Scopus, Web of Science, Prelude Medicinal Plants—http://www.ethnopharmacologia.org/recherche-dans-prelude/?plant, The Plant List (http://www.theplantlist.org/), POWO (http://powo.science.kew.org/) and IUCN Red List Categories (https://www.iucnredlist.org/)], conference proceedings, books, M.Sc. and Ph.D. dissertations. The information retrieved on the ethnomedicinal indications of Eriosema genus allowed to list 25 species (∼16.6% of the genus). The majority of uses is recorded from Africa. Phytochemical analyses of 8 species led to the identification and/or isolation of 107 compounds, with flavonoids (69.2%), chromones (7.5%) and benzoic acid derivatives (3.7%) as the main chemical classes. Pharmacological investigations with crude extracts and isolated compounds showed a broad range of activities including aphrodisiac, estrogenic, anti-osteoporosis, hypolipidemic, anti-diabetic, anti-diarrheal, anti-microbial, anti-oxidant, anthelmintic, anti-cancer, and acetylcholinesterase inhibitory activities. Despite the low number of Eriosema species tested, there is convincing evidence in vitro and in vivo studies validating some traditional and ethnobotanical uses. However, the utility of several of the described uses has not yet been confirmed in pharmacological studies. Reviewed data could serve as a reference tool and preliminary information for advanced research on Eriosema species.

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