cytotoxic compounds
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Author(s):  
Sławomir Liberski ◽  
Bartlomiej J. Kaluzny ◽  
Jarosław Kocięcki

AbstractMethanol-induced optic neuropathy (Me-ION) is a serious condition that may result in long-term or irreversible visual impairment or even blindness secondary to damage and loss of function of the optic nerve and retina. Me-ION shows a tendency to occur as mass poisonings around the world with a clear predilection for poor societies in developing countries. The main mechanism underlying the molecular basis of Me-ION is the inhibition of the mitochondrial oxidative phosphorylation process through the binding of the toxic metabolite of methanol—formic acid—with the key enzyme of this process—cytochrome c oxidase. However, other mechanisms, including damage to the eye tissues by oxidative stress causing the intensification of the oxidative peroxidation process with the formation of cytotoxic compounds, as well as an increase in the synthesis of pro-inflammatory cytokines and influence on the expression of key proteins responsible for maintaining cell homeostasis, also play an important role in the pathogenesis of Me-ION. Histopathological changes in the eye tissues are mainly manifested as the degeneration of axons and glial cells of the optic nerve, often with accompanying damage of the retina that may involve all its layers. Despite the development of therapeutic approaches, persistent visual sequelae are seen in 30–40% of survivors. Thus, Me-ION continues to be an important problem for healthcare systems worldwide.


2021 ◽  
Vol 20 (2) ◽  
pp. 247-265
Author(s):  
Nadia Tasnim Ahmed ◽  
Sadia Noor ◽  
Md Mustafizur Rahman ◽  
Md Abdul Mazid

Endophytes have gained particular interest in the search of potential pharmaceutical candidates for a long time due to their diversity, species richness and bioprospecting nature. They generally produce the essential metabolites for their expansion inside the plant which is involved in various biotransformation processes of utilizing host nutrients and cell components to continue microbial growth, sustenance, and reproduction. In above processes, they produce a huge amount of both structurally and functionally diverse secondary metabolites for maintaining an effective symbiosis with hosts. These compounds are proven to have significant bioactive properties like antibacterial, antifungal, antiviral, anti-inflammatory, antioxidants, antitumor activities. Despite the proven significance, a little is exploited so far about endophytes. Particularly marine fungal endophytes which are the centre of attention in this review have gained much less importance. Due to unique environmental feature, fungal endophytes derived from marine environment offer vast diversity in different bioactive secondary metabolites. This review has focused on algicolous endophytes and bioactive secondary metabolites discovered during the last two decades. Particular importance has been given to cytotoxic and antimicrobial metabolites. Due to intensive studies during last several years, an extensive number of publications are now available on cytotoxic compounds derived from endophytic fungi of marine algicolous and spongicolous origin that have been summarized in this review. Dhaka Univ. J. Pharm. Sci. 20(2): 247-265, 2021 (December)


2021 ◽  
Vol 8 (3) ◽  
Author(s):  
Kafa Khalaf Hammud

Chamomile is an ancient herb used for various medications. It contains many bioactive constituents such as volatile oils, terpenoids, flavonoids, lactones, acid esters, glycosides and others. By reviewing many references, a confliction appeared of using Chamomile preparations to treat primary teeth eruption symptoms as a therapy administered by pediatric dentist or pediatrician. In this study, thirteen bioactive constituents (α-bisabolol (B), chamazulene (C), umbelliferone (U), apigenin (A), apigetrin (AT), apiin (AI), luteolin (L), quercetin (Q), quercimertrin (QT), rutin (R), α-cadinene (CD), α-farnesene (F), and matricarin (M) were subject to computational predication through various online websites to predicate their taste, activity towards several CYP450 enzymes and their action as Hepatotoxic, carcinogenic, immunotoxic, mutagenic, and cytotoxic compounds. Our calculations revealed several points such as high value of taste predication indicated that Chamomile constituents under study were with sour taste, did not classify as individual fatal compound Class (GHS) 1 or 2, 44.87% of them showed inhibition character toward specific cytochrome P450 enzyme while 43.59% were non- inhibition character, more than (0.5) probability predication of various cytochrome P450 enzymes gave a positive activity that may affect liver functions. Also, hepatotoxicity, carcinogenicity, immunotoxicity, mutagenicity, and cytotoxicity predictions were more than (0.5), unsaturated Chamomile constituent (Farnesene, F) had highest immune – and mutagenic properties whilst the disaccharide flavonoid (Rutin, R) had the highest Carcino- immunogenic response. According to the above notes, our conclusion is to use minimum concentration of Chamomile preparation for less period of time and lowest repeating intake that ensure effective treatment of teething symptoms under supervision of pediatricians with minimum side effect.


Author(s):  
Anna Skarżyńska ◽  
Marta Kowalczyk ◽  
Mariusz Majchrzak ◽  
Marta Piętka ◽  
Adam W. Augustyniak ◽  
...  
Keyword(s):  

Materials ◽  
2021 ◽  
Vol 14 (23) ◽  
pp. 7477
Author(s):  
Rocío Cuervo-Rodríguez ◽  
Fátima López-Fabal ◽  
Alexandra Muñoz-Bonilla ◽  
Marta Fernández-García

Herein, we develop a well-defined antibacterial polymer based on poly(2-hydroxyethyl methacrylate) (PHEMA) and a derivative of vitamin B1, easily degradable into inactive and biocompatible compounds. Hence, thiazole moiety was attached to HEMA monomer through a carbonate pH-sensitive linkage and the resulting monomer was polymerized via reversible addition-fragmentation chain transfer (RAFT) polymerization. N-alkylation reaction of the thiazole groups leads to cationic polymer with thiazolium groups. This polymer exhibits excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) with an MIC value of 78 µg mL−1, whereas its degradation product, thiazolium small molecule, was found to be inactive. Hemotoxicity studies confirm the negligible cytotoxicity of the degradation product in comparison with the original antibacterial polymer. The degradation of the polymer at physiological pH was found to be progressive and slow, thus the cationic polymer is expected to maintain its antibacterial characteristics at physiological conditions for a relative long period of time before its degradation. This degradation minimizes antimicrobial pollution in the environment and side effects in the body after eradicating bacterial infection.


2021 ◽  
Author(s):  
M Erdoğan ◽  
B Aru ◽  
ŞT Yılmaz ◽  
E Yeşilada ◽  
G Yanıkkaya Demirel ◽  
...  
Keyword(s):  

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 631
Author(s):  
Muh. Ade Artasasta ◽  
Yanwirasti Yanwirasti ◽  
Muhammad Taher ◽  
Akmal Djamaan ◽  
Ni Putu Ariantari ◽  
...  

Sponge-derived fungi have recently attracted attention as an important source of interesting bioactive compounds. Aspergillus nomius NC06 was isolated from the marine sponge Neopetrosia chaliniformis. This fungus was cultured on rice medium and yielded four compounds including three new oxisterigmatocystins, namely, J, K, and L (1, 2, and 3), and one known compound, aspergillicin A (4). Structures of the compounds were elucidated by 1D and 2D NMR spectroscopy and by high-resolution mass spectrometry. The isolated compounds were tested for cytotoxic activity against HT 29 colon cancer cells, where compounds 1, 2, and 4 exhibited IC50 values of 1.21, 2.23, and 5.62 µg/mL, respectively. Under the fluorescence microscope by using a double staining method, HT 29 cells were observed to be viable, apoptotic, and necrotic after treatment with the cytotoxic compounds 1, 2, and 4. The result shows that compounds 1 and 2 were able to induce apoptosis and cell death in HT 29 cells.


2021 ◽  
Author(s):  
Dmitriy Veriutin ◽  
Irina Doroshenko ◽  
Ekaterina Martynova ◽  
Ksenya Sapozhnikova ◽  
Elena Svirshchevskaya ◽  
...  

Heptamethine carbocyanine dyes possess bright fluorescence in the near IR range and affinity to cancer cells. Thus, these dyes could be utilized as fluorescent labels and vectors for drug delivery in their covalent conjugates with cytotoxic compounds. In this work we synthesized four drug-dye conjugates of tricarbocyanine dyes with anthracycline drug daunorubicin using a CuAAC reaction. Conjugates with hydrophobic dyes possess submicromolar cytotoxicity. Fluorescent imaging revealed significant accumulation of the conjugates in mitochondria, suggesting an enhancement of an additional mechanism of anthracycline cytotoxicity – generation of ROS. The hypothesis was supported by significant reduction of activity of the conjugates in presence of an antioxidant compound.


Author(s):  
Rafat M. Mohareb ◽  
Nadia Y. Megally Abdo ◽  
Rehab A. Ibrahim ◽  
Eman M. Samir

Background: 1,3-Diones are versatile reagents used for many heterocyclic transformations. Among such groups of compounds, cyclohexane-1,3-dione is widely used in organic synthesis to produce biologically active compounds. Objective: In this work, target molecules were synthesized from tetrahydrobenzo[b]thiophen-3- carboxamide derivative with different substituents, and their structure-activity relationships were discussed in detail. Method: Cyclohexane-1,3-dione underwent different multi-component reactions to produce fused thiophene, thiazole, coumarin, pyran, and pyridine derivatives. The anti-proliferative activity of the newly synthesized compounds toward the six cancer cell lines, namely A549, H460, HT-29, MKN-45, U87MG, and SMMC-7721 was studied. In addition, inhibitions of the most active compounds toward cancer cell lines classified according to the disease were also studied. Furthermore, Pan Assay Interference compounds (PAINS) of the selected compounds were analyzed, along with the c-Met inhibitions. Results: Anti-proliferative evaluations were performed for all of the synthesized compounds, in which the varieties of substituents through the aryl ring and the heterocyclic ring afforded compounds with high activities. Inhibition activity against the cancer cell lines classified according to the disease, c-Met, and PAINS of the synthesized compounds were measured. Conclusion: Compounds 3, 13a, 13b, 14a, 16f, 17a, 28, 30a, and 31were the most cytotoxic compounds toward the six cancer cell lines. Inhibition toward cancer cell lines classified according to the disease showed that, in most cases, the presence of the electronegative CN and or Cl groups within the molecule was responsible for its high activity.


Insects ◽  
2021 ◽  
Vol 12 (10) ◽  
pp. 951
Author(s):  
Stella Bergmann ◽  
Jan-Phillipp Gerhards ◽  
Anne Schmitz ◽  
Stefanie C. Becker ◽  
Michael Stern

Similar to vertebrates, insects are exposed to a broad variety of pathogens. The innate insect immune system provides several response mechanisms such as phagocytosis, melanization, and the synthesis of antimicrobial or cytotoxic compounds. The cytotoxic nitric oxide (NO), which is also a neurotransmitter, is involved in the response to bacterial infections in various insects but has rarely been shown to be actually produced in hemocytes. We quantified the NO production in hemocytes of Locusta migratoria challenged with diverse immune stimuli by immunolabeling the by-product of NO synthesis, citrulline. Whereas in untreated adult locusts less than 5% of circulating hemocytes were citrulline-positive, the proportion rose to over 40% after 24 hours post injection of heat-inactivated bacteria. Hemocytes surrounded and melanized bacteria in locust nymphs by forming capsules. Such sessile hemocytes also produced NO. As in other insect species, activated hemocytes were found dorsally, close to the heart. In addition, we frequently observed citrulline-positive hemocytes and capsules near the ventral nerve cord. Neurites in the CNS of sterile locust embryos responded with elevation of the second messenger cGMP after contact with purified adult NO-producing hemocytes as revealed by immunofluorescence. We suggest that hemocytes can mediate a response in the CNS of an infected animal via the NO/cGMP signaling pathway.


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