• Title/Summary/Keyword: Bioactive agents

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An In sight into Novel Drug Delivery System: In Situ Gels

  • Bashir, Rabiah;Maqbool, Mudasir;Ara, Irfat;Zehravi, Mehrukh
    • CELLMED
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    • v.11 no.1
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    • pp.6.1-6.7
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    • 2021
  • In situ gelling devices, as they enter the body, are dosage forms in the shape of the sol but turn into gel types under physiological circumstances. Transition from sol to gel is contingent on one or a mixture of diverse stimuli, such as transition of pH control of temperature, irradiation by UV, by the occurrence of certain ions or molecules. Such characteristic features may be commonly employed in drug delivery systems for the production of bioactive molecules for continuous delivery vehicles. The technique of in situ gelling has been shown to be impactful in enhancing the potency of local or systemic drugs supplied by non-parenteral pathways, increasing their period of residence at the absorption site. Formulation efficacy is further improved with the use of mucoadhesive agents or the use of polymers with both in situ gelling properties and the ability to bind with the mucosa/mucus. The most popular and common approach in recent years has provided by the use of polymers with different in situ gelation mechanisms for synergistic action between polymers in the same formulation. In situ gelling medicine systems in recent decades have received considerable interest. Until administration, it is in a sol-zone and is able to form gels in response to various endogenous factors, for e.g elevated temperature, pH changes and ions. Such systems can be used in various ways for local or systemic supply of drugs and successfully also as vehicles for drug-induced nano- and micro-particles. In this review we will discuss about various aspects about use of these in situ gels as novel drug delivery systems.

Overexpression of Capsular Polysaccharide Biosynthesis Protein in Lactobacillus plantarum P1 to Enhance Capsular Polysaccharide Production for Di-n-butyl Phthalate Adsorption

  • Liu, Wei-Bing;Lin, Zhi-Wei;Zhou, Ying;Ye, Bang-Ce
    • Journal of Microbiology and Biotechnology
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    • v.31 no.11
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    • pp.1545-1551
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    • 2021
  • Exopolysaccharides (EPSs) such as capsular polysaccharide (CPS) are important bioactive carbohydrate compounds and are often used as bioenrichment agents and bioabsorbers to remove environmental pollutants like di-n-butyl phthalate (DBP). Among the EPS-producing bacteria, lactic acid bacteria (LAB) have gained the most attention. As generally recognized as safe (GRAS) microorganisms, LAB can produce EPSs having many different structures and no health risks. However, EPS production by LAB does not meet the needs of large-scale application on an industrial scale. Here, the capA gene (encoding CPS biosynthesis protein) was overexpressed in Lactobacillus plantarum P1 to improve the production of EPSs and further enhance the DBP adsorption capability. Compared with P1, the CPS production in capA overexpressed strain was increased by 11.3 mg/l, and the EPS thickness was increased from 0.0786 ± 0.0224 ㎛ in P1 to 0.1160 ± 0.0480 ㎛ in P1-capA. These increases caused the DBP adsorption ratio of P1-capA to be doubled. Overall, the findings in this study provide a safe method for the adsorption and removal of DBP.

Anti-Inflammatory and Anti-Fibrotic Activities of Nocardiopsis sp. 13G027 in Lipopolysaccharides-Induced RAW 264.7 Macrophages and Transforming Growth Factor Beta-1-Stimulated Nasal Polyp-Derived Fibroblasts

  • Choi, Grace;Kim, Geum Jin;Choi, Hyukjae;Choi, Il-Whan;Lee, Dae-Sung
    • Microbiology and Biotechnology Letters
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    • v.49 no.4
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    • pp.543-551
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    • 2021
  • Nocardiopsis species produce bioactive compounds, such as antimicrobial and anti-cancer agents and toxins. However, no reports have described their anti-inflammatory and anti-fibrotic effects during nasal polyp (NP) formation. In this study, we investigated whether marine-derived bacterial Nocardiopsis sp. 13G027 exerts anti-inflammatory and anti-fibrotic effects on lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages and transforming growth factor (TGF)-β1-induced NP-derived fibroblasts (NPDFs). Nitric oxide (NO) and prostaglandin E2 (PGE2) levels were analyzed. Extract from Nocardiopsis sp. 13G027 significantly inhibited the upregulation of NO and PGE2 in LPS-activated RAW 264.7 macrophages. The expression of mitogen-activated protein kinases (MAPKs) and protein kinase B (Akt/PKB) in LPS-induced RAW 264.7 macrophages was evaluated; smooth muscle alpha-actin (α-SMA), collagen type I (Col-1), and fibronectin also phosphorylated small mothers against decapentaplegic (SMAD) 2 and 3 in TGF-β1-stimulated NPDFs. The Nocardiopsis sp. 13G027 extract suppressed the phosphorylation of MAPKs and Akt and the DNA-binding activity of activator protein 1 (AP-1). The expression of pro-fibrotic components such as α-SMA, Col-1, fibronectin, and SMAD2/3 was inhibited in TGF-β1-exposed NPDFs. These findings suggest that Nocardiopsis sp. 13G027 has the potential to treat inflammatory disorders, such as NP formation.

In-vitro Antimalarial Investigations and Molecular Docking Studies of Compounds from Trema orientalis L. (blume) Leaf Extract

  • Samuel, Babatunde Bolorunduro;Oluyemi, Wande Michael;Okedigba, Ayoyinka Oluwaseun
    • Natural Product Sciences
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    • v.28 no.2
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    • pp.45-52
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    • 2022
  • The identification of Plasmodium falciparum enoyl acyl-carrier protein reductase (pfENR) is considered as a potential biological target against malaria. Trema orientalis is considered a rich source of phytochemicals useful in malaria treatment. This study evaluated the in-vitro inhibitory activity of the extract and isolated compounds of T. orientalis leaf; the isolated compounds and the analogues of the most active compound were subjected to in-silico molecular docking studies on pfENR. The methanolic extract of T. orientalis was subjected to repeated chromatographic separation which led to the isolation of some compounds. The isolated compounds from the plant were examined for their antimalarial activity using β-hematin inhibition assay. Virtual screening via molecular docking and ADMET studies were conducted to gain insight into the mechanism of binding of ligand and to identify effective pfENR inhibitors. The isolated compounds and the analogues of the most active isolates were gotten from PubChem library for use in docking study. Hexacosanol and β-sitosterol showed inhibition of the β-hematin formation. The docking results showed that hexacosanol, β-sitosterol and the analogues of β-sitosterol displayed binding energy ranging between -6.1 kcal/mol and -11.6 kcal/mol. Sitosterol glucoside has the highest docking score. Some of the ligands showed more binding affinity than known bioactive compounds used as reference. Analogues of β-sitosterol has been shown to be potential inhibitors of pfENR, therefore, the findings from this study suggest that sitosterol glucoside and ergosterol peroxide could act as antimalarial agents after further lead optimisation investigations.

U.S. Whey Proteins and New Fractions as Ingredients in Functional Dairy Products and Innovative Nutraceuticals (기능성 유제품과 개선된 기능성 물질로서 미국에서 개발된 유청 단백질과 그 분획물)

  • Lagrange, V.
    • Journal of Dairy Science and Biotechnology
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    • v.16 no.2
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    • pp.106-118
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    • 1998
  • Whey is a natural product obtained during cheese production. With the advent of new technology, whey protein concentrates and whey fractions have become readily available and versatile food ingredients. Whey protein concentrates are highly functional ingredients that have gelling, emulsifying, whipping, water-binding and fat-replacement properties. New fractions derived from whey (such as alpha-lactalbumin, lactoferrin, lactoperoxidase and peptides) attract considerable interest worldwide because of their bioactive or health-enhancing properties. Some of these fractions also find new uses as natural antibiotic, natural preservative and immunity-enhancing agents. With the growth of the functional foods industry sector, an increasing number of manufacturers take advantage of whey's nutritional and functional benefits to develop successful new products. The United States is the world's largest single producer and exporter of whey products. In 1997, more than 1 million metric tons of whey products were manufacturers in the U.S.

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Nanoemulsion application in meat product and its functionality: review

  • Tri Ujilestari;Andi Febrisiantosa;Mohammad Miftakhus Sholikin;Rina Wahyuningsih;Teguh Wahyono
    • Journal of Animal Science and Technology
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    • v.65 no.2
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    • pp.275-292
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    • 2023
  • Nanotechnology in the food industry can increase the effectiveness of food ingredients. Nanotechnology can increase the bioavailability and absorption of bioactive compounds, enhance their stability, and improve the sensory quality of the product. Processed meat products are easily damaged due to bacterial activity. Advanced nanoemulsions as a meat preservative are nanoemulsions that can be used as preservative agents in meat products, particularly essential oil nanoemulsions, due to their antimicrobial and antioxidant properties. Its application is still limited to foods made from meat products. Therefore, this literature review examines nanoemulsion and its application in meat products and functionality improvement. Also, in the future, nanoemulsions in meat products must be made safe, and the government and businesses must work together to build consumer trust. It can be concluded that essential oil-based nanoemulsion has the potential to be used as an additive in meat products because it can kill bacteria, fight free radicals, improve flavor, and keep food fresh. Nanoemulsion is challenging in the meat industry because it can be toxic due to its tiny droplets (under 200 nm).

One-step phyto-mediated fabrication of silver nanoparticles and its anti-microbial properties

  • Velmurugan Palanivel;Sung-Chul Hong;Veera Ravi Arumugam;Sivakumar Subpiramaniyam;Pyong-In Yi;Seong-Ho Jang;Jeong-Min Suh;Eun-Sang Jung;Je-Sung Park
    • Advances in nano research
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    • v.14 no.4
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    • pp.391-397
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    • 2023
  • This manuscript describes the one-step eco-friendly green fabrication of silver nanoparticles (AgNPs) through the in-situ bio-reduction of an aqueous solution of silver nitrate using Syzygium aromaticum leaf extract. UV-vis spectroscopy shows a characteristic SPR peak around 442 nm. FTIR spectroscopy showed that the AgNPs were capped with bioactive phyto-molecules. TEM images revealed oval and spherical particles with a mean diameter of ~12.6 nm. XRD analysis revealed crystalline and face-cantered cubic AgNPs. The phytosynthesized AgNPs showed broad-spectrum anti-microbial activity against two foodborne pathogenic bacteria, Listeria monocytogenes and Staphylococcus aureus. The AgNPs showed a prominent ability to inhibit biofilms formed by L. monocytogenes and S. aureus in laboratory conditions through a crystal violet assay. The results suggest that the AgNPs could be a novel nanotool to develop effective antimicrobial and anti-biofilm agents in food preservation.

Alpha-Glucosidase Inhibitory Activity of Saponins Isolated from Vernonia gratiosa Hance

  • Pham Van Cong;Hoang Le Tuan Anh;Le Ba Vinh;Yoo Kyong Han;Nguyen Quang Trung;Bui Quang Minh;Ngo Viet Duc;Tran Minh Ngoc;Nguyen Thi Thu Hien;Hoang Duc Manh;Le Thi Lien;Ki Yong Lee
    • Journal of Microbiology and Biotechnology
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    • v.33 no.6
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    • pp.797-805
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    • 2023
  • Species belonging to the Vernonia (Asteraceae), the largest genus in the tribe Vernonieae (consisting of about 1,000 species), are widely used in food and medicine. These plants are rich sources of bioactive sesquiterpene lactones and steroid saponins, likely including many as yet undiscovered chemical components. A phytochemical investigation resulted in the separation of three new stigmastane-type steroidal saponins (1 - 3), designated as vernogratiosides A-C, from whole plants of V. gratiosa. Their structures were elucidated based on infrared spectroscopy (IR), one-dimensional (1D) and two-dimensional nuclear magnetic resonance (2D NMR), high-resolution electrospray ionization mass spectrometry (HR-ESI-MS), and electronic circular dichroism analyses (ECD), as well as chemical reactivity. Molecular docking analysis of representative saponins with α-glucosidase inhibitory activity was performed. Additionally, the intended substances were tested for their ability to inhibit α-glucosidase activity in a laboratory setting. The results suggested that stigmastane-type steroidal saponins from V. gratiosa are promising candidate antidiabetic agents.

Newly identified maltol derivatives in Korean Red Ginseng and their biological influence as antioxidant and anti-inflammatory agents

  • Jeong Hun Cho;Myoung Chong Song;Yonghee Lee;Seung-Taek Noh;Dae-Ok Kim;Chan-Su Rha
    • Journal of Ginseng Research
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    • v.47 no.4
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    • pp.593-603
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    • 2023
  • Background: Korean Red Ginseng is a major source of bioactive substances such as ginsenosides. Efficacy of red ginseng extract (RGE), which contains not only saponins but also various non-saponins, has long been studied. In the water-soluble component-rich fraction of RGE (WS), a byproduct generated in the process of extracting saponins from the RGE, we identified previously unidentified molecules and confirmed their efficacy. Methods: The RGE was prepared and used to produce WS, whose components were isolated sequentially according to their water affinity. The new compounds from WS were fractionized and structurally analyzed using nuclear magnetic resonance spectroscopy. Physiological applicability was evaluated by verifying the antioxidant and anti-inflammatory efficacies of these compounds in vitro. Results: High-performance liquid chromatography confirmed that the obtained WS comprised 11 phenolic acid and flavonoid substances. Among four major compounds from fractions 1-4 (F1-4) of WS, two compounds from F3 and F4 were newly identified in red ginseng. The analysis results show that these compound molecules are member of the maltol-structure-based glucopyranose series, and F1 and F4 are particularly effective for decreasing oxidative stress levels and inhibiting nitric oxide secretion, interleukin (IL)-1β and IL-6, and tumor necrosis factor-α. Conclusion: Our findings suggest that a few newly identified maltol derivatives, such as red ginseng-derived non-saponin in the WS, exhibit antioxidant and anti-inflammatory effects, making them viable candidates for application to pharmaceutical, cosmetic, and functional food materials.

Effect of platelet-rich plasma in Achilles tendon allograft in rabbits

  • Seok-Hong Park;Dong-Yub Kim;Won-Jae Lee;Min Jang;Seong Mok Jeong;Sae-Kwang Ku;Young-Sam Kwon;Sungho Yun
    • Journal of Veterinary Science
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    • v.25 no.2
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    • pp.22.1-22.15
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    • 2024
  • Background: Achilles tendon is composed of dense connective tissue and is one of the largest tendons in the body. In veterinary medicine, acute ruptures are associated with impact injury or sharp trauma. Healing of the ruptured tendon is challenging because of poor blood and nerve supply as well as the residual cell population. Platelet-rich plasma (PRP) contains numerous bioactive agents and growth factors and has been utilized to promote healing in bone, soft tissue, and tendons. Objective: The purpose of this study was to evaluate the healing effect of PRP injected into the surrounding fascia of the Achilles tendon after allograft in rabbits. Methods: Donor rabbits (n = 8) were anesthetized and 16 lateral gastrocnemius tendons were fully transected bilaterally. Transected tendons were decellularized and stored at -80℃ prior to allograft. The allograft was placed on the partially transected medial gastrocnemius tendon in the left hindlimb of 16 rabbits. The allograft PRP group (n = 8) had 0.3 mL of PRP administered in the tendon and the allograft control group (n = 8) did not receive any treatment. After 8 weeks, rabbits were euthanatized and allograft tendons were transected for macroscopic, biomechanical, and histological assessment. Results: The allograft PRP group exhibited superior macroscopic assessment scores, greater tensile strength, and a histologically enhanced healing process compared to those in the allograft control group. Conclusions: Our results suggest administration of PRP on an allograft tendon has a positive effect on the healing process in a ruptured Achilles tendon.