scholarly journals A Comparative Evaluation of the Cytotoxic and Antioxidant Activity of Mentha crispa Essential Oil, Its Major Constituent Rotundifolone, and Analogues on Human Glioblastoma

2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Hasan Turkez ◽  
Ozlem Ozdemir Tozlu ◽  
Tamires Cardoso Lima ◽  
Anna Emmanuela Medeiros de Brito ◽  
Damião Pergentino de Sousa
Keyword(s):  
Essential Oil ◽  
Cell Line ◽  
Blood Cells ◽  
Molecular Genetic ◽  
Public Health Problem ◽  
Chemotherapeutic Agents ◽  
Major Constituent ◽  
Major Public Health Problem ◽  
Mentha Crispa

Cancer is a major public health problem around the globe. This disorder is affected by alterations in multiple physiological processes, and oxidative stress has been etiologically implicated in its pathogenesis. Glioblastoma (GBM) is considered the most common and aggressive brain tumor with poor prognosis despite recent improvements in surgical, radiation, and chemotherapy-based treatment approaches. The purpose of this study was to evaluate antitumor activity from Mentha crispa essential oil (MCEO), its major constituent rotundifolone (ROT), and a series of six analogues on the human U87MG glioblastoma cell line. Cytotoxic effects of the compounds on the human U87MG-GBM cell line were assessed using in vitro cell viability and oxidative and molecular genetic assays. In addition, biosafety assessment tests were performed on cultured human blood cells. Our findings revealed that MCEO, 1,2-perillaldehyde epoxide (EPER1), and perillaldehyde (PALD) were the most cytotoxic compounds against U87MG cells, with IC50 values of 16.263, 15.087, and 14.888 μg/mL, respectively. Further, these compounds increased the expressions of BRAF, EGFR, KRAS, NFκB1, NFκB1A, NFκB2, PIK3CA, PIK3R, PTEN, and TP53 genes at different degrees and decreased the expression of some genes such as AKT1, AKT2, FOS, and RAF1. Finally, treatment with MCEO, EPER1, and PALD did not lead to genotoxic damage in blood cells. Taken together, our findings reveal antiproliferative potential of MCEO, its major component ROT, and its tested analogues. Some of these chemical analogues may be useful as prototypes for the development of novel chemotherapeutic agents for treating human brain cancer and/or other cancers due to their promising activities as well as nonmutagenic property and safety.

scholarly journals Antimalarial Activities of Peptide Antibiotics Isolated from Fungi

2001 ◽  
Vol 45 (1) ◽  
pp. 145-149 ◽  
Author(s):  
G. Nagaraj ◽  
M. V. Uma ◽  
M. S. Shivayogi ◽  
Hemalatha Balaram
Keyword(s):  
High Performance ◽  
Public Health Problem ◽  
Chemotherapeutic Agents ◽  
Major Public Health Problem ◽  
Drug Resistant ◽  
Peptide Antibiotics ◽  
Mass Spectral Analysis ◽  
Mass Spectral ◽  
Micromolar Range

ABSTRACT Malaria caused by Plasmodium falciparum is a major public health problem in the developing countries of the world. Clinical treatment of malaria has become complicated due to the occurrence of infections caused by drug resistant parasites. Secondary metabolites from fungi are an attractive source of chemotherapeutic agents. This work reports the isolation and in vitro antiplasmodial activities of peptide antibiotics of fungal origin. The three peptide antibiotics used in this study were efrapeptins, zervamicins, and antiamoebin. The high-performance liquid chromatography-purified peptides were characterized by nuclear magnetic resonance and mass spectral analysis. All three fungal peptides kill P. falciparum in culture with 50% inhibitory concentrations in the micromolar range. A possible mode of action of these peptide antibiotics on P. falciparum is presented.

Medicinal Plants and Bioactive Compounds for Diabetes Management: Important Advances for Drug Discovery

2020 ◽  
Vol 26 ◽  
Author(s):  
Kondeti Ramudu Shanmugam ◽  
Bhasha Shanmugam ◽  
Gangigunta Venkatasubbaiah ◽  
Sahukari Ravi ◽  
Kesireddy Sathyavelu Reddy
Keyword(s):  
Herbal Medicine ◽  
Medicinal Plants ◽  
Bioactive Compounds ◽  
Diabetes Management ◽  
Therapeutic Potential ◽  
Public Health Problem ◽  
In Vivo Studies ◽  
Major Public Health Problem

Background : Diabetes is a major public health problem in the world. It affects each and every part of the human body and also leads to organ failure. Hence, great progress made in the field of herbal medicine and diabetic research. Objectives: Our review will focus on the effect of bioactive compounds of medicinal plants which are used to treat diabetes in India and other countries. Methods: Information regarding diabetes, oxidative stress, medicinal plants and bioactive compounds were collected from different search engines like Science direct, Springer, Wiley online library, Taylor and francis, Bentham Science, Pubmed and Google scholar. Data was analyzed and summarized in the review. Results and Conclusion: Anti-diabetic drugs that are in use have many side effects on vital organs like heart, liver, kidney and brain. There is an urgent need for alternative medicine to treat diabetes and their disorders. In India and other countries herbal medicine was used to treat diabetes. Many herbal plants have antidiabetic effects. The plants like ginger, phyllanthus, curcumin, aswagandha, aloe, hibiscus and curcuma showed significant anti-hyperglycemic activities in experimental models and humans. The bioactive compounds like Allicin, azadirachtin, cajanin, curcumin, querceitin, gingerol possesses anti-diabetic, antioxidant and other pharmacological properties. This review focuses on the role of bioactive compounds of medicinal plants in prevention and management of diabetes. Conclusion: Moreover, our review suggests that bioactive compounds have the potential therapeutic potential against diabetes. However, further in vitro and in vivo studies are needed to validate these findings.

Chemical Composition and in-vitro antimicrobial screening of leaf essential oil of Plectranthus gerardianus Benth., and isolation of the major constituent of oil

2020 ◽  
Vol 10 ◽  
Author(s):  
Navadha Bhatt ◽  
Navabha Joshi ◽  
Kapil Ghai ◽  
Om Prakash
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oil ◽  
Major Constituent ◽  
In Vitro Antimicrobial Activity ◽  
Gram Positive Bacteria ◽  
Medicinal Value ◽  
Leaf Essential Oil ◽  
Plant Families ◽  
Total Oil

Background: The Lamiaceae (Labiatae) is one of the most diverse and widespread plant families’ in terms of ethno medicine and its medicinal value is based on the volatile oils concentration. This family is important for flavour, fragrance and medicinal properties. Manyplants belonging to this family have indigenous value. Method: The essential oil of Plectranthus gerardianusBenth. (Lamiaceae), was analysed by GC and GC-MS analysis, while the major component was isolated and conformed by NMR spectroscopy. Result: The oil was found to be rich in oxygenated monoterpenes, which contribute around 62% of the total oil. The major components identified were fenchone (22.90%) and carvenone oxide (16.75%), besides other mono and sesquiterpenoids. The in-vitro antimicrobial activity of essential oil was tested against three gram negative bacteria viz. Pasteurellamultocida, Escherichia coli, and Salmonella enterica, two gram positive bacteria viz. Staphylococcus aureus and Bacillus subtilis and two fungi viz. Candida albicans and Aspergillusflavus. The antimicrobial activity of the oil was also compared to the antimicrobial activity of leaf essential oil of another Himalayan plant viz. Nepetacoerulescens. Conclusion: The oil showed in-vitro antimicrobial activity against all the microbial strains and can lessen the ever-growing demand of potentially hazardous antibiotics for treatment.

scholarly journals Microwave-Assisted Synthesis of (Piperidin-1-yl)quinolin-3-yl)methylene)hydrazinecarbothioamides as Potent Inhibitors of Cholinesterases: A Biochemical and In Silico Approach

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 656
Author(s):  
Rubina Munir ◽  
Muhammad Zia-ur-Rehman ◽  
Shahzad Murtaza ◽  
Sumera Zaib ◽  
Noman Javid ◽  
...  
Keyword(s):  
Neurodegenerative Disorder ◽  
Critical Role ◽  
Public Health Problem ◽  
Microwave Assisted Synthesis ◽  
Major Public Health Problem ◽  
Spectroscopic Techniques ◽  
Dual Inhibitor ◽  
Microwave Assisted ◽  
Ic50 Values

Alzheimer’s disease (AD), a progressive neurodegenerative disorder, characterized by central cognitive dysfunction, memory loss, and intellectual decline poses a major public health problem affecting millions of people around the globe. Despite several clinically approved drugs and development of anti-Alzheimer’s heterocyclic structural leads, the treatment of AD requires safer hybrid therapeutics with characteristic structural and biochemical properties. In this endeavor, we herein report a microwave-assisted synthesis of a library of quinoline thiosemicarbazones endowed with a piperidine moiety, achieved via the condensation of 6/8-methyl-2-(piperidin-1-yl)quinoline-3-carbaldehydes and (un)substituted thiosemicarbazides. The target N-heterocyclic products were isolated in excellent yields. The structures of all the synthesized compounds were fully established using readily available spectroscopic techniques (FTIR, 1H- and 13C-NMR). Anti-Alzheimer potential of the synthesized heterocyclic compounds was evaluated using acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The in vitro biochemical assay results revealed several compounds as potent inhibitors of both enzymes. Among them, five compounds exhibited IC50 values less than 20 μM. N-(3-chlorophenyl)-2-((8-methyl-2-(piperidin-1-yl)quinolin-3-yl)methylene)hydrazine carbothioamide emerged as the most potent dual inhibitor of AChE and BChE with IC50 values of 9.68 and 11.59 μM, respectively. Various informative structure–activity relationship (SAR) analyses were also concluded indicating the critical role of substitution pattern on the inhibitory efficacy of the tested derivatives. In vitro results were further validated through molecular docking analysis where interactive behavior of the potent inhibitors within the active pocket of enzymes was established. Quinoline thiosemicarbazones were also tested for their cytotoxicity using MTT assay against HepG2 cells. Among the 26 novel compounds, there were five cytotoxical and 18 showed proliferative properties.

scholarly journals In Vitro and In Silico Anti-Arboviral Activities of Dihalogenated Phenolic Derivates of L-Tyrosine

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3430
Author(s):  
Vanessa Loaiza-Cano ◽  
Laura Milena Monsalve-Escudero ◽  
Manuel Pastrana Restrepo ◽  
Diana Carolina Quintero-Gil ◽  
Sergio Andres Pulido Muñoz ◽  
...  
Keyword(s):  
Cell Line ◽  
Viral Protein ◽  
In Silico ◽  
Public Health Problem ◽  
Cellular Proteins ◽  
Vero Cell Line ◽  
Viral Particles ◽  
Pre Treatment ◽  
Line Infection

Despite the serious public health problem represented by the diseases caused by dengue (DENV), Zika (ZIKV) and chikungunya (CHIKV) viruses, there are still no specific licensed antivirals available for their treatment. Here, we examined the potential anti-arbovirus activity of ten di-halogenated compounds derived from L-tyrosine with modifications in amine and carboxyl groups. The activity of compounds on VERO cell line infection and the possible mechanism of action of the most promising compounds were evaluated. Finally, molecular docking between the compounds and viral and cellular proteins was evaluated in silico with Autodock Vina®, and the molecular dynamic with Gromacs®. Only two compounds (TDC-2M-ME and TDB-2M-ME) inhibited both ZIKV and CHIKV. Within the possible mechanism, in CHIKV, the two compounds decreased the number of genome copies and in the pre-treatment strategy the infectious viral particles. In the ZIKV model, only TDB-2M-ME inhibited the viral protein and demonstrate a virucidal effect. Moreover, in the U937 cell line infected with CHIKV, both compounds inhibited the viral protein and TDB-2M-ME inhibited the viral genome too. Finally, the in silico results showed a favorable binding energy between the compounds and the helicases of both viral models, the NSP3 of CHIKV and cellular proteins DDC and β2 adrenoreceptor.

scholarly journals Determination of Chemical Composition, In Vitro and In Silico Evaluation of Essential Oil from Leaves of Apium graveolens Grown in Saudi Arabia

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7372
Author(s):  
Ahmed I. Foudah ◽  
Mohammed H. Alqarni ◽  
Aftab Alam ◽  
Mohammad Ayman Salkini ◽  
Pravej Alam ◽  
...  
Keyword(s):  
Saudi Arabia ◽  
Essential Oil ◽  
In Silico ◽  
Docking Simulation ◽  
Antimicrobial Activities ◽  
Apium Graveolens ◽  
Gas Chromatography Mass Spectrometry ◽  
Major Constituent ◽  
Anti Inflammatory

The aim of this study was to explore the composition and evaluate the in silico and in vitro antioxidants and antimicrobial and anti-inflammatory effects of Apium graveolens var. dulce leaves essential oil (AGO) collected from Al-Kharj (Saudi Arabia). AGO was isolated using the hydro-distillation method, and its composition was studied using gas-chromatography-mass Spectrometry (GC–MS), antimicrobial activities using well diffusion assay, and antioxidant and anti-inflammatory activities using spectrophotometric methods. The pharmacological activities of their major compounds were predicted using PASS (prediction of activity spectra for substances) and drug-likening properties by ADME (absorption, distribution, metabolism, and excretion) through web-based online tools. Isocnidilide (40.1%) was identified as the major constituent of AGO along with β-Selinene, Senkyunolide A, Phytyl acetate, and 3-Butylphthalide. AGO exhibited a superior antibacterial activity, and the strongest activity was detected against Gram-positive bacteria and Candida albicans. Additionally, it exhibited a weaker antioxidant potential and stronger anti-inflammatory effects. PASS prediction supported the pharmacological finding, whereas ADMET revealed the safety of AGO. The molecular docking of isocnidilide was carried out for antibacterial (DNA gyrase), antioxidant (tyrosinase), and anti-inflammatory (cyclooxygenase-2) activities. The docking simulation results were involved hydrophilic interactions and demonstrated high binding affinity of isocnidilide for anti-inflammatory protein (cycloxygenase-2). The presence of isocnidilide makes AGO a potential anti-inflammatory and antimicrobial agent. AGO, and its major metabolite isocnidilide, may be a suitable candidate for the future drug development.

scholarly journals Does Bromelain-Cisplatin Combination Afford In-Vitro Synergistic Anticancer Effects on Human Prostatic Carcinoma Cell Line, PC3?

2020 ◽  
Vol 9 ◽  
pp. 1749
Author(s):  
Fatemeh Amini Chermahini ◽  
Elham Raeisi ◽  
Mathias Hossain Aazami ◽  
Abbas Mirzaei ◽  
Esfandiar Heidarian ◽  
...  
Keyword(s):  
Gene Expression ◽  
Cell Viability ◽  
Cell Line ◽  
Colony Formation ◽  
Prostatic Carcinoma ◽  
Carcinoma Cell ◽  
Quantitative Polymerase Chain Reaction ◽  
Chemotherapeutic Agents ◽  
Carcinoma Cell Line

Background: Bromelain enhances anticancer impacts to chemotherapeutic agents. The question as to whether bromelain does promote in-vitro cytotoxic and proapoptotic effects of cisplatin on human prostatic carcinoma PC3 cell line was investigated. Materials and Methods: PC3 (human prostatic carcinoma) cells were treated either single or in combination with bromelain and/or cisplatin. MTT, clonogenic assay, flow cytometry and real-time quantitative polymerase chain reaction were used to investigate cell viability, colony formation, proapoptotic potential and p53 gene expression, respectively. Results: Cisplatin (IC10) combined with bromelain (IC40) significantly affected PC3 cell viability, inhibited colony formation, as well increased p53 proapoptotic gene expression compared to cisplatin single treatment. Nevertheless, bromelain-cisplatin chemoherbal combination did not display any additive proapoptotic effect compared to single treatments. Conclusion: Bromelain-cisplatin chemoherbal combination demonstrated synergistic in-vitro anticancer effect on human prostatic carcinoma cell line, PC3, that drastically reduced required cisplatin dose. [GMJ.2020;9:e1749]

scholarly journals Non-Toxic Virucidal Macromolecules Show High Efficacy Against Influenza Virus Ex Vivo and In Vivo

2020 ◽  
Author(s):  
Ozgun Kocabiyik ◽  
Valeria Cagno ◽  
Paulo Jacob Silva ◽  
Yong Zhu ◽  
Laura Sedano ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Viral Infections ◽  
Ex Vivo ◽  
Public Health Problem ◽  
Major Public Health Problem ◽  
New Class ◽  
Influenza Strain ◽  
Low Toxicity

AbstractInfluenza is one of the most widespread viral infections worldwide and represents a major public health problem. The risk that one of the next pandemics is caused by an influenza strain is very high. It is very important to develop broad-spectrum influenza antivirals to be ready for any possible vaccine shortcomings. Anti-influenza drugs are available but they are far from ideal. Arguably, an ideal antiviral should target conserved viral domains and be virucidal, i.e. irreversibly inhibit viral infectivity. Here, we describe a new class of broad-spectrum anti-influenza macromolecules that meets these criteria and displays exceedingly low toxicity. These compounds are based on a cyclodextrin core modified on its primary face with long hydrophobic linkers terminated in 6’sialyl-N-acetyllactosamine (6’SLN) or 3’SLN. SLN enables nanomolar inhibition of the viruses while the hydrophobic linkers confer irreversibility to the inhibition. The combination of these two properties allows for efficacy in vitro against several human or avian influenza strains, as well as against a 2009 pandemic influenza strain ex vivo. Importantly, we show that, in mice, the compounds provide therapeutic efficacy when administered 24h post-infection allowing 90% survival as opposed to no survival for the placebo and oseltamivir..

Chemical profile and antiperiodontal potential of Thymus linearis Benth. Essential oil using ADMET prediction, In silico and in vitro tools

2021 ◽  
pp. 1-16
Author(s):  
Abdul Rafey ◽  
Aqsa Batool ◽  
Muhammad Kamran ◽  
Samiullah Khan ◽  
Muhammad Akram ◽  
...  
Keyword(s):  
Essential Oil ◽  
In Silico ◽  
Treatment Options ◽  
Significant Inhibition ◽  
Bacterial Biofilm ◽  
Health Concern ◽  
Major Constituent ◽  
Antimicrobial Studies ◽  
Development Of Resistance

Periodontitis is an important health concern that is associated with long term complications. Development of resistance to antibiotics limits the treatment options in periodontitis. We investigated Thymus linearis essential oil for treatment of periodontitis. The essential oil was collected using hydrodistillation and characterized using GC-MS. The constituents were further analyzed for druglikeness, ADMET properties and molecular docking using transcription regulators 2UV0 and 3QP5. The GC-MS results revealed that carvacrol was a major constituent (76.26%) followed by caryophyllene oxide (6.83%) and L-borneol (6.08%). The in vitro antimicrobial studies showed significant inhibition against Staphylococcus aureus, Staphylococcus epidermidis and Pseudomonas aeruginosa (MIC range 0.024 –0.312μg/mL). The essential oil showed a good inhibition of bacterial biofilm produced by S. aureus (72%) and S. epidermidis (70%). Finally, the antiquorum sensing property (30 mm zone of inhibition) was recorded with violacein inhibition (58%). Based on in silico and in vitro findings, it was concluded that T. linearis essential oil can be used for the treatment of periodontal infections.

Development of new dinuclear Fe(III) coordination compounds with in vitro nanomolar antitrypanosomal activity

2021 ◽  
Author(s):  
Felipe Figuerôa Moreira ◽  
Juliana de Araujo Portes ◽  
Nathalia Florencia Barros Azeredo ◽  
Christiane Fernandes ◽  
Adolfo Horn ◽  
...  
Keyword(s):  
Public Health ◽  
Trypanosoma Cruzi ◽  
Chagas Disease ◽  
Health Problem ◽  
Coordination Compounds ◽  
Public Health Problem ◽  
Neglected Tropical Disease ◽  
Major Public Health Problem ◽  
Protozoan Pathogen

Chagas disease is a neglected tropical disease caused by the protozoan pathogen Trypanosoma cruzi. The disease is the major public health problem affecting about 6 to 7 million people worldwide,...

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