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Natural Products and Pharmacoeconomics-1 |
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Open Access

Natural Products and Pharmacoeconomics-1

Special Issue Article

Pages: 1 - 1

Novel PPARα antagonists bearing Stilbene or Bioisosteres endowed with antiproliferative effects in cancer cell lines

Alessandra Ammazzalorso

Peroxisome Proliferator-Activated Receptors (PPARs) have been widely studied in the last decades, and they attracted the attention of scientists as promising therapeutic
targets. Intensive efforts by researchers produced a wide panel of drugs targeting the three PPAR subtypes (PPARα PPARγ PPARδ) able to modulate important metabolic
functions. PPAR activation is involved in several physiologic pathways, as lipid and glucose metabolism, insulin sensitivity, energy homeostasis, and cell differentiation.
Fibrates and thiazolidinediones, respectively synthetic PPARα and PPARγ agonists, are currently used for the treatment of hyperlipidemia and hyperglycemia, in patients
affected by type 2 diabetes and metabolic syndrome.
In recent years, an increased expression of PPARα has been found in different tumors: it is well known that cancer cells present altered metabolic pathways, switching from
the glycolysis to fatty acid oxidation metabolism. In this scenario, PPARα antagonists emerged as novel potential drugs in tumors overexpressing PPARα by interfering
with cellular survival and metastasis formation.[2] In vitro anticancer effects were found for PPARα antagonists in chronic lymphocytic leukemia [3], renal cancer, colorectal
and pancreatic cancer [4], paraganglioma [5].
In this study we report on the synthesis of novel PPARα antagonists bearing stilbene or its bioisosteres, starting from the structure of a dual PPARα/γ agonist, previously
synthesized in our laboratory. We explored the cytotoxicity of the novel compounds in different cancer cell lines (colorectal, pancreatic, renal, paraganglioma) expressing PPARα.

Special Issue Article

Pages: 2 - 2

Thymoquinone attenuates phosphorylation of AKT to inhibit kidney cancer cell proliferation

Ayed Dera *, Prasanna Rajagopalan

Background: Nigella sativa is extensively used for medical remedies since ages in Middle East. Thymoquinone (Tq) is the major active constituent of this plant in which many reports confirmed the anticancer activities of the compound. However, the effect of Tq in kidney cancer cells and the pathway of action remains unproven. Herein we report anticancer properties of Tq in the kidney cancer cells. Methods: Cancer proliferation was assessed using A498 and Caki1 kidney cancer cells 000by MTT assay. Nuclear fragmentation was detected using Hoechst 333258 and Propedium iodide dual straining. Trans endothelial migration assay was used to study migration inhibitory effects of Tq. Flow cytometry was used to analyze apoptosis and cell cycle. Anti, pro apoptotic markers and Akt phosphorylation were measured by Western bolting procedure. Results: Tq demonstrated anti-proliferative effects in A498 cells with GI50 value of 40.07 μM and Caki-1 cells with GI50 of 51.04 μM. Tq exhibited nuclear fragmentation and inhibited trans-endothelial migration of A498 and Caki-1 cells in a dose dependent manner. Time dependent increase of Annexin V positive cells and sub G0/G1 cell population was observed in both cell lines after Tq treatment. Tq increased the pro apoptotic Bax protein and reduced anti-apoptotic Bcl-2 protein dose dependently in A498 and Caki-1 cells favoring apoptosis. Increasing concentration of Tq decreased the phosphorylation of Akt in both kidney cell types. Conclusion: Our observations suggest effective anticancer activity of Tq in kidney cancer cells which may be mediated by the Akt pathway.

Special Issue Article

Pages: 3 - 3

Use of antioxidants from Brazilian Cerrado plants on veterinary medicine

Melo, FR *, Cruz-Junior, CA, Fidelis, AAG

Statement of the Problem: Several animal diseases involve an increase on reactive oxygen species (ROS) production, which could cause biological effects as aggravating of preexisting
diseases or cell damage in infectious diseases. In addition, in vitro embryo production (IVP) induces excessive ROS production, which affects blastocyst quality. Therefore,
the use of antioxidants represents an alternative to overcome oxidative stress damage both, in infectious diseases and in improving animal reproduction procedures. Brazil is a
country of interest to ethnopharmacology, especially the ecological domain Cerrado, which represents a source of biological diversity. The purpose of this study is to evaluate crude
extracts of plants from Cerrado used in traditional medicine, for the presence of phenolic compounds as well as its antioxidant activity, antibacterial and effect on apoptosis in IVP.
Methodology & Theoretical Orientation: the crude extracts were obtained from several plants selected due to its traditional use. Leaves were dried, powdered and exhaustively
extracted by maceration. The crude extracts were used do determinate in vitro phenolic compounds, antioxidant activity, antimicrobial activity, and apoptosis proportion on IVP.
Findings: All plants studied showed expressive antioxidant activity, and the phenolic compounds amounts were different for each other. Those that showed majority
antioxidant activity were used in antibacterial activity and in IVP tests. The crude extract of cagaita (Eugenia dysenterica Mart. DC.) showed antimicrobial activity against
Staphylococcus intermedius, an important bacterium that causes infection in dogs and cats. The same extract also showed a significant reduction (p<0.05) in the proportion
of apoptotic cells from embryos cultivated with 0.01 mg/mL.
Conclusion & Significance: Antioxidative activity of natural products, especially those extracted from medicinal plants, is extremally important to provide scientific data for
the treatment of infectious disease or in procedures of IVP. These extracts, normally, cause low side effects and can take advantage of complementary veterinary medicine

Special Issue Article

Pages: 4 - 4

Revisting the use of Rubefacient in reducing the blood sugar level of people with type II diabetes via Clinical Aromatherapy

Fai Chan

acceptance among the medical professionals. The word “Rubefacient” stems from the use of the drug to“produce redness of the skin, e.g. by causing dilation of the
capillaries and an increase in blood circulation. “ According to Wikipedia definition and there are some topical drugs that can achieve it. In fact , the TCM (Traditional Chinese
Medicine) uses of the technique “Gua Sha” can achieve rubefacient effect too.
The speech will discuss this technique combining with the use of essential oil massage in treating type II diabetes and how this integrative approach brings down the blood
sugar levels to a significant extent that complement well with the conventional drugs in treating the diabetes. Actually, the author made use of this to help one diabetic person
to reverse her diabetes and two of them to significant drops of blood sugar level and resolved the severe insomnia issue…
Except for the mechanical technique of “Gua Sha” , essential oil blend that can create “rubefacient” effect is also employed… The formulation and its therapeutic applications
will also be discussed. Last but not least, not each part of the whole body deserves the same attention. There will be discussion on which should go first as this will affect
the result, specially when time is limited. This presentation not only tells you the facts or evidence but also points to the way that you can improve your formulation to better
serve your customers.

Special Issue Article

Pages: 5 - 4

Supercritical CO2 technologies: A GREEN alternative with applications in natural products (HEMP) isolation and characterization

Gerard Rosse

Supercritical fluid technologies for CO2 purification (SFC) and CO2 Extraction (SFE) are efficient and cost-effective to produce intact extracts and high purity ingredients relevant to
Hemp, Flavors and Fragrances, Herbal Medicines, Spices, Decaffeination, Sterilization, Nutraceuticals & Aroma Therapy, Algae Extraction and Pharma industries. The seminar
covers fundamentals and latest applications of SFC and SFE in analysis and purification of chiral/achiral small molecules, peptides and complex extracts relevant to the Pharma,
Hemp and other Natural Products industries. CO2 extraction is a non-flammable, non-toxic process enabling isolation of volatile/non-volatile compounds and leaving no trace
of toxic residual solvent. CO2 purification is a form of liquid chromatography that happens to use CO2 as a solvent to facilitating fast analysis and separation of complex mixtures.
Both SFE and SFC use reclaimed carbon dioxide and automatically recycle it, contributing further to sustainability, high efficiency, low operating costs and increased profitability.

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