scholarly journals Biological Activity of Cannabis sativa L. Extracts Critically Depends on Solvent Polarity and Decarboxylation

Separations ◽  
2020 ◽  
Vol 7 (4) ◽  
pp. 56
Author(s):  
Guillermo Moreno-Sanz ◽  
Carlos Ferreiro Vera ◽  
Carolina Sánchez-Carnerero ◽  
Xavier Nadal Roura ◽  
Verónica Sánchez de Medina Baena
Keyword(s):  
Biological Activity ◽  
Pharmacological Activity ◽  
Transcriptional Activation ◽  
Cannabis Sativa ◽  
Solvent Polarity ◽  
Solvent Selection ◽  
Extraction And Purification ◽  
Key Aspects ◽  
The Eu

Minor cannabinoid and non-cannabinoid molecules have been proposed to significantly contribute to the pharmacological profile of cannabis extracts. Phytoplant Research has developed highly productive cannabis cultivars with defined chemotypes, as well as proprietary methods for the extraction and purification of cannabinoids. Here, we investigate the effect of solvent selection and decarboxylation on the composition and pharmacological activity of cannabis extracts. A library of forty cannabis extracts was generated from ten different cannabis cultivars registered by Phytoplant Research at the EU Community Plant Variety Office. Plant material was extracted using two different solvents, ethanol and hexane, and crude extracts were subsequently decarboxylated or not. Cannabinoid content in the resulting extracts was quantified, and biological activity was screened in vitro at three molecular targets involved in hypoxia and inflammation (NF-κB, HIF-1α and STAT3). Changes in transcriptional activation were strongly associated to solvent selection and decarboxylation. Two decarboxylated extracts prepared with hexane were the most potent at inhibiting NF-κB transcription, while HIF-1α activation was preferentially inhibited by ethanolic extracts, and decarboxylated extracts were generally more potent at inhibiting STAT3 induction. Our results indicate that solvent selection and proper decarboxylation represent key aspects of the standardized production of cannabis extracts with reproducible pharmacological activity.

scholarly journals Cannabinoids in cancer treatment: Therapeutic potential and legislation

2019 ◽  
Vol 19 (1) ◽  
pp. 14-23 ◽  
Author(s):  
Barbara Dariš ◽  
Mojca Tancer Verboten ◽  
Željko Knez ◽  
Polonca Ferk
Keyword(s):  
Cancer Treatment ◽  
Cancer Patients ◽  
Cannabis Sativa ◽  
Therapeutic Potential ◽  
Herbal Remedy ◽  
Synthetic Cannabinoids ◽  
Cancer Type ◽  
Antitumor Effects ◽  
The Eu

The plant Cannabis sativa L. has been used as an herbal remedy for centuries and is the most important source of phytocannabinoids. The endocannabinoid system (ECS) consists of receptors, endogenous ligands (endocannabinoids) and metabolizing enzymes, and plays an important role in different physiological and pathological processes. Phytocannabinoids and synthetic cannabinoids can interact with the components of ECS or other cellular pathways and thus affect the development/progression of diseases, including cancer. In cancer patients, cannabinoids have primarily been used as a part of palliative care to alleviate pain, relieve nausea and stimulate appetite. In addition, numerous cell culture and animal studies showed antitumor effects of cannabinoids in various cancer types. Here we reviewed the literature on anticancer effects of plant-derived and synthetic cannabinoids, to better understand their mechanisms of action and role in cancer treatment. We also reviewed the current legislative updates on the use of cannabinoids for medical and therapeutic purposes, primarily in the EU countries. In vitro and in vivo cancer models show that cannabinoids can effectively modulate tumor growth, however, the antitumor effects appear to be largely dependent on cancer type and drug dose/concentration. Understanding how cannabinoids are able to regulate essential cellular processes involved in tumorigenesis, such as progression through the cell cycle, cell proliferation and cell death, as well as the interactions between cannabinoids and the immune system, are crucial for improving existing and developing new therapeutic approaches for cancer patients. The national legislation of the EU Member States defines the legal boundaries of permissible use of cannabinoids for medical and therapeutic purposes, however, these legislative guidelines may not be aligned with the current scientific knowledge.

scholarly journals Study on Transformation of Ginsenosides in Different Methods

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Meng-meng Zheng ◽  
Fang-xue Xu ◽  
Yu-juan Li ◽  
Xiao-zhi Xi ◽  
Xiao-wei Cui ◽  
...  
Keyword(s):  
Biological Activity ◽  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Pharmacological Activity ◽  
Theoretical Foundation ◽  
Major Constituent ◽  
Chemical Methods ◽  
Physical Methods ◽  
Medicinal Value

Ginseng is a traditional Chinese medicine and has the extensive pharmacological activity. Ginsenosides are the major constituent in ginseng and have the unique biological activity and medicinal value. Ginsenosides have the good effects on antitumor, anti-inflammatory, antioxidative and inhibition of the cell apoptosis. Studies have showed that the major ginsenosides could be converted into rare ginsenosides, which played a significant role in exerting pharmacological activity. However, the contents of some rare ginsenosides are very little. So it is very important to find the effective way to translate the main ginsenosides to rare ginsenosides. In order to provide the theoretical foundation for the transformation of ginsenoside in vitro, in this paper, many methods of the transformation of ginsenoside were summarized, mainly including physical methods, chemical methods, and biotransformation methods.

scholarly journals Structure-Activity Relationship Analysis of Benzotriazine Analogues as HIV-1 Latency-Reversing Agents

2020 ◽  
Vol 64 (8) ◽  
Author(s):  
Eric S. Sorensen ◽  
Amanda B. Macedo ◽  
Rachel S. Resop ◽  
J. Natalie Howard ◽  
Racheal Nell ◽  
...  
Keyword(s):  
Biological Activity ◽  
Transcriptional Activation ◽  
Transcriptional Activity ◽  
Cell Model ◽  
Systematic Analysis ◽  
Immune Effector ◽  
Relationship Analysis ◽  
Latent Hiv

ABSTRACT “Shock and kill” therapeutic strategies toward HIV eradication are based on the transcriptional activation of latent HIV with a latency-reversing agent (LRA) and the consequent killing of the reactivated cell by either the cytopathic effect of HIV or an arm of the immune system. We have recently found several benzotriazole and benzotriazine analogues that have the ability to reactivate latent HIV by inhibiting signal transducer and activator of transcription 5 (STAT5) SUMOylation and promoting STAT5 binding to the HIV long terminal repeat and increasing its transcriptional activity. To understand the essential structural groups required for biological activity of these molecules, we performed a systematic analysis of >40 analogues. First, we characterized the essential motifs within these molecules that are required for their biological activity. Second, we identified three benzotriazine analogues with similar activity. We demonstrated that these three compounds are able to increase STAT5 phosphorylation and transcriptional activity. All active analogues reactivate latent HIV in a primary cell model of latency and enhance the ability of interleukin-15 to reactivate latent HIV in cells isolated from aviremic participants. Third, this family of compounds also promote immune effector functions in vitro in the absence of toxicity or global immune activation. Finally, initial studies in mice suggest lack of acute toxicity in vivo. A better understanding of the biological activity of these compounds will help in the design of improved LRAs that work via inhibition of STAT5 SUMOylation.

scholarly journals Chemical Composition and Biological Activity of Trapa Natans L.

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Rosa Cukic Corovic ◽  
Jovana Bradic ◽  
Marina Tomovic ◽  
Vera Dabanovic ◽  
Vladimir Jakovljevic ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biological Activity ◽  
Chemical Composition ◽  
North America ◽  
Pharmacological Activity ◽  
In Vitro Antimicrobial Activity ◽  
Water Chestnut ◽  
Trapa Natans ◽  
Anti Inflammatory

Abstract Trapa natans L., water chestnut (indian name singada, montenegrin name kasaronja) belonging to Trapaceae family is annual aquatic floating herb native to Asia but widely distributed in the Europe and in North America. The presence of two species, Trapa natans L. and Trapa longicarpa M.Jank. ssp. scutarensis M.Jank has been confirmed on the Skadar lake in Montenegro. Trapa natans is a plant demonstrating promising pharmacological activity mostly due to the presence of its constituens, phenols and flavonoids, showed hepatoprotective potential, antioxidant, anti-inflammatory, antidiabetic, antifungal and in vitro antimicrobial activity.

scholarly journals Use of octadecasilyl-silica for the extraction and purification of peptides in biological samples. Application to the identification of circulating metabolites of corticotropin-(1-24)-tetracosapeptide and somatostatin in vivo

1977 ◽  
Vol 168 (1) ◽  
pp. 9-13 ◽  
Author(s):  
H P J Bennett ◽  
A M Hudson ◽  
C McMartin ◽  
G E Purdon
Keyword(s):  
Aqueous Solution ◽  
Biological Activity ◽  
Solvent Mixtures ◽  
Plasma Samples ◽  
Peptide Fragments ◽  
Single Product ◽  
Extraction And Purification ◽  
Aqueous Solvent

Peptides can be adsorbed on octadecasilyl-silica from large volumes of aqueous solution and eluted with aqueous solvent mixtures containing methanol or acetonitrile. These properties may be used for the extraction and purification of peptide fragments in plasma samples collected from rats. After intravenous injection of Synacthen [corticotropin-(1-24)-tetracosapeptide], it was shown that within 2 min the main circulating products were intact peptide and its sulphoxide. In addition, a number of fragments indicative of cleavage at the N- and C-termini were present. Most of the products formed from Synacthen have low biological activity. Somatostatin was rapidly cleaved in vivo and in vitro to a single product, which probably retains biological activity. The absence of other circulating products suggests that somatostatin is only inactivated once it leaves the circulation.

In Vitro Activity of Phytocannabinoids from High Potency Cannabis sativa

Planta Medica ◽  
2012 ◽  
Vol 78 (05) ◽  
Author(s):  
A Husni ◽  
S Ross ◽  
O Dale ◽  
C Gemelli ◽  
G Ma ◽  
...  
Keyword(s):  
Cannabis Sativa ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
High Potency

Pharmacological activity of Mexican basidiomycetes species cultivated in vitro

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
L Garza-Ocañas ◽  
E Tamez de la O ◽  
XS Ramírez-Gómez ◽  
F Garza-Ocañas ◽  
MT Zanatta Calderón ◽  
...  
Keyword(s):  
Pharmacological Activity

COMPARATIVE STUDIES OF THE POTENTIATION OF CORTICOTROPHIN ACTIVITY BY SEVERAL INACTIVE DERIVATIVES

1963 ◽  
Vol 42 (2) ◽  
pp. 209-213 ◽  
Author(s):  
Arthur I. Cohen ◽  
Edward H. Frieden
Keyword(s):  
Biological Activity ◽  
Comparative Studies ◽  
Free Amino ◽  
Hormonal Activity ◽  
Amino Groups

ABSTRACT A number of corticotrophin analogues have been prepared, some of which potentiate the biological activity of the untreated hormone in vitro. The free amino groups of corticotrophin appear to be essential not only for hormonal activity, but also for the interaction of the analogues with the tissue corticotrophin inactivating system which is assumed to account for the potentiating effect.

Biological activity mediated by sfingosine-1-phospate receptors in human primary granulosa cells and immortalized granulosa cell line in vitro

2017 ◽  
Author(s):  
Livio Casarini ◽  
Giulia Fornari ◽  
Manuela Simoni ◽  
Francesco Poti
Keyword(s):  
Biological Activity ◽  
Cell Line ◽  
Granulosa Cell ◽  
Granulosa Cells

Political aspects of security of the European Union Member States

2020 ◽  
pp. 97-105
Author(s):  
Aleksandra Kusztykiewicz-Fedurek
Keyword(s):  
European Union ◽  
Negative Impact ◽  
The European Union ◽  
Member States ◽  
Eu Member States ◽  
Political Security ◽  
New Institutions ◽  
The Stability ◽  
Key Aspects ◽  
The Eu

Political security is very often considered through the prism of individual states. In the scholar literature in-depth analyses of this kind of security are rarely encountered in the context of international entities that these countries integrate. The purpose of this article is to draw attention to key aspects of political security in the European Union (EU) Member States. The EU as a supranational organisation, gathering Member States first, ensures the stability of the EU as a whole, and secondly, it ensures that Member States respect common values and principles. Additionally, the EU institutions focus on ensuring the proper functioning of the Eurozone (also called officially “euro area” in EU regulations). Actions that may have a negative impact on the level of the EU’s political security include the boycott of establishing new institutions conducive to the peaceful coexistence and development of states. These threats seem to have a significant impact on the situation in the EU in the face of the proposed (and not accepted by Member States not belonging to the Eurogroup) Eurozone reforms concerning, inter alia, appointment of the Minister of Economy and Finance and the creation of a new institution - the European Monetary Fund.

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