scholarly journals Synthesis, Characterization, Self-Assembly, and Irritation Studies of Polyglyceryl-10 Caprylates

Polymers ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 294 ◽  
Author(s):  
Guangyan Zhang ◽  
Chenhui Bao ◽  
Kaiqiao Fu ◽  
Yaolin Lin ◽  
Tianlong Li ◽  
...  
Keyword(s):  
Size Distribution ◽  
Self Assembly ◽  
Water Solubility ◽  
Light Transmittance ◽  
Narrow Particle Size Distribution ◽  
Esterification Reaction ◽  
Chemical Structures ◽  
Consumer Safety

1,4-dioxane should be less than or equal to 10 ppm in finished cosmetic products according to the recommendation of the Scientific Committee on Consumer Safety, but it is often generated as a by-product during the manufacturing process of poly(ethylene glycol) (PEG)-based derivatives. In order to avoid the possible risk caused by 1,4-dioxane, it might be a good choice for preparing cosmetic ingredients by using polyglycerin (PG) instead of PEG as a hydrophilic segment. In the present study, polyglyceryl-10 caprylates were synthesized by the esterification reaction between polyglycerin-10 and caprylic acid. FTIR and 1H NMR were utilized to confirm the chemical structures of the obtained polyglyceryl-10 caprylates. Light transmittance was availed to investigate the water solubility of polyglyceryl-10 caprylates. The self-assembly behavior, size, and size distribution of polyglyceryl-10 caprylates were investigated by dynamic light scattering. The makeup cleansing effect was also evaluated by in vitro and in vivo methods. Irritation was evaluated by hen’s egg test-chorioallantoic membrane assay (HET-CAM). Results showed that polyglyceryl-10 monocaprylate could self-assemble into nanoparticles in the water at the concentration range of 2.5–10 wt% with a transparent appearance. The diameter of formed nanoparticles was around 100 nm with a narrow particle size distribution around 0.1 at the concentration of 2.5 wt% or 5 wt%. Polyglyceryl-10 monocaprylate exhibited good removal effect against makeup and excellent removal efficacy against pen eyeliner. The irritation of polyglyceryl-10 monocaprylate evaluated by HET-CAM at the concentration of 4 wt% was moderate irritant (irritation score = 8.4), which was lower than that of PEG-6 caprylic/capric glycerides (severe irritant, irritation score = 14.1). Therefore, polyglyceryl-10 monocaprylate might be a promising cosmetic ingredient for transparent makeup removing water.

scholarly journals Investigating the Anti-Inflammatory Activity of Curcumin-Loaded Silica-Containing Redox Nanoparticles

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Khoa Minh Le ◽  
Nhu-Thuy Trinh ◽  
Vinh Dinh-Xuan Nguyen ◽  
Tien-Dat Van Nguyen ◽  
Thu-Ha Thi Nguyen ◽  
...  
Keyword(s):  
Chronic Inflammation ◽  
Self Assembly ◽  
Water Solubility ◽  
Nitroxide Radical ◽  
Pharmacokinetic Profile ◽  
Ros Scavenging ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Chronic inflammation is considered as one of the challenging diseases, and overproduction of reactive oxygen species (ROS) is strongly related to the onset of chronic inflammation. Therefore, antioxidant and anti-inflammatory approaches are particularly becoming suitable treatment and prevention of inflammation. Curcumin (CUR), a main component of turmeric extract, is well known as an effective agent in both antioxidant and anti-inflammatory activities; however, there are still some limitations of its use including poor water solubility, low bioavailability, and oxidation by ROS. Nanotechnology has been used as a drug delivery system, which is a promising approach in overcoming the aforementioned drawbacks of CUR; hence, it improves the antioxidant and anti-inflammatory effects of conventional medications. In this research, silica-containing redox nanoparticles (siRNP) were designed with the size of several tens of nanometers, prepared by self-assembly of an amphiphilic block copolymer consisting of drug absorptive silica moiety and ROS-scavenging nitroxide radical moiety in the hydrophobic segment. CUR was simply encapsulated into siRNP through the dialysis method, creating CUR-loaded siRNP (CUR@siRNP), which significantly improved the water solubility of CUR. The efficient antioxidant activity and anti-inflammatory effect of CUR@siRNP in vitro were also improved via 2,2-diphenyl-1-picrylhydrazyl assay and lipopolysaccharide-induced macrophage cell line activation, respectively. Oral administration of CUR@siRNP showed improvement in pharmacokinetic profile in vivo including AUC and Cmax values as compared to free CUR. Furthermore, the anti-inflammatory effect of nanoformulation was investigated in the colitis mouse model induced by dextran sodium sulfate.

In vitro and in vivo polysaccharides assembly: ultrastructural and cytochemical study of growing plant cell wall components.

1978 ◽  
Vol 36 (2) ◽  
pp. 434-435
Author(s):  
D. Reis ◽  
B. Vian ◽  
J. C. Roland
Keyword(s):  
Cell Wall ◽  
Self Assembly ◽  
Plant Cell Wall ◽  
Higher Plants ◽  
Three Dimensional ◽  
Cytochemical Study ◽  
Wall Components

Wall morphogenesis in higher plants is a problem still open to controversy. Until now the possibility of a transmembrane control and the involvement of microtubules were mostly envisaged. Self-assembly processes have been observed in the case of walls of Chlamydomonas and bacteria. Spontaneous gelling interactions between xanthan and galactomannan from Ceratonia have been analyzed very recently. The present work provides indications that some processes of spontaneous aggregation could occur in higher plants during the formation and expansion of cell wall.Observations were performed on hypocotyl of mung bean (Phaseolus aureus) for which growth characteristics and wall composition have been previously defined.In situ, the walls of actively growing cells (primary walls) show an ordered three-dimensional organization (fig. 1). The wall is typically polylamellate with multifibrillar layers alternately transverse and longitudinal. Between these layers intermediate strata exist in which the orientation of microfibrils progressively rotates. Thus a progressive change in the morphogenetic activity occurs.

Formation and Structure of Casein Micelles in Lactating Mammary Tissue

1970 ◽  
Vol 28 ◽  
pp. 150-151
Author(s):  
Robert J. Carroll ◽  
Marvin P. Thompson ◽  
Harold M. Farrell
Keyword(s):  
Size Distribution ◽  
G Protein ◽  
Milk Proteins ◽  
Mammary Tissue ◽  
Colloidal System ◽  
Casein Micelles ◽  
The Stability

Milk is an unusually stable colloidal system; the stability of this system is due primarily to the formation of micelles by the major milk proteins, the caseins. Numerous models for the structure of casein micelles have been proposed; these models have been formulated on the basis of in vitro studies. Synthetic casein micelles (i.e., those formed by mixing the purified αsl- and k-caseins with Ca2+ in appropriate ratios) are dissimilar to those from freshly-drawn milks in (i) size distribution, (ii) ratio of Ca/P, and (iii) solvation (g. water/g. protein). Evidently, in vivo organization of the caseins into the micellar form occurs in-a manner which is not identical to the in vitro mode of formation.

Programmable in vitro Co-Encapsidation of Guest Proteins Inside Protein Nanocages

2018 ◽  
Author(s):  
Noor H. Dashti ◽  
Rufika S. Abidin ◽  
Frank Sainsbury
Keyword(s):  
Self Assembly ◽  
Mammalian Cells ◽  
Resonance Energy Transfer ◽  
Resonance Energy ◽  
Super Resolution ◽  
Cell Engineering ◽  
Particle Analysis ◽  
Protein Cages

Bioinspired self-sorting and self-assembling systems using engineered versions of natural protein cages have been developed for biocatalysis and therapeutic delivery. The packaging and intracellular delivery of guest proteins is of particular interest for both <i>in vitro</i> and <i>in vivo</i> cell engineering. However, there is a lack of platforms in bionanotechnology that combine programmable guest protein encapsidation with efficient intracellular uptake. We report a minimal peptide anchor for <i>in vivo</i> self-sorting of cargo-linked capsomeres of the Murine polyomavirus (MPyV) major coat protein that enables controlled encapsidation of guest proteins by <i>in vitro</i> self-assembly. Using Förster resonance energy transfer (FRET) we demonstrate the flexibility in this system to support co-encapsidation of multiple proteins. Complementing these ensemble measurements with single particle analysis by super-resolution microscopy shows that the stochastic nature of co-encapsidation is an overriding principle. This has implications for the design and deployment of both native and engineered self-sorting encapsulation systems and for the assembly of infectious virions. Taking advantage of the encoded affinity for sialic acids ubiquitously displayed on the surface of mammalian cells, we demonstrate the ability of self-assembled MPyV virus-like particles to mediate efficient delivery of guest proteins to the cytosol of primary human cells. This platform for programmable co-encapsidation and efficient cytosolic delivery of complementary biomolecules therefore has enormous potential in cell engineering.

Flavonoids as P-gp Inhibitors: A Systematic Review of SARs

2019 ◽  
Vol 26 (25) ◽  
pp. 4799-4831 ◽  
Author(s):  
Jiahua Cui ◽  
Xiaoyang Liu ◽  
Larry M.C. Chow
Keyword(s):  
Molecular Mechanisms ◽  
Metastatic Cancer ◽  
Drug Candidates ◽  
Chemical Structures ◽  
Transporter Family ◽  
Promising Area ◽  
New Generation ◽  
Nontoxic Inhibitors

P-glycoprotein, also known as ABCB1 in the ABC transporter family, confers the simultaneous resistance of metastatic cancer cells towards various anticancer drugs with different targets and diverse chemical structures. The exploration of safe and specific inhibitors of this pump has always been the pursuit of scientists for the past four decades. Naturally occurring flavonoids as benzopyrone derivatives were recognized as a class of nontoxic inhibitors of P-gp. The recent advent of synthetic flavonoid dimer FD18, as a potent P-gp modulator in reversing multidrug resistance both in vitro and in vivo, specifically targeted the pseudodimeric structure of the drug transporter and represented a new generation of inhibitors with high transporter binding affinity and low toxicity. This review concerned the recent updates on the structure-activity relationships of flavonoids as P-gp inhibitors, the molecular mechanisms of their action and their ability to overcome P-gp-mediated MDR in preclinical studies. It had crucial implications on the discovery of new drug candidates that modulated the efflux of ABC transporters and also provided some clues for the future development in this promising area.

Novel Phytochemical Constituents and their Potential to Manage Diabetes

2020 ◽  
Vol 26 ◽  
Author(s):  
Shaik Ibrahim Khalivulla ◽  
Arifullah Mohammed ◽  
Kokkanti Mallikarjuna
Keyword(s):  
Natural Products ◽  
Large Population ◽  
World Health ◽  
In Vivo Studies ◽  
Antidiabetic Activity ◽  
Therapeutic Drug ◽  
Pharmacological Activities ◽  
Chemical Structures

Background: Diabetes is a chronic disease affecting a large population worldwide and stands as one of the major global health challenges to be tackled. According to World Health Organization, about 400 million are having diabetes worldwide and it is the seventh leading cause of deaths in 2016. Plant based natural products had been in use from ancient time as ethnomedicine for the treatment of several diseases including diabetes. As a result of that, there are several reports on plant based natural products displaying antidiabetic activity. In the current review, such antidiabetic potential compounds reported from all plant sources along with their chemical structures are collected, presented and discussed. This kind of reports are essential to pool the available information to one source followed by statistical analysis and screening to check the efficacy of all known compounds in a comparative sense. This kind of analysis can give rise to few numbers of potential compounds from hundreds, whom can further be screened through in vitro and in vivo studies, and human trails leading to the drug development. Methods: Phytochemicals along with their potential antidiabetic property were classified according to their basic chemical skeleton. The chemical structures of all the compounds with antidiabetic activities were elucidated in the present review. In addition to this, the distribution and their other remarkable pharmacological activities of each species is also included. Results: The scrutiny of literature led to identification of 44 plants with antidiabetic compounds (70) and other pharmacological activities. For the sake of information, the distribution of each species in the world is given. Many plant derivatives may exert antidiabetic properties by improving or mimicking the insulin production or action. Different classes of compounds including sulfur compounds (1-4), alkaloids (5-11), phenolic compounds (12-17), tannins (18-23), phenylpropanoids (24-27), xanthanoids (28-31), amino acid (32), stilbenoid (33), benzofuran (34), coumarin (35), flavonoids (36-49) and terpenoids (50-70) were found to be active potential compounds for antidiabetic activity. Of the 70 listed compounds, majorly 17 compounds are from triterpenoids, 13 flavonoids and 7 are from alkaloids. Among all the 44 plant species, maximum number (7) of compounds are reported from Lagerstroemia speciosa followed by Momordica charantia (6) and S. oblonga with 5 compounds. Conclusion: This is the first paper to summarize the established chemical structures of phytochemicals that have been successfully screened for antidiabetic potential and their mechanisms of inhibition. The reported compounds could be considered as potential lead molecules for the treatment of type-2 diabetes. Further, molecular and clinical trials are required to select and establish the therapeutic drug candidates.

Polyamines and Related Nitrogen Compounds in the Chemotherapy of Neglected Diseases Caused by Kinetoplastids

2018 ◽  
Vol 18 (5) ◽  
pp. 321-368 ◽  
Author(s):  
Juan A. Bisceglia ◽  
Maria C. Mollo ◽  
Nadia Gruber ◽  
Liliana R. Orelli
Keyword(s):  
Drug Targets ◽  
Redox Homeostasis ◽  
Cost Effective ◽  
Structural Features ◽  
Mammalian Host ◽  
Neglected Diseases ◽  
Nitrogen Compounds ◽  
Chemical Structures

Neglected diseases due to the parasitic protozoa Leishmania and Trypanosoma (kinetoplastids) affect millions of people worldwide, and the lack of suitable treatments has promoted an ongoing drug discovery effort to identify novel nontoxic and cost-effective chemotherapies. Polyamines are ubiquitous small organic molecules that play key roles in kinetoplastid parasites metabolism, redox homeostasis and in the normal progression of cell cycles, which differ from those found in the mammalian host. These features make polyamines attractive in terms of antiparasitic drug development. The present work provides a comprehensive insight on the use of polyamine derivatives and related nitrogen compounds in the chemotherapy of kinetoplastid diseases. The amount of literature on this subject is considerable, and a classification considering drug targets and chemical structures were made. Polyamines, aminoalcohols and basic heterocycles designed to target the relevant parasitic enzyme trypanothione reductase are discussed in the first section, followed by compounds directed to less common targets, like parasite SOD and the aminopurine P2 transporter. Finally, the third section comprises nitrogen compounds structurally derived from antimalaric agents. References on the chemical synthesis of the selected compounds are reported together with their in vivo and/or in vitro IC50 values, and structureactivity relationships within each group are analyzed. Some favourable structural features were identified from the SAR analyses comprising protonable sites, hydrophobic groups and optimum distances between them. The importance of certain pharmacophoric groups or amino acid residues in the bioactivity of polyamine derived compounds is also discussed.

Potential Antiulcer Agents From Plants: A Comprehensive Review

2019 ◽  
Vol 5 (3) ◽  
pp. 170-231
Author(s):  
Minky Mukhija ◽  
Bhuwan Chandra Joshi
Keyword(s):  
Medicinal Plants ◽  
Developed Countries ◽  
Scientific Data ◽  
Antiulcer Activity ◽  
Peptic Ulcers ◽  
Comprehensive Review ◽  
Chemical Structures ◽  
Mucosal Thickness

Background: Peptic ulcer is a deep gastrointestinal erosion disorder that involves the entire mucosal thickness and can even penetrate the muscular mucosa. Nowadays, several plants and compounds derived from it have been screened for their antiulcer activity. In the last few years, there has been an exponential growth in the field of herbal medicine. This field has gained popularity in both developing and developed countries because of their natural origin and less side effects. Objective: This review aims to provide a comprehensive summary of currently available knowledge of medicinal plants and phytoconstituents reported for their anti-ulcer properties. Methods: The worldwide accepted database like SCOPUS, PUBMED, SCIELO, NISCAIR, ScienceDirect, Springerlink, Web of Science, Wiley, SciFinder and Google Scholar were used to retrieve available published literature. Results: A comprehensive review of the present paper is an attempt to list the plants with antiulcer activity. The review narrates the dire need to explore potential chemical moieties that exert an antiulcer effect, from unexploited traditional plants. Furthermore, the present study reveals the intense requirement to exploit the exact mechanism through which either the plant extracts or their active constituents exhibit their antiulcer properties. Conclusion: This article is the compilation of the plants and its constituents reported for the treatment of peptic ulcers. The Comprehensive data will surely attract the number of investigators to initiate further research that might lead to the drugs for the treatment of ulcers. As sufficient scientific data is not available on plants, most of the herbals cannot be recommended for the treatment of diseases. This can be achieved by research on pure chemical structures derived from plants or to prepare new lead compounds with proven beneficial preclinical in vitro and in vivo effects. However, a lot remains to be done in further investigations for the better status of medicinal plants.

scholarly journals In Vitro and In Vivo Antifungal Activity of Sorbicillinoids Produced by Trichoderma longibrachiatum

2021 ◽  
Vol 7 (6) ◽  
pp. 428
Author(s):  
Men Thi Ngo ◽  
Minh Van Nguyen ◽  
Jae Woo Han ◽  
Myung Soo Park ◽  
Hun Kim ◽  
...  
Keyword(s):  
Late Blight ◽  
Culture Filtrate ◽  
Fungal Pathogens ◽  
Gray Mold ◽  
Trichoderma Longibrachiatum ◽  
Chemical Structures ◽  
Natural Agents ◽  
Blight Disease

In the search for antifungal agents from marine resources, we recently found that the culture filtrate of Trichoderma longibrachiatum SFC100166 effectively suppressed the development of tomato gray mold, rice blast, and tomato late blight. The culture filtrate was then successively extracted with ethyl acetate and n-butanol to identify the fungicidal metabolites. Consequently, a new compound, spirosorbicillinol D (1), and a new natural compound, 2′,3′-dihydro-epoxysorbicillinol (2), together with 11 known compounds (3–13), were obtained from the solvent extracts. The chemical structures were determined by spectroscopic analyses and comparison with literature values. The results of the in vitro antifungal assay showed that of the tested fungal pathogens, Phytophthora infestans was the fungus most sensitive to the isolated compounds, with MIC values ranging from 6.3 to 400 µg/mL, except for trichotetronine (9) and trichodimerol (10). When tomato plants were treated with the representative compounds (4, 6, 7, and 11), bisvertinolone (6) strongly reduced the development of tomato late blight disease compared to the untreated control. Taken together, our results revealed that the culture filtrate of T. longibrachiatum SFC100166 and its metabolites could be useful sources for the development of new natural agents to control late blight caused by P. infestans.

scholarly journals Development of In Situ Self-Assembly Nanoparticles to Encapsulate Lopinavir and Ritonavir for Long-Acting Subcutaneous Injection

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 904
Author(s):  
Irin Tanaudommongkon ◽  
Asama Tanaudommongkon ◽  
Xiaowei Dong
Keyword(s):  
Sustained Release ◽  
Trough Concentration ◽  
Self Assembly ◽  
Subcutaneous Injection ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Long Acting

Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. Here, a long-acting subcutaneous injection of lopinavir (LPV) in combination with ritonavir (RTV) using in situ self-assembly nanoparticles (ISNPs) was developed to potentially overcome adherence barriers. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. LPV/RTV ISNPs were 167.8 nm in size, with a polydispersity index of less than 0.35. The entrapment efficiency was over 98% for both LPV and RTV, with drug loadings of 25% LPV and 6.3% RTV. A slow release rate of LPV was observed at about 20% on day 5, followed by a sustained release beyond 14 days. RTV released faster than LPV in the first 5 days and slower than LPV thereafter. LPV trough concentration remained above 160 ng/mL and RTV trough concentration was above 50 ng/mL after 6 days with one subcutaneous injection. Overall, the ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies.

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