• Title/Summary/Keyword: Alkaloids

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Studies on the Processing of Crude Drugs(VIII): The Changes of Physico-chemical Parameter and Biological Activities by Processing of Evodia Fruit (한약수치에 관한 연구(제 8보): 오수유 탕포법)

  • Park, Sung-Hwan;Lee, Woo-Jung;Choi, Hyuck-Jai;Song, Bo-Whan;Kim, Dong-Hyun;Kim, Nam-Jae
    • Korean Journal of Pharmacognosy
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    • v.36 no.2 s.141
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    • pp.102-108
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    • 2005
  • We have studied the physico-chemical change and pharmacological transformation of traditional herbal medicines with processing. Evodia fruit (EF) has processed for the purpose of detoxification and reduction of its bitter taste. There are various methods of processing EF in Oriental medicinal reference. Among them, we processed EF according to the method of Sang-han theory, the most famous medicinal reference. We processed EF with washing in hot water, and then dried. Processed EFs(PEFs) were prepared according to the above procedure through repetition of 1,3,5 and 7 times respectively. The contents of weight loss, water extract, diluted ethanol extract, ether extract, total ash, acid insoluble ash, alkaloids and limonin in non-processed EF (NPEF) and PEFs were examined. The weight loss, and contents of water extract and dilute ethanol extract in PEF showed decrease in proportion to increase of washing time, while the contents of ether extract, total ash and acid insoluble ash showed little change as compared with those of NPEF. And the content of evodiamine and rutaecarpine was not changed distinctly. However, the content of limonin decreased in the final processed material in proportion to increase of washing times with hot water. And the intense of bitter taste in PEF was also reduced. These results were ascribed to the flowing-out of the water-soluble portion. The biological activities of NPEF and PEF were also investigated. In the test of DPPH scavenging effect, xanthine oxidase inhibition effect and TBA-Rs effect, PEF was more effective than NPEF in vitro. Also, both NPEF and PEF showed potent analgesic and anti-inflammatory effects against in mice. Especially, PEF by 3 times washing with hot water was more effective than other PEFs. From these results, it is considered that PEF should be prepared by 3 times washing with hot water.

Antioxidant and Antiaging Assays of Hibiscus sabdariffa Extract and Its Compounds

  • Widowati, Wahyu;Rani, Andani Puspita;Hamzah, R. Amir;Arumwardana, Seila;Afifah, Ervi;Kusuma, Hanna Sari W.;Rihibiha, Dwi Davidson;Nufus, Hayatun;Amalia, Annisa
    • Natural Product Sciences
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    • v.23 no.3
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    • pp.192-200
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    • 2017
  • Skin aging is a complex biological process due to intrinsic and extrinsic factors. Free radical oxidative is one of extrinsic factors that induce activation of collagenase, elastase and hyaluronidase. Natural product from plants has been used as antioxidant and antiaging. This study aimed to evaluate antioxidant and antiaging properties of Hibiscus sabdariffa extract (HSE) and its compounds including myricetin, ascorbic acid, and ${\beta}$ carotene. The phytochemical of H. sabdariffa was determined using modified Farnsworth method and presence of phenols, flavonoids and tannins were in moderate content, whereas triterpenoids and alkaloids were in low content. Total phenolic content performed using Folin-Ciocalteu method, was $23.85{\mu}gGAE/mg$. Quantitative analysis of myricetin, ${\beta}-carotene$, and ascorbic acid of HSE was performed with Ultra-High Performance Liquid Chromatography (UHPLC) that shows $78.23{\mu}g/mg$ myricetin, $0.034{\mu}g/mg$ ${\beta}-carotene$, whilst ascorbic acid was not detected. HSE has lower activity on DPPH ($IC_{50}=195.73{\mu}g/mL$) compared to ${\beta}-carotene$, the lowest in ABTS assay ($IC_{50}=74.58{\mu}g/mL$) and low activity in FRAP assay ($46.24{\mu}MFe(II)/{\mu}g\;$) compared to myricetin, ${\beta}-carotene$. Antiaging was measured through inhibitory activity of collagenase, elastase, and hyaluronidase. HSE had weakest collagenase inhibitory activity ($IC_{50}=750.33{\mu}g/mL$), elastase inhibitory activity ($103.83{\mu}g/mL$), hyaluronidase inhibitory activity ($IC_{50}=619.43{\mu}g/mL$) compared to myricetin, ${\beta}-carotene$, and ascorbic acid. HSE contain higher myricetin compared to ${\beta}-carotene$. HSE has moderate antioxidants and lowest antiaging activities. Myricetin is the most active both antioxidant and antiaging activities.

Quali-Quantitative Analysis of Flavonoids for Mulberry Leaf and Fruit of 'Suhyang'

  • Ju, Wan-Taek;Kwon, O-Chul;Lee, Min-Ki;Kim, Hyun-Bok;Sung, Gyoo-Byung;Kim, Yong-Soon
    • Korean Journal of Environmental Agriculture
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    • v.36 no.4
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    • pp.249-255
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    • 2017
  • BACKGROUND: Globally, mulberry (Morus sp.) is exploited for feeding leaf to silkworms in order to obtain silk fiber or for animal feedstock production. Also, mulberry fruit is known to a by-product that was produced from mulberry tree after harvesting leaves for silkworm rearing, as a yield and consumption of mulberry fruit was increased, it has been fixing to a newincome crop. Mulberry leaves and fruits are used for the health benefits of human beings. Mulberry contains various bioactive components, such as alkaloids and flavonoids. Mulberry flavonoids are an important part of the diet because of their effects on human nutrition. The flavonoids in mulberry leaf and fruit of 'Suhyang'(Morus alba L.) were determined. METHODS AND RESULTS: Flavonoids for mulberry leaf and fruit of 'Suhyang' were analysed using ultrahigh performance liquid chromatography coupled with diode array detection and quadrupole time-of-flight mass spectrometry (UPLC-DAD-QTOF/MS)technique. An UPLC-DAD-QTOF/MS system was used, and identification of mulberry leaves constituents was carried out on the basis of the complementary information obtained from LC spectra, MS ions, and MS/MS fragments. The mulberry leaf (16 flavonoids) and fruit (9 flavonoids) were isolated and analyzed from Suhyang using UPLC-DAD-QTOF/MS chromatogram. To the best of our knowledge, Quercetin 3-O-(6"-O-malonyl) glucoside and quercetin 3-O-rutinoside (rutin) was detected on the highest content in leaf and fruit, respectively and further research will be devoted to evaluate their biological activity. CONCLUSION: Obtaining information about the concentration of functional materials in mulberry leaves could contribute to the development and promotion of processed, functional products and offer possible industrial use of 'Suhyang', holding promises to enhance the overall profitability of sericulture.

1-Deoxynojirimycin Content and Blood Glucose-Lowering Effect of Silkworm (Bombyx mori) Extract Powder

  • Ryu, Kang-Sun;Lee, Heui-Sam;Kim, Kee-Young;Kim, Mi-Ja;Sung, Gyoo-Byung;Ji, Sang-Deok;Kang, Pil-Don
    • International Journal of Industrial Entomology and Biomaterials
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    • v.27 no.2
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    • pp.237-242
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    • 2013
  • We investigated the 1-deoxynojirimycin (1-DNJ) content of extracts from silkworm larvae at each developmental stage within three silkworm varieties. We also compared the content of the following polyhydroxylated alkaloids in the silkworm extracts: 1-DNJ, fagomine, and 1,4-dideoxy-1,4-imino-d-arabinitol (DAB). In addition, we evaluated the glucose-lowering effects of silkworm extract powder in db/db mice. The 1-DNJ content was the highest in Yeonnokjam $5^{th}$ instar $3^{rd}$ d larvae and Hansaengjam $5^{th}$ instar $3^{rd}$ d larvae, which contained 18.4 mg/100 g dry weight and 18.3 mg/100 g dry weight, respectively. The $5^{th}$ instar $3^{rd}$ d larvae exhibited a higher content of 1-DNJ than that of $5^{th}$ instar $5^{th}$ d larvae among all varieties. The glucose-lowering effects of silkworm extracts and Yeonnokjam powder were tested on db/db mice, and the blood glucose levels were found to decrease significantly in the YR70 group. Silkworm extracts (180 mg/kg, 90 mg/kg, 45 mg/kg, and 22.5 mg/kg) and acarbose (50 mg/kg) were administered orally for 4 wk. Changes in water intake were not statistically significant between control and silkworm extract-treated groups. Compared to the control group, blood glucose levels in the silkworm extract powder-treated group decreased in the 22.5 mg/kg/d group after being administered for 4 wk. This decrease was statistically significant. Furthermore, biochemical changes in the AST(Aspartate aminotransferase), ALT(Alanine aminotransferase), TCHO(Total Cholesterol), TG(Triglyceride), LDL(Low density lipoprotein), and HDL(High density lipoprotein) levels in blood were not observed. However, statistically significant decreases in blood GLU in the 22.5 mg/kg/d group compared to that of the control group occurred. In addition, the epididymal fat weight of the silkworm extract powder-treated group decreased significantly in both the 22.5 mg/kg/d group and 180 mg/kg/d group compared to that of the control group, but there were no statistically significant changes in perirenal fat weight. These results demonstrate that silkworm extracts inhibit changes in blood glucose levels in model diabetic mice.

Construction and Optimization of Selective Membrane Electrodes for Determination of Doxepin Hydrochloride in Pharmaceutical Preparations and Biological Fluids (약의 조제와 생물학적 유체에서 독스핀 하이드로클로라이드의 확인을 위한 선택적 막 전극의 구성과 최적화)

  • El-Tohamy, Maha;Razeq, Sawsan;El-Maamly, Magda;Shalaby, Abdalla
    • Journal of the Korean Chemical Society
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    • v.54 no.2
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    • pp.198-207
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    • 2010
  • The construction and performance characteristics of doxepin hydrochloride selective electrodes were developed. Three types of electrodes: plastic membrane I, coated wire II, and coated graphite rod III were constructed based on the incorporation of doxepin hydrochloride with ammonium reineckate. The influence of membrane composition, kind of plasticizer, pH of the test solution, soaking time, and foreign ions on the electrodes was investigated. The electrodes showed a Nernstain response with a mean slope of 57.41 ${\pm}$ 0.5, 56.22 ${\pm}$ 0.2 and 52.88 ${\pm}$ 0.7 mV at $25^{\circ}C$ for electrode I, II and III respectively, over Doxepin hydrochloride concentration range from $1{\times}10^{-2}-1{\times}10^{-6}M$, $5{\tims}10^{-2}-1{\times}10^{-6}M$ and $1{\times}10^{-3}-5{\times}10^{-6}M$, and with a detection limit $5.0{\times}10^{-7}M$, $6.3{\times}10^{-7}M$ and $2.5{\times}10^{-6}M$ for electrode I, II and III respectively. The constructed electrodes gave average selective precise and usable within the pH range 3 - 7. Interferences from common cations, alkaloids, sugars, amino acids and drug excipients were reported. The results obtained by the proposed electrodes were also applied successfully to the determination of the drug in pharmaceutical preparations and biological fluids.

Four Novel Synthetic Tryptamine Analogs Induce Head-Twitch Responses and Increase 5-HTR2a in the Prefrontal Cortex in Mice

  • Abiero, Arvie;Ryu, In Soo;Botanas, Chrislean Jun;Custodio, Raly James Perez;Sayson, Leandro Val;Kim, Mikyung;Lee, Hyun Jun;Kim, Hee Jin;Seo, Joung-Wook;Cho, Min Chang;Lee, Kun Won;Yoo, Sung Yeun;Jang, Choon-Gon;Lee, Yong Sup;Cheong, Jae Hoon
    • Biomolecules & Therapeutics
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    • v.28 no.1
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    • pp.83-91
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    • 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.

Compounds Obtained from Sida acuta with the Potential to Induce Quinone Reductase and to Inhibit 7,12-Dimethylbenz-[a]anthracene-Induced Preneoplastic Lesions in a Mouse Mammary Organ Culture Model

  • Jang, Dae-Sik;Park, Eun-Jung;Kang, Young-Hwa;Su, Bao-Ning;Hawthorne, Michael-E.;Vigo, Jose-Schunke;Graham, James-G.;Cabieses, Fernando;Fong, Harry H.S.;Mehta, Rajendra-G.;Pezzuto, John-M.;Kinghorn, A.-Douglas
    • Archives of Pharmacal Research
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    • v.26 no.8
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    • pp.585-590
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    • 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.

Biogenic Synthesis of Metallic Nanoparticles and Their Antibacterial Applications (금속 나노입자의 생체 합성과 항균적 적용)

  • Patil, Maheshkumar Prakash;Kim, Jong-Oh;Seo, Yong Bae;Kang, Min-jae;Kim, Gun-Do
    • Journal of Life Science
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    • v.31 no.9
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    • pp.862-872
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    • 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.

Intravenous patient-controlled analgesia hydromorphone combined with pregabalin for the treatment of postherpetic neuralgia: a multicenter, randomized controlled study

  • Huang, Ying;Xu, Chenjie;Zeng, Tao;Li, Zhongming;Xia, Yanzhi;Tao, Gaojian;Zhu, Tong;Lu, Lijuan;Li, Jing;Huang, Taiyuan;Huai, Hongbo;Ning, Benxiang;Ma, Chao;Wang, Xinxing;Chang, Yuhua;Mao, Peng;Lin, Jian
    • The Korean Journal of Pain
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    • v.34 no.2
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    • pp.210-216
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    • 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.

Inhibitory effects of Broussonetia kazinoki twig extract on allergic inflammatory reactions in TNF-𝛼/IFN-𝛾-stimulated HaCaT and IgE-sensitized RBL-2H3 cells (TNF-𝛼/IFN-𝛾로 자극된 HaCaT 및 IgE로 감작된 RBL-2H3 세포에서 닥나무 가지 추출물의 알러지 염증반응 억제 효과)

  • Won-Bin Bae;Eun-Hye Kim;Min-Ju Kim;Seun-Ah Yang
    • Food Science and Preservation
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    • v.31 no.2
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    • pp.307-314
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    • 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.