• Biomolecules & Therapeutics
• /
• v.28 no.1
• /
• pp.83-91
• /
• 2020

Tryptamines are monoamine alkaloids with hallucinogenic properties and are widely abused worldwide. To hasten the regulations of novel substances and predict their abuse potential, we designed and synthesized four novel synthetic tryptamine analogs: Pyrrolidino tryptamine hydrochloride (PYT HCl), Piperidino tryptamine hydrochloride (PIT HCl), N,N-dibutyl tryptamine hydrochloride (DBT HCl), and 2-Methyl tryptamine hydrochloride (2-MT HCl). Then, we evaluated their rewarding and reinforcing effects using the conditioned place preference (CPP) and self-administration (SA) paradigms. We conducted an open field test (OFT) to determine the effects of the novel compounds on locomotor activity. A head-twitch response (HTR) was also performed to characterize their hallucinogenic properties. Lastly, we examined the effects of the compounds on 5-HTR1a and 5-HTR2a in the prefrontal cortex using a quantitative real-time polymerase chain reaction (qRT-PCR) assay. None of the compounds induced CPP in mice or initiated SA in rats. PYT HCl and PIT HCl reduced the locomotor activity and elevated the 5-HTR1a mRNA levels in mice. Acute and repeated treatment with the novel tryptamines elicited HTR in mice. Furthermore, a drug challenge involving a 7-day abstinence from drug use produced higher HTR than acute and repeated treatments. Both the acute treatment and drug challenge increased the 5-HTR2a mRNA levels. Ketanserin blocked the induced HTR. Taken together, the findings suggest that PYT HCl, PIT HCl, DBT HCl, and 2-MT HCl produce hallucinogenic effects via 5-HTR2a stimulation, but may have low abuse potential.

• Archives of Pharmacal Research
• /
• v.26 no.8
• /
• pp.585-590
• /
• 2003

Activity-guided fractionation of the EtOAc-soluble extract of the whole plants of Sida acuta using a bioassay based on the induction of quinone reductase (OR) in cultured Hepa 1c1c7 mouse hepatoma cells, led to the isolation of ten active compounds of previously known structure, quindolinone (1), cryptolepinone (2), 11-methoxyquindoline (3), N-trans-feruloyltyramine (4), vomifoliol (5), loliolide (6), 4-ketopinoresinol (7), scopoletin (8), evofolin-A (9), and evofolin-B (10), along with five inactive compounds of known structure, ferulic acid, sinapic acid, syringic acid, ($\pm$)-syringaresinol, and vanillic acid. These isolates were identified by physical and spectral data measurement. A new derivative of quindolinone, 5,10-dimethylquindolin-11-one (1a) was synthesized and characterized spectroscopically. Of the active substances, compounds 1-3 and 1a exhibited the most potent QR activity, with observed CD (concentration required to double induction) values ranging from 0.01 to 0.12 $\mu$ g/mL. Six compounds were then evaluated in a mouse mammary organ culture assay, with cryptolepinone (2), N-trans-feruloyltyramine (4), and 5,10-dimethylquindolin-11-one (1a) found to exhibit 83.3, 75.0, and 66.7% inhibition of 7,12-dimethylbenz[a]anthracene-induced preneoplastic lesions, respectively, at a dose of 10 $\mu\textrm{g}$/mL.

• Journal of Life Science
• /
• v.31 no.9
• /
• pp.862-872
• /
• 2021

Recent studies on synthesis of metallic nanomaterials such as silver (Ag), gold (Au), platinum (Pt), cerium (Ce), zinc (Zn), and copper (Cu) nanoparticles (NPs) using plants and microbes are attracted researchers for their wide range of applications in the field of biomedical sciences. The plant contains abundant of bioactive contents such as flavonoids, alkaloids, saponins, steroids tannins and nutritionals components. Similarly, microbes produce bioactive metabolites, proteins and secretes valuable chemicals such as color pigments, antibiotics, and acids. Recently reported, biogenic synthesis of NPs in non-hazardous way and are promising candidates for biomedical applications such as antibacterial, antifungal, anti-cell proliferative and anti-plasmodia activity. All those activities are dose dependent, along with their shape and size also matters on potential of NPs. Microbes and plants are great source of metabolites, those useful in biomedical field, such metabolites or chemicals involved in synthesis of NPs in an ecofriendly way. NPs synthesized using microbes or plant materials are reveals more non-toxic, facile, and cost-effective compare to chemically synthesized NPs. In present review we are focusing on NPs synthesis using biological agents such as microbes (bacteria, fungi and algae) and plant, characterization using different techniques and their antibacterial applications on pathogenic Gram-positive and Gram-negative organisms.

• The Korean Journal of Pain
• /
• v.34 no.2
• /
• pp.210-216
• /
• 2021

Background: Postherpetic neuralgia (PHN) is the most common complication of acute herpes zoster. The treatment of PHN remains a challenge for clinical pain management. Despite the effectiveness of anticonvulsants, antidepressants, and lidocaine patches in reducing PHN, many patients still face intractable pain disorders. In this randomized controlled study, we evaluated whether hydromorphone through intravenous patient-controlled analgesia (IV PCA) was effective in relieving PHN. Methods: Patients with PHN were randomly divided into two groups, one group received oral pregabalin with IV normal saline, another group received oral pregabalin with additional IV PCA hydromorphone for two weeks. Efficacy was evaluated at 1, 4, and 12 weeks after the end of the treatments. Results: Two hundred and one patients were followed up for 12 weeks. After treatment, numerical rating scale (NRS) score of patients in the hydromorphone group was significantly lower than that of the control group, and the difference of NRS scores between the two groups was statistically significant at 4 and 12 weeks after treatment. The frequency of breakthrough pain in the hydromorphone group was significantly lower than that in the control group 1 and 4 weeks after treatment. After treatment, the quality of sleep in the hydromorphone group was significantly improved compared with the control group. The most common adverse reactions in the hydromorphone group were dizziness and nausea, with no significant respiratory depression. Conclusions: IV PCA hydromorphone combined with oral pregabalin provides superior pain relief in patients with PHN, which is worthy of clinical application and promotion.

• Food Science and Preservation
• /
• v.31 no.2
• /
• pp.307-314
• /
• 2024

Broussonetia kazinoki twig extract (BKT) is recognized for its antioxidant and anti-cancer effects and natural whitening properties. So, it is used as a raw material for cosmetics. B. kazinoki twig is also an edible raw material. B. kazinoki has been used in Asia for paper production and oriental medicine, has anti-diabetic effects, and contains various flavonoids and alkaloids. In this study, to evaluate the efficacy of BKT on allergic skin inflammatory responses, we investigated its effects on factors related to skin inflammation in HaCaT keratinocytes and allergic responses in RBL-2H3 cells. There was no cytotoxicity of the 70% ethanol extract against HaCaT and RBL-2H3 cells. In HaCaT cells, stimulation with tumor necrosis factor-alpha (TNF-𝛼) and interferon-gamma (IFN-𝛾) increased the production of several chemokines, including thymus and activation-regulated chemokine (TARC), macrophage-derived chemokine (MDC), and regulated on activation, normal T cell expressed and secreted (RANTES). However, it was observed that this elevation was notably mitigated in a concentration-dependent manner upon treatment with BKT. Furthermore, BKT treatment demonstrated a significant reduction of 𝛽-hexosaminidase and inflammatory cytokines TNF-𝛼 and IL-4 in IgE-sensitized RBL-2H3 cells. Thus, it is expected that BKT can be used as a natural cosmetic and food ingredient that effectively suppresses allergic inflammatory reactions.

• Journal of Korean Medicine for Obesity Research
• /
• v.24 no.1
• /
• pp.94-101
• /
• 2024

Herbal medicine (HM)-containing Ephedra Sinica (ES) has been associated with false-positive amphetamine immunoassay (FP IA) results. This study retrospectively evaluated the effects of dose, duration, and withdrawal instructions on FP IA and the safety of HM-containing ES at a clinic in Seoul from 2022 to 2023. The study included 6 patients in the FP IA group and 5 patients in the withdrawal instruction negative (Neg) group. The pre-test ephedrine alkaloids dose in the FP IA group was 95.17±31.90 mg, compared with 88.6±20.43 mg in the Neg group. The FP IA group had taken HM for 226.67±152.87 days before testing, and testing was performed while taking HM. In contrast, the Neg group had taken HM for 147.6±23.49 days and had 5.4±1.50 days of withdrawal period before the test following instructions of Korean medicine doctors. All adverse events (AEs) were moderate in severity, and the number of occurrences was similar: 5 in the FP IA group and 7 in the Neg group. AEs included constipation, insomnia (3 cases each), and palpitations (2 cases). The results of this study show that ES-induced FP IA can be resolved with withdrawal instructions and ES can be safely prescribed and administered by Korean medicine doctors. Further studies are needed to determine how to prevent FP IA after taking ES.

• Journal of Life Science
• /
• v.34 no.9
• /
• pp.647-655
• /
• 2024

The synthesis of cerium oxide nanoparticles (nanoceria, CeO₂) has received significant attention across scientific and technological disciplines in the last decade. This article explores an overview of the green synthesis method and the antibacterial activity of nanoceria. The utilization of biological materials, such as plants and microorganisms, in the synthesis of nanoceria, has gained attention as an ecofriendly approach. Plants are rich in phytochemicals, including alkaloids, flavonoids, phenols, proteins, and other nutritious components. Likewise, microorganisms generate bioactive metabolites, pigments, enzymes, proteins, acids, and antibiotics. The phytochemicals and metabolites are involved in the reduction of metal salt into nanoceria and provide stability to synthesized nanoparticles. Nanoceria synthesis using plants and microorganisms is facile and ecofriendly, and synthesized nanoceria are biocompatible. Many biomedical applications of nanoceria have been reported, including those that are anticancer, anti-inflammatory, larvicidal, enzyme inhibiting, antibiofilm, and antimicrobial. However, in this review, we focused on and described in detail the antibacterial potential of nanoceria. The antibacterial activity of nanoceria occurs due to excessive reactive oxygen species generation, the impairment of the cell membrane, and the inhibition of cellular mechanisms. Ultimately, this review's primary goal is to provide readers with a logical understanding of the significant achievements of nanoceria as a cutting-edge therapeutic agent for treating a range of microbial pathogens and combating other diseases.

• Journal of Food Hygiene and Safety
• /
• v.13 no.4
• /
• pp.377-382
• /
• 1998

This study was carried out to measure the contents of moisture, crude ash, crude fat, total amino acid, with amino acid composition, vitamin C, ${\beta}-carotene$, vitamin E, total catechins, EGCG, EGC, ECG, EC, GA, caffeine, theobromine and theophylline of the green tea I, II, III, oolong, and black tea. The content of crude fat of green tea I, II, III, oolong, and black teas was 1.1, 2.5, 4.9, 0.8 and 1.2% respectively, total amino acid content was 0.87, 0.78, 0.60, 0.63 and 1.05% respectively, and theanine content was 0.52, 0.48, 0.31, 0.41 and 0.61%, respectively. Total amino acid content of green tea increased in the order of green tea I> green tea II> green tea III, and among the teas, the content of theanine was the highest in the amino acids present. The content of vitamin C of green teal, II, III, oolong, and black tea was 101.6, 87.5, 95.9, 99.1 and 108.0 mg%, respectively, ${\beta}-carotene$ content was 270, 268, 481, 80 and 181 ppm, respectively. Among the ${\alpha}-,\;{\beta}-,\;{\gamma}-\;and\;{\delta}-tocopherol$, the content of ${\alpha}-tocopherol$ was the highest in vitamin E present, and ${\beta}-\;and\;{\delta}-tocopherol$ were not detected in the samples of green teal, II, III, oolong, and black teas. The total catechins of green teal, II, III, oolong, and black teas was 10.5, 10.4, 7.2, 8.4 and 1.8% respectively, and among them, EGCG content was the highest. The content of EGC increased in the order of green tea I > green tea III > green tea II > oolong tea> black tea. The contents EGCG and ECG increased in the order of oolong tea> green tea I > green tea II> green tea III> black tea, and the highest contents of EGCG and ECG were observed in the samples of oolong tea. The content of GA was 0.01, 0.02, 0.05, 0.13 and 0.31%, respectively, and the highest contents of GA, caffeine and theobromine were observed in the sample of black tea. The highest content of theophylline, however, was observed in the sample of green tea I.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.37 no.11
• /
• pp.1401-1407
• /
• 2008

1-Deoxynojirimycin (DNJ) is a strong $\alpha$-glucosidase inhibitor which inhibits hyperglycemia in animals. To select the Bacillus strains highly producing DNJ, 4,000 strains were isolated from soil and grain samples. By the inhibitory activity against $\alpha$-glucosidase, nine Bacillus strains were selected and then identified by 16S rDNA sequencing. B. subtilis S10 was finally selected as the best strain for the production of DNJ. Various carbon sources and nitrogen sources in culture medium were evaluated for the highest production of DNJ. As the results, the optimized concentration of carbon source and nitrogen source was 1.0% galactose and 1.6% polypeptone and the concentration of DNJ produced was 0.75 g/L. The effect of culture supernatant of B. subtilis S10 on lowering blood glucose level was investigated in streptozotocin (STZ)-induced diabetic mice model. Mice were randomly assigned to control group (saline) and three test groups such as acarbose group, silkworm powder group and B. subtilis S10 group. After eight-week oral feeding, blood glucose levels of the B. subtilis S10 and silkworm powder groups were respectively $209.1{\pm}19.6\;mg/dL$ (59.1%) and $208.6{\pm}39.8\;mg/dL$ (59.0%) lower than $510{\pm}10\;mg/dL$ of the control group. These results indicated that the culture supernatant of B. subtilis S10 was able to reduce the blood glucose level in STZ-induced diabetic mice.

• Journal of Food Hygiene and Safety
• /
• v.25 no.4
• /
• pp.410-417
• /
• 2010

Various functional foods, marketing health and functional effects, have been distributed in the market. These products, being in forms of foods, tablets, and capsules, are likely to be mistaken as drugs. In addition, non-experts may sell these as foods, or use these for therapy. Efforts for creating health food regulations or building regulatory system for improving the current status of functional foods have been made, but these have not been communicated to consumers yet. As a result, problems of circulating functional foods for therapy or adding illegal medical to such products have persisted, which has become worse by internet media. The cause of this problem can be categorized into (1) product itself and (2) its use, but in either case, one possible cause is lack of communications with consumers. Potential problems that can be caused by functional foods include illegal substances, hazardous substances, allergic reactions, considerations when administered to patients, drug interactions, ingredients with purity or concentrations too low to be detected, products with metabolic activations, health risks from over- or under-dose of vitamin and minerals, and products with alkaloids. (Journal of Health Science, 56, Supplement (2010)). The reason why side effects related to functional foods have been increasing is that under-qualified functional food companies are exaggerating the functionality for marketing purposes. KFDA has been informing consumers, through its web pages, to address the above mentioned issues related to functional foods, but there still is room for improvement, to promote proper use of functional foods and avoid drug interactions. Specifically, to address these issues, institutionalizing to collect information on approved products and their side effects, settling reevaluation systems, and standardizing preclinical tests and clinical tests are becoming urgent. Also to provide crucial information, unified database systems, seamlessly aggregating heterogeneous data in different domains, with user interfaces enabling effective one-stop search, are crucial.