Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

This review aims to provide an overview of studies that address the use, in therapeutic applications, of solid dispersions (SDs) with biological activities in vitro and/or in vivo mainly made up of polymeric matrices, as well as to evaluate the bioactive activity of their constituents. This bibliographic survey shows that the development of solid dispersions provides benefits in the physicochemical properties of bioactive compounds, which lead to an increase in their biological potential. However, despite the reports found on solid dispersions, there is still a need for biological assay-based studies, mainly in vivo, to assist in the investigation and to devise new applications. Therefore, studies based on such an approach are of great importance to enhance and extend the use of solid dispersions in the most diverse therapeutic applications.

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Extraction of bioactive compounds from Curcuma longa L. using deep eutectic solvents: In vitro and in vivo biological activities

Innovative Food Science & Emerging Technologies ◽

10.1016/j.ifset.2021.102697 ◽

2021 ◽

pp. 102697

Author(s):

Grazielle Oliveira ◽

Caroline Marques ◽

Anielle de Oliveira ◽

Amanda de Almeida dos Santos ◽

Wanderlei do Amaral ◽

...

Keyword(s):

Bioactive Compounds ◽

Biological Activities ◽

Curcuma Longa ◽

Deep Eutectic Solvents

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Anti-Inflammatory and Antinociceptive Activity of Pollen Extract Collected by Stingless Bee Melipona fasciculata

International Journal of Molecular Sciences ◽

10.3390/ijms20184512 ◽

2019 ◽

Vol 20 (18) ◽

pp. 4512 ◽

Cited By ~ 8

Author(s):

Alberto Jorge Oliveira Lopes ◽

Cleydlenne Costa Vasconcelos ◽

Francisco Assis Nascimento Pereira ◽

Rosa Helena Moraes Silva ◽

Pedro Felipe dos Santos Queiroz ◽

...

Keyword(s):

Native Species ◽

Biological Activities ◽

Stingless Bee ◽

In Vitro Assays ◽

Pollen Extract ◽

Biological Potential ◽

Anti Inflammatory ◽

Analgesic Activities

The stingless bee, Melipona fasciculata Smith (Apidae, Meliponini), is a native species from Brazil. Their products have high biotechnological potential, however there are no studies about the biological activities of pollen collected by M. fasciculata. In this context, the present study investigated the chemical composition, anti-oxidant, anti-inflammatory, and analgesic activities of hydroethanolic pollen extracts collected by M. fasciculata in three cities in Maranhão State, Brazil. We verified the antioxidant activity of the extracts and inhibitory activity against the cyclooxygenase enzyme using in vitro assays and in allowed to select the extract with higher efficiency to be used on in vivo assays. In these trials, the selected extract showed high anti-inflammatory activity as well as nociceptive effects at central and peripheral level, suggesting that this extract acts on inhibition of histamine release and decreased synthesis of prostaglandins and the in-silico study suggested that polyphenols and acids fatty acids in the extract may be associated with these activities. The results of the present study report the high biological potential of pollen extract and we conclude that the pollen collected by M. fasciculata can be considered as the object of research for new pharmacological alternatives.

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Characterization of Andean Blueberry in Bioactive Compounds, Evaluation of Biological Properties and in vitro Bioaccessibility

10.20944/preprints202009.0055.v1 ◽

2020 ◽

Author(s):

Nieves Baenas ◽

Jenny Ruales ◽

Diego A. Moreno ◽

Daniel Alejandro Barrio ◽

Carla M. Stinco ◽

...

Keyword(s):

Antioxidant Capacity ◽

Bioactive Compounds ◽

Biological Activities ◽

In Vitro Digestion ◽

Biological Properties ◽

Wide Range ◽

Zebrafish Embryogenesis

Andean blueberries are wild berries grown and consumed in Ecuador which contain high values of bioactive compounds, mainly anthocyanins, with powerful antioxidant activity. The aim of this study was to evaluate the profile and contents of (poly)phenols and carotenoids in Andean blueberry by HPLC-DAD-MSn and determine a wide range of its biological activities. The antioxidant capacity of this fruit was evaluated in vitro by three different methods and in vivo using the zebrafish animal model, also the toxicity effect was determined by the zebrafish embryogenesis test. Besides, the antimicrobial activity and the capacity of Andean blueberry to produce hemagglutination in blood cells were evaluated. Finally, the bioaccessibility of (poly)phenols and related antioxidant capacity were determined in the different phases of an in vitro digestion. The global results indicated no toxicity of Andean blueberry, weakly bacteriostatic activity, and high contents of anthocyanins and antioxidant capacity, which were partially bioaccesible in vitro (~ 50 % at the final intestinal step), contributing to the knowledge of its health benefits for consumers and its potential use in the food and pharmaceutical industry as functional ingredient.

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Ethnopharmacology, Phytochemistry, and Pharmacological Properties of Thymus satureioides Coss.

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2021/6673838 ◽

2021 ◽

Vol 2021 ◽

pp. 1-23

Author(s):

Naoufal El Hachlafi ◽

Abderrahim Chebat ◽

Kawtar Fikri-Benbrahim

Keyword(s):

Essential Oils ◽

Bioactive Compounds ◽

Biological Activities ◽

Chemical Characterization ◽

Pharmacokinetic Studies ◽

Pharmacological Studies ◽

Thymus Satureioides

Thymus satureioides Coss. (Lamiaceae) is a Moroccan medicinal plant locally known as “Azkouni” or “Zaitra.” It is widely used in traditional medicine to treat various ailments, including hypertension, diabetes, cold, fever, dermatological and circulatory disorders, immune problems, bronchitis, nociception, cooling, pharyngitis, cough, and influenza. The current review aims to critically summarize the literature on ethnopharmacological uses, chemical profile, and pharmacological investigations of T. satureioides in order to provide data support and scientific evidences for further investigations. Electronic databases such as Scopus, PubMed, Web of Science, SciFinder, ScienceDirect, Google Scholar, and Medline were used to gather data on T. satureioides. Chemical characterization of T. satureioides essential oils (EOs) and extracts allowed to identify a total of 139 bioactive compounds, mainly belonging to the terpenoids, phenolic acids, and flavonoids classes. T. satureioides especially its essential oils exhibited numerous biological activities such as antibacterial, antifungal, anti-inflammatory, antioxidant, antidiabetic, anticancer, antiparasitic, and hypolipedemic activities. In light of these findings, further studies to transmute the traditional application of T. satureioides into scientific-based information are strongly required. Additional in vivo pharmacological studies are recommended to validate the results of the in vitro studies. Moreover, comprehensive preclinical and clinical trials on the pharmacological mechanisms of action of this plant and its bioactive compounds on molecular targets should be performed. Finally, more efforts must be focused on toxicological assessments and pharmacokinetic studies, in order to ensure the safety and the efficiency of T. satureioides.

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Ethnomedicinal Use, Phytochemistry, Pharmacology, and Toxicology of Salvia verbenaca L. : A Review

Biointerface Research in Applied Chemistry ◽

10.33263/briac122.14371469 ◽

2021 ◽

Vol 12 (2) ◽

pp. 1437-1469

Keyword(s):

Essential Oils ◽

Bioactive Compounds ◽

Biological Activities ◽

Traditional Use ◽

Toxicological Effects ◽

Stomach Pain ◽

Toxicological Investigation ◽

Phytochemical Compounds

Salvia verbenaca L. is a Mediterranean medicinal plant used traditionally to treat several diseases such as burns, ocular wounds, contusion, stomach pain, eye diseases, dermal inflammation. This review highlighted previous reports, including the botanical, taxonomical, geographical distribution, traditional use, phytochemical, biological, and toxicological effects of S. verbenaca. The data were gathered from scientific databases PubMed, Scopus, Web of Science, Google Scholar, ScienceDirect, SpringerLink. The presented data on S. verbenaca were organized according to ethnomedicinal use, bioactive compounds, pharmacology, and toxicological investigation. Ethnobotanical studies reported that many folk medicines use S. verbenaca, especially against wounds, burns, and cicatrization. The phytochemical compounds in different parts of S. verbenaca belonged to different classes of chemical compounds, including terpenoids, flavonoids, phenolic acids, phenolic diterpenoids, and fatty acids. The extracts and essential oils from S. verbenaca have a wide variety of in vitro and in vivo pharmacological activities, i.e., antioxidant, antifungal, antidiabetic, anti-inflammatory, antitumor, antihemolytic, antihypertensive, antileishmanial, and immunomodulatory activities. This research suggests that the biological activities of S. verbenaca prove its traditional uses. However, in-depth investigations are required, such as pharmacokinetic, pharmacodynamic, and toxicological experiments, to prove the efficacy and safety of S. verbenaca extracts and essential oils and their bioactive compounds.

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Phytochemicals with Added Value from Morella and Myrica Species

Molecules ◽

10.3390/molecules25246052 ◽

2020 ◽

Vol 25 (24) ◽

pp. 6052

Author(s):

Gonçalo P. Rosa ◽

Bruno J. C. Silva ◽

Ana M. L. Seca ◽

Laila M. Moujir ◽

Maria Carmo Barreto

Keyword(s):

Traditional Medicine ◽

Skin Diseases ◽

Biological Activities ◽

Folk Medicine ◽

Added Value ◽

Terrestrial Plants ◽

New Applications ◽

Different Parts

Terrestrial plants, due to their sessile nature, are highly exposed to environmental pressure and therefore need to produce very effective molecules that enable them to survive all the threats. Myrica and Morella (Myricaceae) are taxonomically close genera, which include species of trees or shrubs with edible fruits that exhibit relevant uses in traditional medicine. For instance, in Chinese or Japanese folk medicine, they are used to treat diarrhea, digestive problems, headache, burns, and skin diseases. A wide array of compounds isolated from different parts of Myrica and/or Morella species possess several biological activities, like anticancer, antidiabetic, anti-obesity, and cardio-/neuro-/hepatoprotective activities, both in vitro and in vivo, with myricanol, myricitrin, quercitrin, and betulin being the most promising. There are still many other compounds isolated from both genera whose biological activities have not been evaluated, which represents an excellent opportunity to discover new applications for those compounds and valorize Morella/Myrica species.

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Bioactive Compounds and Biological Activities of Sorghum Grains

Foods ◽

10.3390/foods10112868 ◽

2021 ◽

Vol 10 (11) ◽

pp. 2868

Author(s):

Zhenhua Li ◽

Xiaoyan Zhao ◽

Xiaowei Zhang ◽

Hongkai Liu

Keyword(s):

Clinical Trials ◽

Phenolic Compounds ◽

Bioactive Compounds ◽

Biological Activities ◽

In Vivo Studies ◽

Detection Technology ◽

Sorghum Grains ◽

Bound Phenolics

Sorghum is the fifth most commonly used cereal worldwide and is a rich source of many bioactive compounds. We summarized phenolic compounds and carotenoids, vitamin E, amines, and phytosterols in sorghum grains. Recently, with the development of detection technology, new bioactive compounds such as formononetin, glycitein, and ononin have been detected. In addition, multiple in vitro and in vivo studies have shown that sorghum grains have extensive bio-logical activities, such as antioxidative, anticancer, antidiabetic, antiinflammatory, and antiobesity properties. Finally, with the establishment of sorghum phenolic compounds database, the bound phenolics and their biological activities and the mechanisms of biological activities of sorghum bioactive compounds using clinical trials may be researched.

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Anti-Obesity and Anti-Diabetic Effects of Ishige okamurae

Marine Drugs ◽

10.3390/md17040202 ◽

2019 ◽

Vol 17 (4) ◽

pp. 202 ◽

Cited By ~ 6

Author(s):

Hye-Won Yang ◽

K.H.N. Fernando ◽

Jae-Young Oh ◽

Xining Li ◽

You-Jin Jeon ◽

...

Keyword(s):

Bioactive Compounds ◽

Biological Activities ◽

Therapeutic Effects ◽

Cellular Mechanisms ◽

Ishige Okamurae ◽

Obesity And Diabetes ◽

Health Complications ◽

Nutritional Benefits

Obesity is associated with several health complications and can lead to the development of metabolic syndrome. Some of its deleterious consequences are related to insulin resistance, which adversely affects blood glucose regulation. At present, there is a growing concern regarding healthy food consumption, owing to awareness about obesity. Seaweeds are well-known for their nutritional benefits. The brown alga Ishige okamurae (IO) has been studied as a dietary supplement and exhibits various biological activities in vitro and in vivo. The bioactive compounds isolated from IO extract are known to possess anti-obesity and anti-diabetic properties, elicited via the regulation of lipid metabolism and glucose homeostasis. This review focuses on IO extract and its bioactive compounds that exhibit therapeutic effects through several cellular mechanisms in obesity and diabetes. The information discussed in the present review may provide evidence to develop nutraceuticals from IO.

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Peganum spp.: A Comprehensive Review on Bioactivities and Health-Enhancing Effects and Their Potential for the Formulation of Functional Foods and Pharmaceutical Drugs

Oxidative Medicine and Cellular Longevity ◽

10.1155/2021/5900422 ◽

2021 ◽

Vol 2021 ◽

pp. 1-20

Author(s):

Javad Sharifi-Rad ◽

Cristina Quispe ◽

Jesús Herrera-Bravo ◽

Prabhakar Semwal ◽

Sakshi Painuli ◽

...

Keyword(s):

Adverse Effects ◽

Bioactive Compounds ◽

Functional Foods ◽

Biological Activities ◽

Potential Candidate ◽

Pharmaceutical Drugs ◽

Phytochemical Profile ◽

The Mediterranean

The genus Peganum includes four species widely distributed in warm temperate to subtropical regions from the Mediterranean to Mongolia as well as certain regions in America. Among these species, Peganum harmala L., distributed from the Mediterranean region to Central Asia, has been studied and its phytochemical profile, traditional folk use, and application in pharmacological and clinical trials are well known. The review is aimed at presenting an insight into the botanical features and geographical distribution of Peganum spp. along with traditional folk uses. This manuscript also reviews the phytochemical profile of Peganum spp. and its correlation with biological activities evidenced by the in vitro and in vivo investigations. Moreover, this review gives us an understanding of the bioactive compounds from Peganum as health promoters followed by the safety and adverse effects on human health. In relation to their multipurpose therapeutic properties, various parts of this plant such as seeds, bark, and roots present bioactive compounds promoting health benefits. An updated search (until December 2020) was carried out in databases such as PubMed and ScienceDirect. Chemical studies have presented beta-carboline alkaloids as the most active constituents, with harmalol, harmaline, and harmine being the latest and most studied among these naturally occurring alkaloids. The Peganum spp. extracts have shown neuroprotective, anticancer, antimicrobial, and antiviral effects. The extracts are also found effective in improving respiratory disorders (asthma and cough conditions), dermatoses, and knee osteoarthritis. Bioactivities and health-enhancing effects of Peganum spp. make it a potential candidate for the formulation of functional foods and pharmaceutical drugs. Nevertheless, adverse effects of this plant have also been described, and therefore new bioproducts need to be studied in depth. In fact, the design of new formulations and nanoformulations to control the release of active compounds will be necessary to achieve successful pharmacological and therapeutic treatments.

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Calixarenes (CAs) are promising in biomedicine, biosensing, bioimaging and gene delivery systems

10.31219/osf.io/n9vjy ◽

2021 ◽

Author(s):

Moataz Dowaidar

Keyword(s):

Gene Delivery ◽

Supramolecular Chemistry ◽

Biological Activities ◽

Molecular Structures ◽

Biological Applications ◽

Ongoing Research ◽

Biological Potential ◽

Wide Range

Calixarenes (CAs) are widely employed in biomedicine, e.g. biosensing and bioimaging, and contributed to in vivo and in vitro diagnostics. CAs were also employed to construct medication and gene delivery devices that helped create targeted treatments. CAs' ability to inhibit antibacterial, antiviral, anticancer, detoxifying, and amyloid fibrillation also aids in the development of macrocyclic therapies.Because of their ease of modification, CAs' rich (supramolecular) chemistry and their extensive chemical design space benefit such a wide range of medicinal applications. CAs' supramolecular chemistry permits studying biological functions. CAs have unique recognition properties as its cavity can identify and quench many dyes' fluorescence and photoactivity, making them excellent for turn-on fluorescence sensing, imaging, and activatable PDT. CA skeleton may also be utilized as a podand-like ligand to develop novel recognition systems. CAs are also skilled at assembling things. While these early investigations highlighted the biological potential of CA homologues for biosensing, bioimaging, drug/gene delivery, and therapy, there are currently few examples of clinical CA application. CAs' bench-to-bedside translation in biological applications is highly demanded. One CA is undertaking a phase I clinical study, a good indicator. However, from both scientific research and clinical trials, CAs still confront significant practical hurdles in biological applications. To make biosensing applications practicable in clinical settings, sensing systems need to be further developed into sensors or even in-vitro diagnostic kits. In vivo diagnosis and therapy More CA safety investigations including long-term toxicity effects, metabolic pathways, and immune reactions are needed. Some advanced modalities can be employed and explored to improve diagnostic and therapeutic performance, such as multimodal imaging, multiple targeting, and combination therapy. Moreover, despite the huge number of CA derivatives described, their physicochemical features and biological roles remain unclear. Exploring the novel functionalities of existing CAs is crucial, taking the combined efforts of diverse specialists from the domains of supramolecular chemistry, chemical biology, life sciences, pharmacy, and medicine. We believe that ancient molecules can still be employed for various new tricks. This can summarize the underlying link between molecular structures and biological activities to assist drive the creation of novel CA derivatives. We anticipate that CA-based biomedicine will deliver considerable benefits in the near future with ongoing research and development.

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