Trans-β-Caryophyllene: An Effective Antileishmanial Compound Found in Commercial Copaiba Oil (Copaiferaspp.)

This study investigated the leishmanicidal activity againstLeishmania amazonensisof four commercial oils fromCopaiferaspp. named as C1, C2, C3, and C4, the sesquiterpene and diterpene pools obtained from distilling C4, and isolatedβ-caryophyllene (CAR). Copaiba oils chemical compositions were analyzed by gas chromatography and correlated with biological activities. Diterpenes-rich oils C2 and C3 showed antipromastigote activity. Sesquiterpenes-rich C1 and C4, and isolated CAR presented a dose-dependent activity against intracellular amastigotes, with IC50sof 2.9 µg/mL, 2.3 µg/mL, and 1.3 µg/mL (6.4 µM), respectively. Based on the highest antiamastigote activity and the low toxicity to the host cells, C4 was steamdistillated to separate pools of sesquiterpenes and diterpenes. Both pools were less active againstL. amazonensisand more toxic for the macrophages than the whole C4 oil. The leishmanicidal activity of C3 and C4 oils, as well as C4 fractions and CAR, appears to be independent of nitric oxide production by macrophages. This study pointed outβ-caryophyllene as an effective antileishmanial compound and also to its role as potential chemical marker in copaiba oils or fractions derived thereof, aiming further development of this rainforest raw material for leishmaniasis therapy.

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Cytotoxic and Anti- Inflammatory Activities of Glycosaminoglycans (GAGs) from Selected Sea Food Waste Extract on Cell Lines

Materials Science Forum ◽

10.4028/www.scientific.net/msf.981.258 ◽

2020 ◽

Vol 981 ◽

pp. 258-264

Author(s):

Nurul Haida Idrus ◽

Nina Suhaity Azmi ◽

Che Nur Mazadillina Che Zahari ◽

Solachuddin Jauhari Arief Ichwan

Keyword(s):

Dermatan Sulfate ◽

Biological Activities ◽

Keratan Sulfate ◽

Sea Bass ◽

Raw Material ◽

No Production ◽

Dependent Manner ◽

Alternative Source ◽

Anti Inflammatory ◽

Dose Dependent

Glycosaminoglycans (GAGs) are long unbranched polysaccharide that composed of repeating disaccharide units. They are classified into heparan sulfate (HS), heparin, chondroitin sulfate (CS), dermatan sulfate (DS), keratan sulfate (KS) and hyaluronic acid (HA). During the last decade, demand of GAGs were getting increased due to their potential uses. Vertebrate animal, commonly cartilaginous mammalian tissue, were potential producer of GAGs and have the higher number of biological activities extracted from sea bass waste. Sea bass waste from Lates calcarifer was used as the raw material to extract crude GAGs. Different part of sea bass waste such as, gills, viscera and air bladders were used. The higher content of crude GAGs in sea bass waste was used in cytotoxic and inflammatory study. Different concentration of extract GAGs from gills were used ranging between 0.16-20 mg/mL. GAGs from sea bass waste (gills) showed dose-dependent cytotoxic activity towards MCF-7 cell line in lower concentration. Meanwhile, for anti-inflammatory study GAGs from sea bass waste (gills) showed dose-dependent manner and also reduce NO production in LPS-stimulated cells. This research study concluded that, GAGs from sea bass waste are the alternative source that can be used for cancer and inflammation study.

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Inhibition of glycogen synthase kinase-3-beta (GSK3β) blocks nucleocapsid phosphorylation and SARS-CoV-2 replication

10.21203/rs.3.rs-1197371/v1 ◽

2022 ◽

Author(s):

Tirosh Shapira ◽

Celine Rens ◽

Virginia Pichler ◽

William Rees ◽

Theodor Steiner ◽

...

Keyword(s):

Glycogen Synthase ◽

Host Cells ◽

N Protein ◽

Kinase Substrate ◽

Protein Levels ◽

Dependent Activity ◽

Multiple Cell ◽

Low Toxicity ◽

Dose Dependent ◽

Targeted Library

Abstract GSK3β has been proposed to have an essential role in Coronaviridae infection. Screening of a targeted library of GSK3β inhibitors against SARS-CoV-2 and HCoV-229E resulted in identification of high proportion of active compounds with low toxicity to host cells. A select lead compound, T-1686568, showed dose-dependent activity against SARS-CoV-2 transcription, translation and viral particle release in multiple cell lines and primary organoids. A protein kinase substrate profiling assay combined with western blot analysis showed that SARS-CoV-2 nucleocapsid is phosphorylated by GSK3β on S180/S184, S190/S194 and T198 which have already been primed in the adjacent phospho-sites S188, T198 and S206 respectively. Inhibition by T-1686568 resulted in reduction of the S1 Spike protein levels, an accumulation of the Nucleocapsid (N) protein and maintenance of the non-structural (NSP2) level in infected Huh-7.5.1 cells, indicating that N phosphorylation might serve as a critical precursor for processing and release of mature viruses.

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The Bioactivities and Potential Clinical Values of Angelica Sinensis Polysaccharides

Natural Product Communications ◽

10.1177/1934578x21997321 ◽

2021 ◽

Vol 16 (3) ◽

pp. 1934578X2199732

Author(s):

Shi-Jie Bi ◽

Rui-Jia Fu ◽

Jia-Jia Li ◽

Yan-Yan Chen ◽

Yu-Ping Tang

Keyword(s):

Biological Activities ◽

Volatile Oil ◽

Extraction Methods ◽

Chemical Components ◽

Angelica Sinensis ◽

Chemical Compositions ◽

Chronic Anemia ◽

Angelica Sinensis Radix ◽

Research Prospect ◽

Further Development

Angelica sinensis Radix (ASR), one of the most commonly used traditional Chinese medicines, contains many chemical components such as polysaccharides, volatile oil, flavonoids, amino acids, and organic acids, among which polysaccharides play an indispensable role in the therapeutic effect of ASR. A. sinensis polysaccharide (ASP) has many biological activities, for instance, hematopoietic, anti-tumor, and liver protection, which are closely related to the treatment of human diseases such as chronic anemia, leukemia, and diabetes. In addition, there are excellent application prospects for drug delivery in nanoparticles. This paper reviews the chemical compositions, extraction methods, biological activity, action mechanism, potential clinical applications, nanoparticles, and research prospect of ASP from 2010 to 2020, so as to provide references for its further development.

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ANTICANCER EFFECT OF UVARIA GENUS

Journal of Medicine and Pharmacy ◽

10.34071/jmp.2013.6.16 ◽

2014 ◽

pp. 98-101

Author(s):

Thi Bich Hien Le ◽

Viet Duc Ho ◽

Thi Hoai Nguyen

Keyword(s):

Biological Activities ◽

Current Trend ◽

Healthcare Systems ◽

Chemical Compositions ◽

Cancer Therapies ◽

Pharmacological Effects ◽

Anticancer Effect ◽

Anti Cancer ◽

Tropical Areas ◽

Cancer Activity

Nowadays, cancer treatment has been a big challenge to healthcare systems. Most of clinical anti-cancer therapies are toxic and cause adverse effects to human body. Therefore, current trend in science is seeking and screening of natural compounds which possess antineoplastic activities to utilize in treatment. Uvaria L. - Annonaceae includes approximately 175 species spreading over tropical areas of Asia, Australia, Africa and America. Studies on chemical compositions and pharmacological effects of Uvaria showed that several compound classes in this genus such as alkaloid, flavonoid, cyclohexen derivaties, acetogenin, steroid, terpenoid, etc. indicate considerable biological activities, for example anti-tumor, anti-cancer, antibacterial, antifungal, antioxidant, etc. Specifically, anti-cancer activity of fractions of extract and pure isolated compounds stands out for cytotoxicity against many cancer cell lines. This study provides an overview of anti-cancer activity of Uvaria and suggests a potential for further studies on seeking and developing novel anti-cancer compounds. Key words: Anti-cancer, Uvaria.

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Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

Current Medicinal Chemistry ◽

10.2174/0929867324666171009122612 ◽

2018 ◽

Vol 25 (5) ◽

pp. 636-658 ◽

Cited By ~ 22

Author(s):

Jan Pokorny ◽

Lucie Borkova ◽

Milan Urban

Keyword(s):

Biological Activities ◽

Synthetic Approach ◽

Clinical Use ◽

New Approach ◽

Click Reactions ◽

Drug Candidates ◽

The Past ◽

Low Toxicity ◽

New Compounds ◽

Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

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Novel Piperazine Amides of Cinnamic Acid Derivatives as Tyrosinase Inhibitors

Letters in Drug Design & Discovery ◽

10.2174/1570180815666180420105652 ◽

2018 ◽

Vol 16 (1) ◽

pp. 36-44 ◽

Cited By ~ 3

Author(s):

Zehra Tuğçe Gür ◽

Fatma Sezer Şenol ◽

Suhaib Shekfeh ◽

İlkay Erdoğan Orhan ◽

Erden Banoğlu ◽

...

Keyword(s):

Cinnamic Acid ◽

Active Site ◽

Agaricus Bisporus ◽

Biological Activities ◽

Docking Simulation ◽

Cinnamic Acid Derivatives ◽

In Silico Docking ◽

Amide Derivatives ◽

Tyrosinase Inhibitors ◽

Further Development

Background: A series of novel cinnamic acid piperazine amide derivatives has been designed and synthesized, and their biological activities were also evaluated as potential tyrosinase inhibitors. Methods: Compounds 9, 11 and 17 showed the most potent biological activity (IC50 = 66.5, 61.1 and 66 µM, respectively). In silico docking simulation was performed to position compound 11 into the Agaricus bisporus mushroom tyrosinase’s active site to determine the putative binding interactions. Results and Conclusion: The results indicated that compound 11 could serve as a promising lead compound for further development of potent tyrosinase inhibitors.

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Naphthalimide-Containing BP100 Leads to Higher Model Membranes Interactions and Antimicrobial Activity

Biomolecules ◽

10.3390/biom11040542 ◽

2021 ◽

Vol 11 (4) ◽

pp. 542

Author(s):

Gustavo Penteado Battesini Carretero ◽

Greice Kelle Viegas Saraiva ◽

Magali Aparecida Rodrigues ◽

Sumika Kiyota ◽

Marcelo Porto Bemquerer ◽

...

Keyword(s):

Anticancer Agents ◽

Biological Activities ◽

Biological Effects ◽

Membrane Surface ◽

Helical Structure ◽

Helical Conformation ◽

Property A ◽

Cellular Processes ◽

Double Stranded Dna ◽

Low Toxicity

In a large variety of organisms, antimicrobial peptides (AMPs) are primary defenses against pathogens. BP100 (KKLFKKILKYL-NH2), a short, synthetic, cationic AMP, is active against bacteria and displays low toxicity towards eukaryotic cells. BP100 acquires a α-helical conformation upon interaction with membranes and increases membrane permeability. Despite the volume of information available, the action mechanism of BP100, the selectivity of its biological effects, and possible applications are far from consensual. Our group synthesized a fluorescent BP100 analogue containing naphthalimide linked to its N-terminal end, NAPHT-BP100 (Naphthalimide-AAKKLFKKILKYL-NH2). The fluorescence properties of naphthalimides, especially their spectral sensitivity to microenvironment changes, are well established, and their biological activities against transformed cells and bacteria are known. Naphthalimide derived compounds are known to interact with DNA disturbing related processes as replication and transcription, and used as anticancer agents due to this property. A wide variety of techniques were used to demonstrate that NAPHT-BP100 bound to and permeabilized zwitterionic POPC and negatively charged POPC:POPG liposomes and, upon interaction, acquired a α-helical structure. Membrane surface high peptide/lipid ratios triggered complete permeabilization of the liposomes in a detergent-like manner. Membrane disruption was driven by charge neutralization, lipid aggregation, and bilayer destabilization. NAPHT-BP100 also interacted with double-stranded DNA, indicating that this peptide could also affect other cellular processes besides causing membrane destabilization. NAPHT-BP100 showed increased antibacterial and hemolytic activities, compared to BP100, and may constitute an efficient antimicrobial agent for dermatological use. By conjugating BP100 and naphthalimide DNA binding properties, NAPHT-BP100 bound to a large extent to the bacterial membrane and could more efficiently destabilize it. We also speculate that peptide could enter the bacteria cell and interact with its DNA in the cytoplasm.

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Cotton stalk-derived hydrothermal carbon for methylene blue dye removal: investigation of the raw material plant tissues

Bioresources and Bioprocessing ◽

10.1186/s40643-021-00364-8 ◽

2021 ◽

Vol 8 (1) ◽

Author(s):

Libo Zhang ◽

Junyan Tan ◽

Gangying Xing ◽

Xintong Dou ◽

Xuqiang Guo

Keyword(s):

Methylene Blue ◽

Functional Materials ◽

Raw Material ◽

Plant Tissues ◽

Chemical Compositions ◽

Waste Biomass ◽

Cotton Stalk ◽

Acid Base ◽

X Ray ◽

Bet Analysis

AbstractConversion of the abundant agricultural residual cotton stalk (CS) into useful chemicals or functional materials could alleviate the fossil fuels caused energy shortages and environmental crises. Although some advances have been achieved, less attention has been paid to the plant tissues effect. In this study, the plant tissue of CS was changed by part degradation of some components (hemicelluloses and lignin, for example) with the aid of acid/base (or both). The pretreated CS was transformed into hydrochar by hydrothermal carbonization (HTC) method. Morphological and chemical compositions of CS hydrochar were analyzed by various techniques, including elemental analysis, Fourier transform infrared (FTIR), BET analysis, X-ray photoelectron spectroscopy (XPS) and X-ray diffraction (XRD). Methylene blue (MB) removal of prepared CS hydrochar was used to evaluate CS hydrochar pollutions adsorption capacity. Results reveal acid/base (or both) pretreatment is beneficial for CS raw material to prepare high-quality CS hydrochar. The effects of some parameters, such as initial MB concentration, temperature, pH value and recyclability on the adsorption of MB onto both acid and base-pretreated CS hydrochar (CS-H2SO4 + NaOH-HTC) were studied. The present work exhibits the importance of agricultural waste biomass material plant tissues on its derived materials, which will have a positive effect on the direct utilization of waste biomass.

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Phytochemical Analysis and Potential Biological Activities of Essential Oil from Rice Leaf

Molecules ◽

10.3390/molecules24030546 ◽

2019 ◽

Vol 24 (3) ◽

pp. 546 ◽

Cited By ~ 3

Author(s):

Truong Minh ◽

Tran Xuan ◽

Truong Van ◽

Yusuf Andriana ◽

Tran Viet ◽

...

Keyword(s):

Mass Spectrometry ◽

Essential Oil ◽

Atmospheric Pressure Chemical Ionization ◽

Biological Activities ◽

Methyl Ricinoleate ◽

Gas Chromatography Mass Spectrometry ◽

Phytochemical Analysis ◽

Chemical Compositions ◽

Rice Leaf ◽

Rice Leaves

Although many investigations on phytochemicals in rice plant parts and root exudates have been conducted, information on the chemical profile of essential oil (EO) and potent biological activities has been limited. In this study, chemical compositions of rice leaf EO and in vitro biological activities were investigated. From 1.5 kg of fresh rice leaves, an amount of 20 mg EO was obtained by distillation and analyzed by gas chromatography-mass spectrometry (GC-MS), electrospray ionization (ESI), and atmospheric pressure chemical ionization (APCI) to reveal the presence of twelve volatile constituents, of which methyl ricinoleate (27.86%) was the principal compound, followed by palmitic acid (17.34%), and linolenic acid (11.16%), while 2-pentadecanone was the least (2.13%). Two phytoalexin momilactones A and B were first time identified in EO using ultra-performance liquid chromatography coupled with electrospray mass spectrometry (UPLC/ESI-MS) (9.80 and 4.93 ng/g fresh weight, respectively), which accounted for 7.35% and 3.70% of the EO, respectively. The assays of DPPH (IC50 = 73.1 µg/mL), ABTS (IC50 = 198.3 µg/mL), FRAP (IC50 = 700.8 µg/mL) and β-carotene oxidation (LPI = 79%) revealed that EO possessed an excellent antioxidant activity. The xanthine oxidase assay indicated that the anti-hyperuricemia potential was in a moderate level (IC50 = 526 µg/mL) as compared with the standard allopurinol. The EO exerted potent inhibition on growth of Raphanus sativus, Lactuca sativa, and two noxious weeds Echinochloa crus-galli, and Bidens pilosa, but in contrast, the growth of rice seedlings was promoted. Among the examined plants, the growth of the E. crus-galli root was the most inhibited, proposing that constituents found in EO may have potential for the control of the problematic paddy weed E. crus-galli. It was found that the EO of rice leaves contained rich phytochemicals, which were potent in antioxidants and gout treatment, as well as weed management. Findings of this study highlighted the potential value of rice leaves, which may provide extra benefits for rice farmers.

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Palm Olein as Renewable Raw Materials for Industrial and Pharmaceutical Products Applications: Chemical Characterization and Physicochemical Properties Studies

Advances in Materials Science and Engineering ◽

10.1155/2014/134063 ◽

2014 ◽

Vol 2014 ◽

pp. 1-5 ◽

Cited By ~ 3

Author(s):

Darfizzi Derawi ◽

Bashar Mudhaffar Abdullah ◽

Hasniza Zaman Huri ◽

Rahimi M. Yusop ◽

Jumat Salimon ◽

...

Keyword(s):

Chemical Modification ◽

Palm Olein ◽

Raw Materials ◽

Viscosity Index ◽

Chemical Characterization ◽

Pharmaceutical Products ◽

Raw Material ◽

Chemical Compositions ◽

Renewable Raw Materials ◽

Modification Process

Palm olein (POo) is widely produced as edible oil in tropical countries. POois considered as renewable raw material for the new industrial and pharmaceutical products synthesis based on its characterization. Palm olein was good on its viscosity index, oxidative stability, and flash and fire point. POocontained unsaturated triacylglycerols (TAGs): POO (33.3%); POP (29.6%) which plays an important role in chemical modification process to produce new industrial products. The double bond was detected on1H-NMR (5.3 ppm) and13C-NMR (130 ppm) spectra. The chemical compositions of POowere tested by using high performance liquid chromatography (HPLC) and gas chromatography (GC) techniques. This unsaturated oil is potentially to be used as renewable raw materials in chemical modification process to synthesise polyols, polyurethane, and biolubricant for industrial and pharmaceutical products application.

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