scholarly journals Marine Alkaloids: Compounds with In Vivo Activity and Chemical Synthesis

Marine Drugs ◽  
2021 ◽  
Vol 19 (7) ◽  
pp. 374
Author(s):  
Paulo E. S. Munekata ◽  
Mirian Pateiro ◽  
Carlos A. Conte-Junior ◽  
Rubén Domínguez ◽  
Asad Nawaz ◽  
...  

Marine alkaloids comprise a class of compounds with several nitrogenated structures that can be explored as potential natural bioactive compounds. The scientific interest in these compounds has been increasing in the last decades, and many studies have been published elucidating their chemical structure and biological effects in vitro. Following this trend, the number of in vivo studies reporting the health-related properties of marine alkaloids has been increasing and providing more information about the effects in complex organisms. Experiments with animals, especially mice and zebrafish, are revealing the potential health benefits against cancer development, cardiovascular diseases, seizures, Alzheimer’s disease, mental health disorders, inflammatory diseases, osteoporosis, cystic fibrosis, oxidative stress, human parasites, and microbial infections in vivo. Although major efforts are still necessary to increase the knowledge, especially about the translation value of the information obtained from in vivo experiments to clinical trials, marine alkaloids are promising candidates for further experiments in drug development.

2016 ◽  
Vol 10 (2) ◽  
pp. 172-186
Author(s):  
Agus Sudibyo ◽  
Tiurlan F. Hutajulu

Morinda Citrifolia, L.  known as Noni or Mengkudu is planting belonging to the family of Rubiaceae. A number of major components have been identified in leaves, roots, fruits of Noni plant, such as scopoletin, octanoic acid, vitamin C, iridoid, terpenoids, alkaloids, anthraquinones, beta-sitosterol, carotene, vitamin A, flavone glycosides, alizarin, amino acids, acubin, austin, caproic acid, caprylic acid and putative procyonine. Its use as a botanical dietary supplement has grown tremendously in recent years. The results of epidemiological studies suggest that the Noni consumption may help prevent several chronic diseases, including cancer disease, cardiovascular disease, type 2 diabetes mellitus, heart disease, artherosclerosis, blood vessel problem, gastric ulcer, drug addiction, muscle ached and pein. Several studies have also demonstrated anti-inflammatory, antioxidant, antimicrobial, analgesic, and immunologicalactivity. Based on a toxicological assessment, Noni juice was considered as safe. Although, a large number of in vitro and to a certain extent, and in vivo studies demonstrated a range potentially beneficial effects, clinical information data are still lacking completely. Therefore, to what extent the information findings from experimental pharmacological studies is not complete at present, so this article reviews potential health benefits for consumptions, its biological effects and looking for a new informationthat needs to be explored in detail before a recommendation can be madeABSTRAKMorinda citrofolia, L (mengkudu) merupakan jenis tanaman yang termasuk dalam golongan Rubiaceadan buahnya dikenal dengan nama Noni atau mengkudu. Beberapa komponen utama dalam tanaman tersebut telah diidentifikasi, mulai dari bagian akar, daun, dan buah, seperti kandungan scopoletin, asam oktanoad, vitamin C, iridoid, terpenoid, alkaloid, anthraquinon, beta-sitosterol, karotene, vitamin A, flavon glikosida, alizarin, asam amino, acubin, austin, asam kaproat, asam kaprilat dan putativ prokseronin. Buah tersebut akhir-akhir ini telah sukses banyak dimanfaatkan sebagai diet suplemen. Hasil studi secara epidemiologi menyatakan bahwa konsumsi mengkudu dapat membantu mencegah beberapa penyakit kronis, seperti penyakit kanker, kardiovaskular, diabetes tipe 2, penyakit jantung, artherosklerosis, masalah pembuluh darah, pencernaan, dan sakit otot. Beberapa studi juga menunjukkan bahwa mengkudu dapat berfungsi sebagai anti inflamasi, antioksidan, antimikroba, analgesik, dan bersifat immunlogis.Berdasarkan kajian secara toksikologi, buah dan jus mengkudu dinyatakan aman untuk dikonsumsi.  Penelitian secara in vitro pada beberapa jenis penyakit tertentu sedang diperluas, dan penelitian secara in vivo menunjukkan bahwa mengkudu mempunyai rentang potensi pengaruh yang baik bagi kesehatan, meskipun data informasinya secara klinis kurang lengkap. Oleh karena itu, untuk mengetahui apa yang sudah ditemukan dari hasil penelitian secara farmalogis yang belum lengkapsaat ini, maka dalam tulisan ini membahas potensi keuntungan kesehatan bila dikonsumsi, pengaruh biologinya dan pencarian informasibaru yang  perlu dikaji lebih rinci sebelum rekomendasi ditetapkan.Kata kunci: Mengkudu (Morinda citrifolia, L), pangan fungsional, rempah medis. 


Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1615
Author(s):  
Abraham J. Domb ◽  
Ghorbanali Sharifzadeh ◽  
Victoria Nahum ◽  
Hossein Hosseinkhani

Nanomaterials are now being used in a wide variety of biomedical applications. Medical and health-related issues, however, have raised major concerns, in view of the potential risks of these materials against tissue, cells, and/or organs and these are still poorly understood. These particles are able to interact with the body in countless ways, and they can cause unexpected and hazardous toxicities, especially at cellular levels. Therefore, undertaking in vitro and in vivo experiments is vital to establish their toxicity with natural tissues. In this review, we discuss the underlying mechanisms of nanotoxicity and provide an overview on in vitro characterizations and cytotoxicity assays, as well as in vivo studies that emphasize blood circulation and the in vivo fate of nanomaterials. Our focus is on understanding the role that the physicochemical properties of nanomaterials play in determining their toxicity.


2019 ◽  
Vol 65 (5) ◽  
pp. 760-765
Author(s):  
Margarita Tyndyk ◽  
Irina Popovich ◽  
A. Malek ◽  
R. Samsonov ◽  
N. Germanov ◽  
...  

The paper presents the results of the research on the antitumor activity of a new drug - atomic clusters of silver (ACS), the colloidal solution of nanostructured silver bisilicate Ag6Si2O7 with particles size of 1-2 nm in deionized water. In vitro studies to evaluate the effect of various ACS concentrations in human tumor cells cultures (breast cancer, colon carcinoma and prostate cancer) were conducted. The highest antitumor activity of ACS was observed in dilutions from 2.7 mg/l to 5.1 mg/l, resulting in the death of tumor cells in all studied cell cultures. In vivo experiments on transplanted Ehrlich carcinoma model in mice consuming 0.75 mg/kg ACS with drinking water revealed significant inhibition of tumor growth since the 14th day of experiment (maximally by 52% on the 28th day, p < 0.05) in comparison with control. Subcutaneous injections of 2.5 mg/kg ACS inhibited Ehrlich's tumor growth on the 7th and 10th days of the experiment (p < 0.05) as compared to control.


Chemosphere ◽  
2021 ◽  
pp. 130826
Author(s):  
Anabel González-Acedo ◽  
Enrique García-Recio ◽  
Rebeca Illescas-Montes ◽  
Javier Ramos-Torrecillas ◽  
Lucía Melguizo-Rodríguez ◽  
...  

Author(s):  
Bogna Grygiel-Górniak

AbstractThe majority of the medical fraternity is continuously involved in finding new therapeutic schemes, including antimalarial medications (AMDs), which can be useful in combating the 2019-nCoV: coronavirus disease (COVID-19). For many decades, AMDs have been widely used in the treatment of malaria and various other anti-inflammatory diseases, particularly to treat autoimmune disorders of the connective tissue. The review comprises in vitro and in vivo studies, original studies, clinical trials, and consensus reports for the analysis, which were available in medical databases (e.g., PubMed). This manuscript summarizes the current knowledge about chloroquine (CQ)/hydroxychloroquine (HCQ) and shows the difference between their use, activity, recommendation, doses, and adverse effects on two groups of patients: those with rheumatic and viral diseases (including COVID-19). In the case of connective tissue disorders, AMDs are prescribed for a prolonged duration in small doses, and their effect is observed after few weeks, whereas in the case of viral infections, they are prescribed in larger doses for a short duration to achieve a quick saturation effect. In rheumatic diseases, AMDs are well tolerated, and their side effects are rare. However, in some viral diseases, the effect of AMDs is questionable or not so noticeable as suggested during the initial prognosis. They are mainly used as an additive therapy to antiviral drugs, but recent studies have shown that AMDs can diminish the efficacy of some antiviral drugs and may cause respiratory, kidney, liver, and cardiac complications.


2021 ◽  
Vol 11 (5) ◽  
pp. 336
Author(s):  
Mohammed Ghiboub ◽  
Ahmed M. I. Elfiky ◽  
Menno P. J. de Winther ◽  
Nicola R. Harker ◽  
David F. Tough ◽  
...  

Histone deacetylases (HDACs) and bromodomain-containing proteins (BCPs) play a key role in chromatin remodeling. Based on their ability to regulate inducible gene expression in the context of inflammation and cancer, HDACs and BCPs have been the focus of drug discovery efforts, and numerous small-molecule inhibitors have been developed. However, dose-limiting toxicities of the first generation of inhibitors, which typically target multiple HDACs or BCPs, have limited translation to the clinic. Over the last decade, an increasing effort has been dedicated to designing class-, isoform-, or domain-specific HDAC or BCP inhibitors, as well as developing strategies for cell-specific targeted drug delivery. Selective inhibition of the epigenetic modulators is helping to elucidate the functions of individual epigenetic proteins and has the potential to yield better and safer therapeutic strategies. In accordance with this idea, several in vitro and in vivo studies have reported the ability of more selective HDAC/BCP inhibitors to recapitulate the beneficial effects of pan-inhibitors with less unwanted adverse events. In this review, we summarize the most recent advances with these strategies, discussing advantages and limitations of these approaches as well as some therapeutic perspectives, focusing on autoimmune and inflammatory diseases.


2021 ◽  
Vol 18 ◽  
Author(s):  
Subheet Kumar Jain ◽  
Neha Panchal ◽  
Amrinder Singh ◽  
Shubham Thakur ◽  
Navid Reza Shahtaghi ◽  
...  

Background: Diclofenac sodium (DS) injection is widely used in the management of acute or chronic pain and inflammatory diseases. It incorporates 20 % w/v Transcutol-P as a solubilizer to make the stable injectable formulation. However, the use of Transcutol-P in high concentration leads to adverse effects such as severe nephrotoxicity, etc. Some advancements resulted in the formulation of an aqueous based injectable but that too used benzyl alcohol reported to be toxic for human use. Objective: To develop an injectable self-micro emulsifying drug delivery system (SMEDDS) as a novel carrier of DS for prompt release with better safety and efficacy. Methods: A solubility study was performed with different surfactants and co-surfactants. The conventional stirring method was employed for the formulation of SMEDDS. Detailed in vitro characterization was done for different quality control parameters. In vivo studies were performed using Wistar rats for pharmacokinetic evaluation, toxicological analysis, and analgesic activity. Results: The optimized formulation exhibited good physical stability, ideal globule size (156±0.4 nm), quick release, better therapeutics, and safety, increase in LD50 (221.9 mg/kg) to that of the commercial counterpart (109.9 mg/kg). Further, pre-treatment with optimized formulation reduced the carrageenan-induced rat paw oedema by 88±1.2 % after 4 h, compared to 77±1.6 % inhibition with commercial DS formulation. Moreover, optimized formulation significantly (p<0.05) inhibited the pain sensation in the acetic-acid induced writhing test in mice compared to its commercial equivalent with a better pharmacokinetic profile. Conclusion: The above findings confirmed that liquid SMEDDS could be a successful carrier for the safe and effective delivery of DS


Cells ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 3088
Author(s):  
Mariana Matias ◽  
Jacinta O. Pinho ◽  
Maria João Penetra ◽  
Gonçalo Campos ◽  
Catarina Pinto Reis ◽  
...  

Melanoma is recognized as the most dangerous type of skin cancer, with high mortality and resistance to currently used treatments. To overcome the limitations of the available therapeutic options, the discovery and development of new, more effective, and safer therapies is required. In this review, the different research steps involved in the process of antimelanoma drug evaluation and selection are explored, including information regarding in silico, in vitro, and in vivo experiments, as well as clinical trial phases. Details are given about the most used cell lines and assays to perform both two- and three-dimensional in vitro screening of drug candidates towards melanoma. For in vivo studies, murine models are, undoubtedly, the most widely used for assessing the therapeutic potential of new compounds and to study the underlying mechanisms of action. Here, the main melanoma murine models are described as well as other animal species. A section is dedicated to ongoing clinical studies, demonstrating the wide interest and successful efforts devoted to melanoma therapy, in particular at advanced stages of the disease, and a final section includes some considerations regarding approval for marketing by regulatory agencies. Overall, considerable commitment is being directed to the continuous development of optimized experimental models, important for the understanding of melanoma biology and for the evaluation and validation of novel therapeutic strategies.


2019 ◽  
Vol 25 (16) ◽  
pp. 1817-1827 ◽  
Author(s):  
Vesna Vučić ◽  
Milkica Grabež ◽  
Armen Trchounian ◽  
Aleksandra Arsić

Background:: Pomegranate (Punica granatum L.) fruits are widely consumed and used as preventive and therapeutic agents since ancient times. Pomegranate is a rich source of a variety of phytochemicals, which are responsible for its strong antioxidative and anti-inflammatory potential. Objective:: The aim of this review is to provide an up-to-date overview of the current knowledge of chemical structure and potential health benefits of pomegranate. Method: : A comprehensive search of available literature. Results:: The review of the literature confirms that juice and extracts obtained from different parts of this plant, including fruit peel, seeds, and leaves exert health benefits in both in vitro and in vivo studies. The antidiabetic, antihypertensive, antimicrobial and anti-tumour effects of pomegranate fruit are of particular scientific and clinical interest. Conclusion:: Further investigations are required to clarify the mechanism of action of the bioactive ingredients and to reveal full potential of pomegranate as both preventive and therapeutic agent.


2020 ◽  
Vol 18 (1) ◽  
pp. 2-14 ◽  
Author(s):  
Aida Doostkam ◽  
Kamyar Iravani ◽  
Shahindokht Bassiri-Jahromi

: Polyphenols have received high attention due to their biological functions. Pomegranate (Punica granatum L.) is a rich source of polyphenols such as tannin, ellagitannin, flavonoids and other phenolic acids. The potential therapeutic uses of pomegranate appear to be wide diversity. Pomegranate contains strong antioxidant activity, and antimicrobial properties, with potential health interests. : This review has been performed on a method of systematic narrative review on the antimicrobial potency of different parts of pomegranate. A search was performed in PubMed, Web of Science, Science Direct, Scopus and Google Scholar from 1986 to 2018 to obtain related studies. The aim of this review present an overview of the aspect and advantages of Punica granatum L. and summarize the present data on the pomegranate anti-microbial activity in in-vitro and in-vivo tests, animal trial systems and human clinical trials. Also, this review discussed the pomegranate extracts activities and their future application. : The findings of this review support that the pomegranate might be possible to use in the control and potential therapeutics of some microbial infections. This review highlights the new researches on the anti-microbial activities of pomegranate.


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