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1.
J Nat Prod ; 80(8): 2224-2231, 2017 08 25.
Artigo em Inglês | MEDLINE | ID: mdl-28783339

RESUMO

Ceratodon purpureus is a cosmopolitan moss that survives some of the harshest places on Earth: from frozen Antarctica to hot South Australian deserts. In a study on the survival mechanisms of the species, nine compounds were isolated from Australian and Antarctic C. purpureus. This included five biflavonoids, with complete structural elucidation of 1 and 2 reported here for the first time, as well as an additional four known phenolic compounds. Dispersion-corrected DFT calculations suggested a rotational barrier, leading to atropisomerism, resulting in the presence of diastereomers for compound 2. All isolates absorbed strongly in the ultraviolet (UV) spectrum, e.g., biflavone 1 (UV-A, 315-400 nm), which displayed the strongest radical-scavenging activity, 13% more efficient than the standard rutin; p-coumaric acid and trans-ferulic acid showed the highest UV-B (280-315 nm) absorption. The more complex and abundant 1 and 2 presumably have dual roles as both UV-screening and antioxidant compounds. They are strongly bound to Antarctic moss cell walls as well as located inside the cells of moss from both locations. The combined high stability and photoprotective abilities of these isolates may account for the known resilience of this species to UV-B radiation and its survival in some of the toughest locations in the world.


Assuntos
Antioxidantes/farmacologia , Biflavonoides/isolamento & purificação , Biflavonoides/farmacologia , Briófitas/química , Bryopsida/química , Ácidos Cumáricos/química , Fenóis/sangue , Regiões Antárticas , Antioxidantes/química , Austrália , Biflavonoides/química , Estrutura Molecular , Propionatos , Raios Ultravioleta
2.
Adv Pharm Bull ; 14(1): 86-104, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38585455

RESUMO

The translocator protein 18-kDa (TSPO) is a mitochondrial membrane protein that is previously identified as the peripheral benzodiazepine receptor (PBR). Furthermore, it plays a significant role in a diverse range of biochemical processes, including steroidogenesis, mitochondrial cholesterol transport, cell survival and death, cell proliferation, and carcinogenesis. Several investigations also reported its roles in various types of cancers, including colorectal, brain, breast, prostate, and lung cancers, as well as melanoma. According to a previous study, the expression of TSPO was upregulated in cancer cells, which corresponds to an aggressive phenotype and/or poor prognosis. Consequently, the potential for crafting diagnostic and prognostic tools with a focus on TSPO holds great potential. In this context, several radioligands designed to target this protein have been identified, and some of the candidates have advanced to clinical trials. In recent years, the use of hybrid probes with radioactive and fluorescence molecules for image-guided surgery has exhibited promising results in animal and human studies. This indicates that the approach can serve as a valuable surgical navigator during cancer surgery. The current hybrid probes are built from various molecular platforms, including small molecules, nanoparticles, and antibodies. Although several TSPO-targeted imaging probes have been developed, their development for image-guided surgery of cancers is still limited. Therefore, this review aims to highlight recent findings on the involvement of TSPO in carcinogenesis, as well as provide a new perspective on the potential application of TSPO-targeted hybrid probes for image-guided surgery.

3.
Bioimpacts ; 12(1): 43-50, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35087715

RESUMO

Introduction: In this work, we used a thread-paper microfluidic device (µTPAD) system, where a threaded part for the handling of the whole blood samples and a paper part for the reaction of plasma with immobilized bioreagents integrated into woman pad as a wearable sensing device namely as smart women pad. The µTPAD as a wearable smart woman pad is developed for the detection of pH and urea in mensuration blood as real samples. Methods: This combined device was constructed to cover the elements required, that is, separation of red blood cell, conditioning, analyte reaction, and colorimetric detection. The color change in sensing areas was measured in the RGB values via a smartphone using the Color Grab after a smart woman pad was used. The thread allowed red blood cell sampling and separation, while the paper microfluidic device was used for conditioning, biorecognition, and colorimetric transduction of pH and urea as analytes. Results: The time needed for analysis was measured as 110 s using the equilibrium method for both analytes, with a limit of detection (LOD) of 72.55 µg/mL for urea, with precision around 1.68%, while for pH around 0.80%. The smart woman pad allowed rapid detection of pH and urea in menstruation blood as real samples for monitoring of the kidney functions, and the results showed an agreement with the conventional methods that have been generally used in the clinical laboratory. Conclusion: The smart woman pad has the potential to be used as a wearable device to monitor the health status of the user via its blood mensuration analysis.

4.
Nat Prod Res ; 35(3): 481-489, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31282747

RESUMO

Annona muricata L. has been used traditionally in Indonesia to treat disease. Phytochemical studies on the alkaloid fractions from the root of Annona muricata L. from Malang-Indonesia resulted in the isolation of an unreported benzylisoquinoline alkaloid (+)-xylopine 5 as well as four known alkaloids (1-4). The crude methanol extract and alkaloid fractions were tested against Plasmodium falciparum K1 and against bacteria (Escherichia coli, Klebsiella pneumonia, Acinetobacter buamanii, Pseudomonas aeruginosa, Methicillin-resistant Staphylococcus aureus) with insignificant activities (MIC > 32 µg/mL). Individual alkaloids were tested against a human suspension cancer cell line (HL-60 leukemia cells) and two human fibroblastic cancer cell lines (A549 lung cancer cells and HepG2 liver cancer cells) in which compound 5 was the most toxic alkaloid with IC50 values ranging from 20 to 80 µM.


Assuntos
Alcaloides/química , Alcaloides/farmacologia , Annona/química , Antibacterianos/farmacologia , Antimaláricos/farmacologia , Células A549 , Antibacterianos/química , Antimaláricos/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Aporfinas/química , Avaliação Pré-Clínica de Medicamentos , Células HL-60 , Células Hep G2 , Humanos , Indonésia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Extratos Vegetais/química , Raízes de Plantas/química , Plantas Medicinais/química , Plasmodium falciparum/efeitos dos fármacos
5.
Nat Prod Res ; 29(20): 1954-8, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25699473

RESUMO

Phytochemical studies of the previously unexplored stem of Boerhavia erecta from Burkina Faso, resulted in the isolation of an unreported glycoside 4, 2,3-dihydroxypropylbenzoate-3-O-ß-[4″-methoxy] glucuronide as well as seven known glycosides (1-3, 5-8). The major isolate 5 and 8 indicated a significant inhibition against HIV integrase (IC50 10 and 22 µg/mL, respectively). The extracts and isolates were also tested for anti-malarial activity, but insignificant activity was observed.


Assuntos
Antimaláricos/química , Glicosídeos/química , Inibidores de Integrase de HIV/química , Nyctaginaceae/química , Antimaláricos/isolamento & purificação , Burkina Faso , Glicosídeos/isolamento & purificação , Inibidores de Integrase de HIV/isolamento & purificação , Concentração Inibidora 50 , Estrutura Molecular , Casca de Planta/química , Extratos Vegetais/química , Plantas Medicinais/química , Plasmodium falciparum/efeitos dos fármacos
6.
Forensic Sci Int ; 241: 102-11, 2014 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-24905152

RESUMO

The larvae of necrophagous fly species are used as forensic tools for the determination of the minimum postmortem interval (PMI). However, any ingested drugs in corpses may affect larval development, thus leading to incorrect estimates of the period of infestation. This study investigated the effects of methamphetamine and its metabolite, p-hydroxymethamphetamine, on the forensically important Australian blowfly Calliphora stygia. It was found that the presence of the drugs significantly accelerated larval growth and increased the size of all life stages. Furthermore, drug-exposed samples remained as pupae for up to 78 h longer than controls. These findings suggest that estimates of the minimum PMI of methamphetamine-dosed corpses could be incorrect if the altered growth of C. stygia is not considered. Different temperatures, drug concentrations and substrate types are also likely to affect the development of this blowfly. Pending further research, the application of C. stygia to the entomological analysis of methamphetamine-related fatalities should be appropriately qualified.


Assuntos
Dípteros/efeitos dos fármacos , Dípteros/crescimento & desenvolvimento , Metanfetamina/análogos & derivados , Metanfetamina/administração & dosagem , Entorpecentes/administração & dosagem , Animais , Larva/efeitos dos fármacos , Larva/crescimento & desenvolvimento , Pupa/efeitos dos fármacos , Pupa/crescimento & desenvolvimento
7.
Nat Prod Commun ; 6(12): 1953-66, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-22312747

RESUMO

Indonesia is rich in medicinal plants which the population has used traditionally from generation to generation for curing diseases. Our interest in the treatment of infectious diseases has lead to the investigation of traditional Indonesian treatments. In this review, we present a comprehensive review of ethnopharmacologically directed screening in Indonesian medicinal plants to search for new anti-viral, antimalarial, anti-bacterial and anti-fungal agents. Some potent drug leads have been isolated from Indonesian medicinal plants. Further research is still required for the lead development as well as the search for new bioactive compounds from the enormous medicinal plant resources.


Assuntos
Anti-Infecciosos/farmacologia , Medicina Tradicional do Leste Asiático , Extratos Vegetais/farmacologia , Plantas Medicinais , Indonésia
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