bioactive metabolite
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2022 ◽  
Vol 12 ◽  
Author(s):  
Zi-Liang Guo ◽  
Mao-Xing Li ◽  
Xiao-Lin Li ◽  
Peng Wang ◽  
Wei-Gang Wang ◽  
...  

Crocetin is an aglycone of crocin naturally occurring in saffron and produced in biological systems by hydrolysis of crocin as a bioactive metabolite. It is known to exist in several medicinal plants, the desiccative ripe fruit of the cape jasmine belonging to the Rubiaceae family, and stigmas of the saffron plant of the Iridaceae family. According to modern pharmacological investigations, crocetin possesses cardioprotective, hepatoprotective, neuroprotective, antidepressant, antiviral, anticancer, atherosclerotic, antidiabetic, and memory-enhancing properties. Although poor bioavailability hinders therapeutic applications, derivatization and formulation preparation technologies have broadened the application prospects for crocetin. To promote the research and development of crocetin, we summarized the distribution, preparation and production, total synthesis and derivatization technology, pharmacological activity, pharmacokinetics, drug safety, drug formulations, and preparation of crocetin.


Bionatura ◽  
2021 ◽  
Vol 6 (4) ◽  
pp. 2187-2192
Author(s):  
Rashid Rahim Hateet ◽  
Zainab Alag Hassan ◽  
Abdulameer Abdullah Al-Mussawi ◽  
Shaima Rabeea Banoon

The present study aimed to optimize cultural conditions for optimum bioactive metabolite production by endophytic fungus Trichoderma harzianum, isolated by surface sterilization method from the leaf of the eucalyptus plant. The fungus was identified based on morphological characterization. Fungal metabolites were carried out by ethyl acetate solvent. The antibacterial activity was tested against Escherichia coli (ATCC 25922) and Staphylococcus aureus (NCTC 6571). Various carbon, nitrogen sources, pH, temperature, incubation period, and NaCl on the antibacterial metabolite production were studied. Bioactive metabolite production of T. harzianum exhibits a broad spectrum of in vitro antibacterial activity against two strains of bacteria. For the optimum production of bioactive metabolites, Dextrose and Glucose were found to be the best sources of carbon and the best sources of Nitrogen Yeast extract (YE) and (NH4)2SO. The maximum production of bioactive metabolites occurs at pH 7 and 25°C.; the NaCl showed a positive influence on bioactive metabolites.


2021 ◽  
pp. 114552
Author(s):  
Sabrin R.M. Ibrahim ◽  
Ahmed E. Altyar ◽  
Ikhlas A. Sindi ◽  
Dina S. El-Agamy ◽  
Hossam M. Abdallah ◽  
...  

Medicine ◽  
2021 ◽  
Vol 100 (27) ◽  
pp. e26601
Author(s):  
Sanjib Kumar Panda ◽  
Somashekara Nirvanashetty ◽  
M. Missamma ◽  
Shavon Jackson-Michel
Keyword(s):  

2021 ◽  
Vol 21 (17) ◽  
pp. 1517-1518
Author(s):  
Dharmendra Kumar Yadav

The discovery and utilization of novel metabolites from natural sources are gaining momentum in the present era. The drug discovery programs have witnessed a remarkable shift from conventional medicines to exploiting natural products and their “value addition”, for treating lifethreatening diseases. The global outbreak of life-threatening diseases namely Ebola, SARS,including infections of the bloodstream (bacteremia), heart valves (endocarditis), lungs (pneumonia), and brain (meningitis) and AIDS calls for a more targeted approach to effectively combat the emerging diseases. In the present scenario, natural products and their extracts are being explored extensively for the treatment of various life threatening diseases. In this thematic issue, several review articles contributed by the scientist and researchers in the different areas of medicinal chemistry, synthetic chemistry, new emerging multi-drug targets were collected. This issue begins with a review article on the “Chemistry and Pharmacology of Natural Catechins from Camellia sinensis as anti-MRSA agents” by Gaur et al. and focuses on the spread of MRSA strains is of great concern because of limited treatment options for staphylococcal infections, since these strains are resistant to the entire class of β-lactam antibiotics. In addition, MRSA exhibits resistance to other classes of antimicrobial agents such as fluoroquinolones, cephalosporins, aminoglycosides, macrolide and even glycopeptides (vancomycin and teicoplanine), leading to the emergence of resistant strains such as glycopeptide intermediate (GISA) and resistant strain (GRSA) of S. aureus. In this review, chemical constituents responsible for the anti-MRSA activity of tea are explored [1]. The next article of this issue is a review article on the “Recent Advancements in the Synthesis and Chemistry of Benzofused Nitrogen- and Oxygen-based Bioactive Heterocycles” by Sharma et al. which focuses on medicinal importance of these bioactive benzo-fused heterocycles; special attention has been given to their synthesis as well as medicinal/pharmaceutical properties in detail [2]. “Trends in pharmaceutical design of Endophytes as anti-infective,” by Tiwari et al., is the third article in this issue. The review focused on the meta-analysis of bioactive metabolite production from endophytes, extensively discussing the bioprospection of natural products for pharmaceutical applications. In light of the emerging importance of endophytes as antiinfective agents, an exploration of the pharmaceutical design of novel chemical entities and analogues has enabled efficient and cost-effective drug discovery programs. However, bottlenecks in endophytic biology and research requires a better understanding of endophytic dynamics and mechanism of bioactive metabolite production towards a sustainable drug discovery program [3]. The last article of this issue is also research article on “Recent development of tetrahydro-quinoline/isoquinoline based compounds as anticancer agents” by Yadav et al. The article reported the synthesis of potent tetrahydroquinoline/isoquinoline molecules of the last 10 years with their anticancer properties in various cancer cell lines and stated their half-maximal inhibitory concentration (IC50). In addition, we also considered the discussion of molecular docking and structural activity relationship wherever provided to understand the possible mode of activity an target involved and structural features responsible for the better activity, so the reader can directly find detail for designing new anticancer agents. [4]. Finally I would like to thank all authors who contributed to this issue, titled “Recent advances on small molecule medicinal chemistry to treat human diseases”.


2021 ◽  
Vol 235 ◽  
pp. 105837
Author(s):  
Anna Huang ◽  
Nico W. van den Brink ◽  
Laura Buijse ◽  
Ivo Roessink ◽  
Paul J. van den Brink

Energies ◽  
2021 ◽  
Vol 14 (11) ◽  
pp. 3092
Author(s):  
Rasha El-Shafei ◽  
Hala Hegazy ◽  
Bishnu Acharya

Non-conventional extraction of bioactive metabolites could provide sustainable alternative techniques to preserve the potency of antioxidants and antiviral compounds extracted from macro-algae. In this paper, we first reviewed the antioxidant and antiviral potential of the active metabolites that exist in the three known macro-algae classes; Phaeophyceae, Rhodophyceae, and Chlorophyceae, and a comparison between their activities is discussed. Secondly, a review of conventional and non-conventional extraction methods is undertaken. The review then focused on identifying the optimal extraction method of sulphated polysaccharide from macro-algae that exhibits both antiviral and antioxidant activity. The review finds that species belonging to the Phaeophyceae and Rhodophceae classes are primarily potent against herpes simplex virus, followed by human immunodeficiency virus and influenza virus. At the same time, species belonging to Chlorophyceae class are recorded by most of the scholars to have antiviral activity against herpes simplex virus 1. Additionally, all three macro-algae classes exhibit antioxidant activity, the potency of which is a factor of the molecular structure of the bioactive metabolite as well as the extraction method applied.


Author(s):  
Pragya Tiwari ◽  
Yashdeep Srivastava ◽  
Hanhong Bae

: Plant-endophyte associations represent an inexhaustible source of novel metabolites, exhibiting significance in environment, agriculture and pharmaceutical perspectives. The global outbreak of life threatening diseases necessitate a need for a more targeted approach through efficient drug-discovery programs. In recent times, endophytes as “bio-factories” have been extensively explored for the production of novel, bioactive metabolites demonstrating therapeutic properties. Resources in computational biology co-integrated with combinational chemistry have made significant contributions in this field, aiding in the discovery and screening of potential “drug-like” molecules from endophytes. The review provides a meta-analysis of bioactive metabolite production from endophytes, extensively discussing the bio-prospection of natural products for pharmaceutical applications. In light of the emerging importance of endophytes as anti-infective agents, an exploration of the pharmaceutical design of novel chemical entities and analogues has enabled efficient and cost-effective drug discovery programs. However, bottlenecks in endophyte biology and research require a better understanding of endophyte dynamics and mechanism of bioactive metabolite production towards a sustainable drug discovery program.


BMC Genomics ◽  
2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Li Yan ◽  
Jianhong Zhang ◽  
Hongyu Chen ◽  
Hongmei Luo

Abstract Background ATP-binding cassette (ABC) transporters have been found to play important roles in metabolic transport in plant cells, influencing subcellular compartmentalisation and tissue distribution of these metabolic compounds. Salvia miltiorrhiza Bunge, known as Danshen in traditional Chinese medicine, is a highly valued medicinal plant used to treat cardiovascular and cerebrovascular diseases. The dry roots and rhizomes of S. miltiorrhiza contain biologically active secondary metabolites of tanshinone and salvianolic acid. Given an assembled and annotated genome and a set of transcriptome data of S. miltiorrhiza, we analysed and identified the candidate genes that likely involved in the bioactive metabolite transportation of this medicinal plant, starting with the members of the ABC transporter family. Results A total of 114 genes encoding ABC transporters were identified in the genome of S. miltiorrhiza. All of these ABC genes were divided into eight subfamilies: 3ABCA, 31ABCB, 14ABCC, 2ABCD, 1ABCE, 7ABCF, 46ABCG, and 10 ABCI. Gene expression analysis revealed tissue-specific expression profiles of these ABC transporters. In particular, we found 18 highly expressed transporters in the roots of S. miltiorrhiza, which might be involved in transporting the bioactive compounds of this medicinal plant. We further investigated the co-expression profiling of these 18 genes with key enzyme genes involved in tanshinone and salvianolic acid biosynthetic pathways using quantitative reverse transcription polymerase chain reaction (RT-qPCR). From this RT-qPCR validation, we found that three ABC genes (SmABCG46, SmABCG40, and SmABCG4) and another gene (SmABCC1) co-expressed with the key biosynthetic enzymes of these two compounds, respectively, and thus might be involved in tanshinone and salvianolic acid transport in root cells. In addition, we predicted the biological functions of S. miltiorrhiza ABC transporters using phylogenetic relationships and analysis of the transcriptome to find biological functions. Conclusions Here, we present the first systematic analysis of ABC transporters in S. miltiorrhiza and predict candidate transporters involved in bioactive compound transportation in this important medicinal plant. Using genome-wide identification, transcriptome profile analysis, and phylogenetic relationships, this research provides a new perspective on the critical functions of ABC transporters in S. miltiorrhiza.


2021 ◽  
Vol 137 ◽  
pp. 111379
Author(s):  
Benjamin Kingsley Harley ◽  
Isaac Kingsley Amponsah ◽  
Inemesit Okon Ben ◽  
Donatus Wewura Adongo ◽  
Nana Ama Mireku-Gyimah ◽  
...  

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