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1.
Pharmaceuticals (Basel) ; 14(3)2021 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-33809034

RESUMO

Though it was once known that upregulated Cannabinoid Receptor (CB1) and downregulated Fatty Acid Amide Hydrolase (FAAH1) are associated with tumour aggressiveness and metastasis, it is now clear that upregulated CB1 levels more than a certain point cause accumulation of ceramide and directs cells to apoptosis. Hence, CB1 analogues/FAAH1 blockers are explored widely as anticancer drugs. There are reports on CB1-agonists and FAAH1-blockers separately, however, dual activities along with ovarian cancer-specific links are not established for any natural compound. With this setting, we describe for the first time the isolation of 3-hydroxypropane-1,2-diyl dipalmitoleate (564.48 Da) from a marine snail, Conus inscriptus, which binds to both CB1 and FAAH1 (glide energies: -70.61 and -30.52 kcal/mol, respectively). MD simulations indicate stable compound-target interaction for a minimum of 50 nanoseconds with relative invariabilities in Rg. The compound inhibited ovarian cancer cell line, PA1 at 1.7 µM. Structural and chemical interpretation of the compound (C2) was done using FT-IR, GC-MS, ESI-MS, 1H and 13C-NMR (1 and 2D). Furthermore, a probable route for gram-scale synthesis of C2 is hinted herein. With the available preliminary data, molecular mechanisms involving dual roles for this potent molecule must be elucidated to understand the possibilities of usage as an anticancer drug.

2.
Chemosphere ; 202: 387-399, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29579674

RESUMO

Dibenz(a,h)Anthracene (DBahA), classified as a probable human carcinogen (B2) is the first Poly Aromatic Hydrocarbons (PAH) to be chemically purified and used for cancer-based studies. Till date, only 30 papers focus on the bioremediation aspects of DBahA out of more than 200 research publications for each of the other 15 priority PAHs. Thus, the review raises an alarm and calls for efficient bioremediation strategies for considerable elimination of this compound from the environment. This article reviews and segregates the available papers on DBahA bioremoval from the beginning till date into bacteria, fungi and plant-mediated remediation and offers suggestions for the most competent and cost-effective modes to bioremove DBahA from the environment. One of the proficient ways to get rid of this PAH could with the use of biosurfactant-enriched bacterial consortium in DBahA polluted environment, which is given considerable importance here. Among the bacterial and fungal microbiomes, unquestionably the former are the beneficiaries which utilize the breakdown products of this PAH metabolized by the latter. Nevertheless, the use of plant communities for efficient DBahA utilization through fibrous root system is also discussed at length. The current status of DBahA as reflected by the publications at https://www.ncbi.nlm.nih.gov and recommendations among the explored groups [bacterial/fungal/plant communities] for better DBahA elimination are pointed out. Finally, the review emphasizes the pros and cons of all the methodologies used for selective/combinatorial removal of DBahA and present the domain to the researchers to carry forward by incorporating their individual ideas.


Assuntos
Poluentes Ambientais/metabolismo , Eucariotos/metabolismo , Hidrocarbonetos Policíclicos Aromáticos/metabolismo , Bactérias/metabolismo , Benzo(a)Antracenos/metabolismo , Biodegradação Ambiental , Carcinógenos , Fungos/metabolismo , Humanos , Plantas/metabolismo , Hidrocarbonetos Policíclicos Aromáticos/análise
3.
Int J Biol Macromol ; 108: 531-540, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29208557

RESUMO

We identified that Pseudomonas guguanensis produced macromolecular mono-rhamnolipid (1264.52 Da) upon sensing n-hexadecane/diesel/kerosene from its surroundings. Permutation experiments were done to improve the laboratory-scale mono-rhamnolipid production (ie, a three-fold increase) using RSM validation. Consequently, maximal mono-rhamnolipids production [40-50 mg/L] and emulsification abilities [65-70%] were encountered on day 8 using vegetable oil, peptone + yeast extract. EI24 values for the rhamnolipids were found to be 78±1.75% at 12.5 mg/ mL. Production and secretion of rhamnolipids were accompanied by aggregation of cells at day 6 as pictured in SEM. Pure monorhamnolipids of P. guguanensis was found to lower the surface tension of water to 32.98±0.3 mN/m than the crude and CFSs of P. aeruginosa indicating efficient activity. Utilization and subsequent removal of hexadecane was 77.2% and the breakdown products were fatty acids [decanoic, hexadecanoic, octadecanoic acids and methyl stearates] as signified in Head-space GC-MS. The breakdown products of hexadecane are also present in the synthesized rhamnolipids suggesting their biosynthetic role. Rapid degradation of hexadecane, diesel and kerosene by this emulsifier combined with non-pathogenic trait of P. guguanensis identifies this organism as a viable option to remove n-alkanes from aquatic environments.


Assuntos
Organismos Aquáticos/metabolismo , Pseudomonas/metabolismo , Ramnose/análogos & derivados , Organismos Aquáticos/isolamento & purificação , Organismos Aquáticos/ultraestrutura , Biotransformação , Decanoatos/química , Emulsificantes/química , Emulsificantes/metabolismo , Poluição Ambiental , Cromatografia Gasosa-Espectrometria de Massas , Hidrocarbonetos/metabolismo , Estrutura Molecular , Peso Molecular , Ácido Palmítico/química , Pseudomonas/isolamento & purificação , Pseudomonas/ultraestrutura , Ramnose/biossíntese , Ramnose/química , Compostos Orgânicos Voláteis/química
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