scholarly journals Pharmacokinetic Comparisons of Naringenin and Naringenin-Nicotinamide Cocrystal in Rats by LC-MS/MS

2020 ◽  
Vol 2020 ◽  
pp. 1-10
Author(s):  
Dan Xu ◽  
Gui-Qiu Zhang ◽  
Ting-Ting Zhang ◽  
Bo Jin ◽  
Chen Ma
Keyword(s):  
Water Solubility ◽  
Relative Bioavailability ◽  
Physical Mixture ◽  
Pharmacological Activities ◽  
Rapid Absorption ◽  
Wide Range ◽  
Poor Water Solubility

Naringenin (NAR), 4′,5,7-trihydroxydihydroflavone, has a wide range of pharmacological activities but shows poor water solubility and low bioavailability. The pharmacokinetics and bioavailability of naringenin-nicotinamide cocrystal (NAR-NCT), which offers improved solubility, were evaluated in this study. Rats were orally administered NAR, a physical mixture of naringenin and nicotinamide (NAR + NCT), and NAR-NCT. The relative bioavailability of NAR-NCT was 175.09% of NAR, Cmax was 8.43 and 2.06 times of NAR and NAR + NCT, respectively, Tmax was advanced from 0.49 h to 0.09 h, CL was decreased from 91.1 L/h/kg to 49.1 L/h/kg, and t1/2 was increased from 5.37 h to 8.24 h, highlighting its rapid absorption and slow elimination. This study showed that NAR-NCT could improve the bioavailability of NAR.

NMR Studies of the Inclusion Complexes Between Ezetimibe and Cyclodextrins

2018 ◽  
Vol 69 (7) ◽  
pp. 1838-1841
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Bela Noszal ◽  
Gabor Orgovan
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Solution Nmr ◽  
Spectroscopic Techniques ◽  
Nmr Studies ◽  
The Poor ◽  
Poor Water Solubility

Ezetimibe, the antihyperlipidemic drug of poor bioavailability was complexed with native and derivatized cyclodextrins.The complexes were characterized in terms stability, stoichiometry and structure using various 1D and 2D solution NMR spectroscopic techniques. The complexes were found to be of moderate stability (logK[3). The least stable inclusion complex is formed with b-cyclodextrin, while the ezetimibe-methylated-b--cyclodextrin has a 7-fold higher stability. The results can be useful to improve the poor water-solubility and the concomitant bioavailability of ezetimibe.

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.

Nanoparticles Functionalized with Venom-Derived Peptides and Toxins for Pharmaceutical Applications

2020 ◽  
Vol 21 (2) ◽  
pp. 97-109 ◽  
Author(s):  
Ana P. dos Santos ◽  
Tamara G. de Araújo ◽  
Gandhi Rádis-Baptista
Keyword(s):  
Oral Absorption ◽  
Current Data ◽  
Pharmacological Activities ◽  
Venom Peptides ◽  
Essential Components ◽  
Wide Range ◽  
Different Types ◽  
Direct Use ◽  
Animal Venoms ◽  
Pharmaceutical Biotechnology

Venom-derived peptides display diverse biological and pharmacological activities, making them useful in drug discovery platforms and for a wide range of applications in medicine and pharmaceutical biotechnology. Due to their target specificities, venom peptides have the potential to be developed into biopharmaceuticals to treat various health conditions such as diabetes mellitus, hypertension, and chronic pain. Despite the high potential for drug development, several limitations preclude the direct use of peptides as therapeutics and hamper the process of converting venom peptides into pharmaceuticals. These limitations include, for instance, chemical instability, poor oral absorption, short halflife, and off-target cytotoxicity. One strategy to overcome these disadvantages relies on the formulation of bioactive peptides with nanocarriers. A range of biocompatible materials are now available that can serve as nanocarriers and can improve the bioavailability of therapeutic and venom-derived peptides for clinical and diagnostic application. Examples of isolated venom peptides and crude animal venoms that have been encapsulated and formulated with different types of nanomaterials with promising results are increasingly reported. Based on the current data, a wealth of information can be collected regarding the utilization of nanocarriers to encapsulate venom peptides and render them bioavailable for pharmaceutical use. Overall, nanomaterials arise as essential components in the preparation of biopharmaceuticals that are based on biological and pharmacological active venom-derived peptides.

Bioprospecting Cryptogams as Potential Source of Unique Biodynamic Phytochemicals with Diverse Pharmaceutical Applications

2016 ◽  
Vol 1 (1) ◽  
Author(s):  
Brahma N. Singh ◽  
Garima Pandey ◽  
Prateeksha ◽  
J. Kumar
Keyword(s):  
Secondary Metabolites ◽  
Higher Plants ◽  
New Drugs ◽  
Terrestrial Plants ◽  
Pharmacological Activities ◽  
Therapeutic Drugs ◽  
Potential Source ◽  
Therapeutic Value ◽  
Wide Range ◽  
Novel Structures

With the advent of green pharmaceuticals, the secondary metabolites derived from plants have provided numerous leads for the development of a wide range of therapeutic drugs; however the discovery of new drugs with novel structures has declined in the past few years. Cryptogams including lichens, bryophytes, and pteridophytes represent a group of small terrestrial plants that remain relatively untouched in the drug discovery process though some have been used as ethnomedicines by various tribes worldwide. Studies of their secondary metabolites are recent but reveal unique secondary metabolites which are not synthesized by higher plants. These compounds can have the potential to develop more potential herbal drugs for prevention and treatment of diseases The present article . deals with the secondary metabolites and pharmacological activities of cryptogams with an objective to bring them forth as potential source of biodynamic compounds of therapeutic value.

scholarly journals Jojoba Oil: An Updated Comprehensive Review on Chemistry, Pharmaceutical Uses, and Toxicity

Polymers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1711
Author(s):  
Heba A. Gad ◽  
Autumn Roberts ◽  
Samirah H. Hamzi ◽  
Haidy A. Gad ◽  
Ilham Touiss ◽  
...  
Keyword(s):  
Industrial Applications ◽  
Literature Survey ◽  
Jojoba Oil ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Liver Functions ◽  
History Of ◽  
History Of Use ◽  
Pharmaceutical Uses ◽  
Obesity And Cancer

Jojoba is a widely used medicinal plant that is cultivated worldwide. Its seeds and oil have a long history of use in folklore to treat various ailments, such as skin and scalp disorders, superficial wounds, sore throat, obesity, and cancer; for improvement of liver functions, enhancement of immunity, and promotion of hair growth. Extensive studies on Jojoba oil showed a wide range of pharmacological applications, including antioxidant, anti-acne and antipsoriasis, anti-inflammatory, antifungal, antipyretic, analgesic, antimicrobial, and anti-hyperglycemia activities. In addition, Jojoba oil is widely used in the pharmaceutical industry, especially in cosmetics for topical, transdermal, and parenteral preparations. Jojoba oil also holds value in the industry as an anti-rodent, insecticides, lubricant, surfactant, and a source for the production of bioenergy. Jojoba oil is considered among the top-ranked oils due to its wax, which constitutes about 98% (mainly wax esters, few free fatty acids, alcohols, and hydrocarbons). In addition, sterols and vitamins with few triglyceride esters, flavonoids, phenolic and cyanogenic compounds are also present. The present review represents an updated literature survey about the chemical composition of jojoba oil, its physical properties, pharmacological activities, pharmaceutical and industrial applications, and toxicity.

scholarly journals Rheology and Water Absorption Properties of Alginate–Soy Protein Composites

Polymers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1807
Author(s):  
Estefanía Álvarez-Castillo ◽  
José Manuel Aguilar ◽  
Carlos Bengoechea ◽  
María Luisa López-Castejón ◽  
Antonio Guerrero
Keyword(s):  
Soy Protein ◽  
Water Solubility ◽  
Divalent Cations ◽  
Low Cost ◽  
Soy Protein Isolate ◽  
Protein Isolate ◽  
Guluronic Acid ◽  
Wide Range ◽  
Anionic Polysaccharides ◽  
Porous Matrices

Composite materials based on proteins and carbohydrates normally offer improved water solubility, biodegradability, and biocompatibility, which make them attractive for a wide range of applications. Soy protein isolate (SPI) has shown superabsorbent properties that are useful in fields such as agriculture. Alginate salts (ALG) are linear anionic polysaccharides obtained at a low cost from brown algae, displaying a good enough biocompatibility to be considered for medical applications. As alginates are quite hydrophilic, the exchange of ions from guluronic acid present in its molecular structure with divalent cations, particularly Ca2+, may induce its gelation, which would inhibit its solubilization in water. Both biopolymers SPI and ALG were used to produce composites through injection moulding using glycerol (Gly) as a plasticizer. Different biopolymer/plasticizer ratios were employed, and the SPI/ALG ratio within the biopolymer fraction was also varied. Furthermore, composites were immersed in different CaCl2 solutions to inhibit the amount of soluble matter loss and to enhance the mechanical properties of the resulting porous matrices. The main goal of the present work was the development and characterization of green porous matrices with inhibited solubility thanks to the gelation of alginate.

scholarly journals Application of Dendrimers for Treating Parasitic Diseases

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 343
Author(s):  
Veronica Folliero ◽  
Carla Zannella ◽  
Annalisa Chianese ◽  
Debora Stelitano ◽  
Annalisa Ambrosino ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Water Solubility ◽  
Parasitic Infection ◽  
Three Dimensional ◽  
Medical Knowledge ◽  
High Ratio ◽  
Molecular Volume ◽  
Parasitic Infections ◽  
Parasitic Diseases ◽  
Wide Range

Despite advances in medical knowledge, parasitic diseases remain a significant global health burden and their pharmacological treatment is often hampered by drug toxicity. Therefore, drug delivery systems may provide useful advantages when used in combination with conventional therapeutic compounds. Dendrimers are three-dimensional polymeric structures, characterized by a central core, branches and terminal functional groups. These nanostructures are known for their defined structure, great water solubility, biocompatibility and high encapsulation ability against a wide range of molecules. Furthermore, the high ratio between terminal groups and molecular volume render them a hopeful vector for drug delivery. These nanostructures offer several advantages compared to conventional drugs for the treatment of parasitic infection. Dendrimers deliver drugs to target sites with reduced dosage, solving side effects that occur with accepted marketed drugs. In recent years, extensive progress has been made towards the use of dendrimers for therapeutic, prophylactic and diagnostic purposes for the management of parasitic infections. The present review highlights the potential of several dendrimers in the management of parasitic diseases.

scholarly journals Tamoxifen and oxidative stress: an overlooked connection

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Nermin S. Ahmed ◽  
Marek Samec ◽  
Alena Liskova ◽  
Peter Kubatka ◽  
Luciano Saso
Keyword(s):  
Breast Cancer ◽  
Oxidative Stress ◽  
Gold Standard ◽  
Pharmacological Activities ◽  
Standard Drug ◽  
Menopausal Women ◽  
Wide Range ◽  
Post Menopausal ◽  
Apoptotic Effects ◽  
And Oxidative Stress

AbstractTamoxifen is the gold standard drug for the treatment of breast cancer in pre and post-menopausal women. Its journey from a failing contraceptive to a blockbuster is an example of pharmaceutical innovation challenges. Tamoxifen has a wide range of pharmacological activities; a drug that was initially thought to work via a simple Estrogen receptor (ER) mechanism was proven to mediate its activity through several non-ER mechanisms. Here in we review the previous literature describing ER and non-ER targets of tamoxifen, we highlighted the overlooked connection between tamoxifen, tamoxifen apoptotic effects and oxidative stress.

Pharmacologic activities of 5, 6-Diaryl/heteroaryl-3-substituted-1, 2, 4-triazines as a privileged scaffold in drug development

2021 ◽  
Vol 21 ◽  
Author(s):  
Zahra Zakeri Khatir ◽  
Hamid Irannejad
Keyword(s):  
Biological Data ◽  
Pharmacological Activities ◽  
Drug Candidates ◽  
Structure Activity ◽  
Wide Range ◽  
Privileged Structure ◽  
Triazine Derivatives ◽  
Privileged Scaffold ◽  
Substituted 1 ◽  
Anti Hiv

: 1, 2, 4-Triazine derivatives have received much attention due to their multifunctional nature, especially in diverse pharmacological properties as well as a key fragment in many drug candidates. Introduction of a vicinal 5, 6-diaryl/heteroaryl moiety on the 1, 2, 4-triazine ring has attracted plentiful attention in the field of medicinal chemistry. 5, 6-Diaryl/heteroaryl-3-substituted-1, 2, 4-triazine is as a prominent scaffold in many drug candidates which has shown a wide range of pharmacological activities such as anti-diabetic, antifungal, anti-inflammatory, anticancer, anti-HIV, neuroprotective, anticonvulsant, anti- Alzheimer, anti-Parkinson and antioxidant. In this review, we have discussed synthesis, various pharmacological activities of 5, 6-diaryl/heteroaryl-3-substituted-1, 2, 4-triazines, their structure-activity relationship (SAR), pharmacophoric elements and their mechanism of action reported in the published articles during 2000-2019. Evaluation of compounds by PAINS filtering tool was accomplished and showed that this versatile structure could be considered as a privileged structure. Compilation of the biological data confirmed that the position 3 of the 1,2,4-triazine is a key location to determine the affinity and selectivity of the 5,6-diaryl/heteroaryl-3-substituted-1, 2, 4-triazines towards different biologic targets. Specific geometrical and thermodynamic characters of this motif have prompted it as a frequent hitter.

scholarly journals ETHNOBOTANICAL, PHYTOCHEMICAL, AND PHARMACOLOGICAL PROPERTIES OF NEPENTHES SPECIES: A REVIEW

2017 ◽  
Vol 10 (11) ◽  
pp. 16 ◽  
Author(s):  
Shuaibu Babaji Sanusi ◽  
Mohd Fadzelly Abu Bakar ◽  
Maryati Mohamed ◽  
Siti Fatimah Sabran ◽  
Muhammad Murtala Mainasara
Keyword(s):  
Folk Medicine ◽  
Therapeutic Agents ◽  
Bioactive Components ◽  
Pharmacological Activities ◽  
Crude Extracts ◽  
Gastrointestinal Discomfort ◽  
Wide Range ◽  
Long Time ◽  
Phytochemical Compounds ◽  
Ethnobotanical Uses

The genus Nepenthes (Nepenthaceae) has been utilized in folk medicine for a long time in India and Southeast Asia countries. They are used in the treatment of leprosy, cholera, night blindness, gastrointestinal discomfort, dysentery, stomachache, and bed-wetting among others. This review highlights the ethnobotanical uses, phytochemicals, and pharmacological activities of both crude extracts and pure bioactive compounds of Nepenthes spp. The phytochemical compounds isolated from Nepenthes species include flavonoids, terpenoids, tannins, alkaloids, and steroids among other phytochemicals. A wide range of pharmacological activities was exhibited by the crude extracts and pure bioactive components such as antibacterial, antifungal, antimalarial antioxidant, antidiabetic, antiosteoporotic, anti-inflammatory, cytotoxicity, and hypolipidemic activities. This review revealed that many active compounds are present in Nepenthes spp. However, many pharmacological screenings such as anticancer, antiviral, wound healing, antihelminthic, antidiarrheal properties, among others have not been carried out yet. Therefore, more biological investigations and phytochemical screenings are required to fully explore the genus Nepenthes which may lead to development of new therapeutic agents.  

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