• Title/Summary/Keyword: Natural product new drugs

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The Study on the History of Pugation therapy From -'Treatise on Febrile Diseases' to 'Longevity and Life Presservation In Oriental Medicine'- (하법(下法)의 발전 과정에 대한 연구(硏究) -상한론(傷寒論)에서 사상의학(四象醫學) 까지-)

  • Choi, Yei-Kwen;Kim, Kyung-Yo
    • The Journal of Internal Korean Medicine
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    • v.19 no.1
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    • pp.524-552
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    • 1998
  • Purgation therapy has played an important role as a influential remedy from the begining of the Chinese medicine. Especially purgation therapy is raised as the effective remedy on the acute infectious disease in the book of 'Treatise on Febrile Disease'. But It was inclined to cold-nature and available only in the excess syndrome. Nevertheless it is evident that the book has showed an example of this therapy. During the middle age, purgation therapy is classified into several subtype; hydrogogue therapy, laxation with lubricants, purgation with cold-natured drugs and purgation with warm-natured drugs. Comparing with the ancient times, it must be a progression. It was investigated earnestly by a school leaded by Zhang Congzheng. They were not restricted to several diseases, but applied it to the wide range of diseases. They thought as following. 'One is ill from pathogenic factor so that you should eliminate it from the human body'. Hence, they frequently used three major remedies such as diaphoresis, emesis and purgation. In this process, purgation therapy had showed eye-opening progress. But opposition to it was not little. Li Gao was a representative man on the opposite side. He expressed a critical opinion and placed great importance on the genuine energy, the natural healing force. Under his influence, a large number of doctors evaded purgation and put it under taboo. On account of these trend, purgation therapy had took a backward step and retrograded. Therefore cathartics such as Rhei Radix et Rhizoma, Rharbitidis Semen, cold drugs such as Gypsum Fibrosum, etc. had been excluded for preservation of the genuine energy, and came about an obnoxious custom to value only 'tonity deficiency', or 'warm and tonify'. As it had came into fashion to approach most disease from the point of view, purgation therapy was merely fall into a remedy of constipation. After the eighteenth century purgation therapy encountered the new period of rivival. It was introduced by them who strived for the study of Epidemics to the new current of thought, so called '增水行舟'. It was because 온병 was apt to dissipate one's Yin fluid. Therefore purgation therapy of this period was characterized by establishing nourishment Yin and body fluid with or without use of timely purgation of accumulation of heat. From the time of Zhang Congzheng, it was accomplished by Lee Je-ma to the most epoch-making change. He caused an improvement in the use of purgation therapy by regarding innate constitutional contradiction as importance than representing clinical symptoms. He warned that existing remedies that depend only upon symptoms and signs, not upon individual characteristics including constitutional features didn't bring round to but kill them. And he understood all the pathologic processes in his constitutional theory, investigated specific drugs on four constitution, made indications of each prescriptions clear. For giving to differentiation of constition before differentiation of syndrom, his new slant on the pathologic phenomena overcome the limitations of 변증시치, and revaluate purgation therapy from remedy impaire the genuine energy to that restore it by recover the balance between the internal organ. It is the product of him to fundamentally upset the cause to be in disregard of purgation therapy.

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2-(Trimethylammonium) Ethyl (R)-3-Methoxy-3-oxo-2-Stearamidopropyl Phosphate Suppresses Osteoclast Maturation and Bone Resorption by Targeting Macrophage-Colony Stimulating Factor Signaling

  • Park, So Jeong;Park, Doo Ri;Bhattarai, Deepak;Lee, Kyeong;Kim, Jaesang;Bae, Yun Soo;Lee, Soo Young
    • Molecules and Cells
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    • v.37 no.8
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    • pp.628-635
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    • 2014
  • 2-(Trimethylammonium) ethyl (R)-3-methoxy-3-oxo-2-stearamidopropyl phosphate [(R)-TEMOSPho], a derivative of an organic chemical identified from a natural product library, promotes highly efficient megakaryopoiesis. Here, we show that (R)-TEMOSPho blocks osteoclast maturation from progenitor cells of hematopoietic origin, as well as blocking the resorptive function of mature osteoclasts. The inhibitory effect of (R)-TEMOSPho on osteoclasts was due to a disruption of the actin cytoskeleton, resulting from impaired downstream signaling of c-Fms, a receptor for macrophage-colony stimulating factor linked to c-Cbl, phosphoinositol-3-kinase (PI3K), Vav3, and Rac1. In addition, (R)-TEMOSPho blocked inflammation-induced bone destruction by reducing the numbers of osteoclasts produced in mice. Thus, (R)-TEMOSPho may represent a promising new class of antiresorptive drugs for the treatment of bone loss associated with increased osteoclast maturation and activity.

The Acetylation-based synthesis of 3,3',4',5,5',7-hexaacetate myricetin and evaluation of its anti-inflammatory activities in lipopolysaccharide-induced RAW264.7 mouse macrophage cells

  • Kristina Lama;Hyehyun Hong;Tae-Jin Park;Jin-Soo Park;Won-Jae Chi;Seung-Young Kim
    • Journal of Applied Biological Chemistry
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    • v.66
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    • pp.29-38
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    • 2023
  • Recent studies have highlighted the link between diseases and inflammation across our lifespan. Our sedentary lifestyle, high-calorie diet, chronic stress, chronic infections, and exposure to pollutants and xenobiotics, collectively intensify the course and recurrence of infections and inflammation in our bodies, promoting the prevalence of chronic diseases and aging. Given such phenomena and considering additional factors such as the frequency of prescription, and easy access to over-the-counter drugs, the need for anti-inflammatory therapeutics is ever-increasing. However, the readily available anti-inflammatory treatment option comes with a greater risk of side effects or high cost (biologics). Therefore in this growing competition of discovering and developing new potent anti-inflammatory drugs, we focused on utilizing the established knowledge of traditional medicine to find lead compounds. Since lead optimization is an indispensable step toward drug development, we applied this concept for the production of potent anti-inflammatory compounds achieved by structural modification of flavonoids. The derivative obtained through acetylation of myricetin, 3,3',4',5,5',7-hexaacetate myricetin, showed a greater inhibitory effect in the production of pro-inflammatory mediators such as nitric oxide, Prostaglandin E2, and pro-inflammatory cytokines like interleukin-6, interleukin1β, in lipopolysaccharide-stimulated RAW264.7 mouse macrophage cells compared to myricetin. The increased potency of inhibition was in conjunction with an increased inhibitory effect on inducible nitric oxide synthase and cyclooxygenase-2 proteins. Through such measures, this study supports lead optimization for well-established lead compounds from traditional medicine using a simpler and greener chemistry approach for the purpose of designing and developing potent anti-inflammatory therapeutics with possibly fewer side effects and increased bioavailability.

Semantic Change of Crude Drug Preparations in Korea and Policy Evaluation (생약제제의 의미 변천과 정책적 문제 검토)

  • Kim, Yun-Kyung;Cho, Sunyoung;Kim, Jiyeon;Kang, Yeonseok
    • Herbal Formula Science
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    • v.21 no.2
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    • pp.29-43
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    • 2013
  • Objectives : The aim of this study is reviewing the past legal definition and regulations, to provide basis for the future desirable direction of Korean herbal pharmaceutical industry and national herbal drug policies. Methods : We reviewed how concept of herbal medicinal preparation has been utilized and changed along with various national laws and regulations. And this study also reviewed problems related herbal medicinal preparation policies. Results : Since 1990s, especially inauguration of Korea Food & Drug Administration (KFDA) at 1998, the concept of crude drug preparation has constantly expanded and distorted the scope of herbal medicinal preparations. This resulted in decline of herbal medicinal preparation industry. Conclusions : It means policies related herbal medicinal preparation which was driven steadily during this decade have lost their consistency. Also, it restricted the various medical options which can guarantee people's health rights.

Anti-arthritic Effect of a New Diet-Supplement Containing Red Ginseng Extract and Glucosamine Complex (홍삼추출물과 글루코사민 복합제제의 관절염에 미치는 영향)

  • Jeong, Choon-Sik;Hyun, Jin-Ee;Kang, Min-Hee;Sim, Joon-Soo;Son, Mi-Jin;Jung, Sang-Hoon;Kim, Jong-Hoon;Lee, Kwang-Seong;Kim, Yeong-Shik
    • Korean Journal of Pharmacognosy
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    • v.34 no.4 s.135
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    • pp.327-334
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    • 2003
  • We evaluated the anti-arthritic effect of a new diet-supplement product containing red ginseng, glucosamine, shark cartilage, ascorbic acid and manganese chloride for the relieving arthritic symptoms. Anti-inflammatory activities of the aqueous extract of red ginseng (250 and 500 mg/kg), glucosamine (240 mg/kg) and shark cartilage (240 mg/kg) were tested individually on vascular permeability and carrageenan-induced paw edema. Glucosamine and shark cartilage showed the inhibition of vascular permeability by 29.6 and 32.9%, respectively. Red ginseng (500 mg/kg) and shark cartilage showed the inhibition of carrageenan-induced paw edema at 0.5, 1, 2 and 3 hr. The supplement (red ginseng mixture: RGM) composed of red ginseng (43.5%), glucosamine (25.0%), shark cartilage (25.0%), ascorbic acid (5.0%) and manganese chloride (1.5%) was prepared and its inhibitory activities including vascular permeability and carrageenan-induced paw edema were comparable to anti-inflammatory drugs such as diclofenac and ibuprofen. It was also tested on adjuvant-induced arthritis in rats as one of chronic arthritic tests and Randall-Selitto assay as an analgesic test. RGM showed the inhibition against the swelling of rat paws induced by Mycobacterium tuberculosis at a dose of 1,500 mg/kg. Determination of cytokines of the sera sampled from arthritis-induced animals indicated that RGM increased the levels of $interferon-{\gamma}$ and interleukin-6, representing the immunostimulatory effect by red ginseng. RGM treatment moderately reduced the production of NO in RAW 264.7 cells in a dose-dependent manner. Taken together, these results support that RGM can be applicable for the improvement of arthritic as a new diet-supplement.

In Vitro Schistosomicidal Activity of Phytol and Tegumental Alterations Induced in Juvenile and Adult Stages of Schistosoma haematobium

  • Eraky, Maysa Ahmad;Aly, Nagwa Shaban Mohamed;Selem, Rabab Fawzy;El-Kholy, Asmaa Abd El-Monem;Rashed, Gehan Abd El-Rahman
    • Parasites, Hosts and Diseases
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    • v.54 no.4
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    • pp.477-484
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    • 2016
  • There is renewed interest in natural products as a starting point for discovery of drugs for schistosomiasis. Recent studies have shown that phytol reveals interesting in vivo and in vitro antischistosomal properties against Schistosoma mansoni adult worms. Here, we report the in vitro antischistosomal activity of phytol against Schistosoma haematobium juvenile and adult worms and alterations on the tegumental surface of the worms by means of scanning electron microscopy. The assay, which was carried out with 6 concentrations (25, 50, 75, 100, 125, and $150{\mu}g/ml$) of phytol, has shown a promising activity in a dose and time-dependent manner. There was a significant decline in the motility of the worms and a mortality rate of 100% was found at 48 hr after they had been exposed to phytol in the concentration of $150{\mu}g/ml$. Male worms were more susceptible. On the ultrastructural level, phytol also induced tegumental peeling, disintegration of tubercles and spines in addition to morphological disfiguring of the oral and ventral suckers. This report provides the first evidence that phytol is able to kill S. haematobium of different ages, and emphasizes that it is a promising natural product that could be used for development of a new schistosomicidal agent.

Physicochemical Characteristics of Antidementia Acetylcholinesterase Inhibitor-containing Methanol Extract from Sorghum bicolor and Industrial Application (항치매성 Acetylcholinesterase저해물질을 함유하고 있는 수수 메탄올 추출물의 특성 및 산업적 응용)

  • Song, Jung-Eun;Lee, Jong-Soo
    • The Journal of Natural Sciences
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    • v.19 no.1
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    • pp.45-55
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    • 2008
  • Alzheimer's disease is charaterized by the acetylcholine depletion, amyloid b-protein aggregation and neurofibrillary tangles. The prevention of the breakdown of acetylcholine by acetylcholinesterase (AChE) inhibitor has the best clinically therapeutic efficacy for Alzheimer's disease patients. To develop new antidementia alternative drugs or nutraceuticals, methanol extracts of Sorghum bicolor was screened from various extracts of cereals and legumes as a potent AChE inhibitor-containing extract in previous paper. In this paper, physicochemical properties of the methanol extracts was investigated. The methanol extracts was soluble by water, methanol and DMSO and had 215 nm and 282nm of maximum absorption spectra. It was also stable at 20-$100^{\circ}C$ and pH 2.0-10.0 for 1 hr. Test product was prepared by using methanol extracts from Sorghum bicolor and changes of its quality during storge at $20^{\circ}C$ and $40^{\circ}C$ were investigated. It was very stable for 8 weeks at $40^{\circ}C$.

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Preparation of an Inactivated Influenza Vaccine Using the Ethanol Extracts of Medical Herbs (한약재 식물 에탄올추출물을 이용한 인플루엔자 불활화백신 제작)

  • Cho, Sehee;Lee, Seung-Hoon;Kim, Seonjeong;Cheong, Yucheol;Kim, Yewon;Kim, Ju Won;Kim, Su Jeong;Seo, Seungin;Seo, Dong-Won;Lim, Jae-Hwan;Jeon, Sejin;Jang, Yo Han
    • Journal of Life Science
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    • v.32 no.12
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    • pp.919-928
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    • 2022
  • As seen in the COVID-19 pandemic, unexpected emergence of new viruses presents serious concern on public health. Especially, the absence of effective vaccines or antiviral drugs against emerging viruses significantly increases the severity of disease and duration of viral circulation among population. Natural products have served as a major source for safe and effective antiviral drugs. In this study, we examined the virucidal activity of medical herb extracts with a view to discover novel antiviral agents with desired levels of safety and antiviral efficacy. Ethanol extracts of ten selected medical herbs were tested for antioxidant activity and in-vitro cytotoxicity in various animal cell lines. Of note, the herbal extracts showed broad and potent virucidal activities against rotavirus, hepatitis A virus, and influenza A virus. The extracts of Sorbus commixta and Glycyrrhiza uralensis showed strong virucidal activities against influenza A virus. We also examined whether the extracts of Sorbus commixta and Glycyrrhiza uralensis can be used as inactivating agents to prepare an inactivated viral vaccine. In a mouse model, influenza A virus inactivated by the extracts elicited high levels of neutralizing antibodies, and the vaccination provided complete protection against lethal challenge. These results suggest that herb-derived natural products can be developed to antiviral drugs as well as inactivating agents for preparation of inactivated viral vaccines.

An International Collaborative Program To Discover New Drugs from Tropical Biodiversity of Vietnam and Laos

  • Soejarto, Djaja D.;Pezzuto, John M.;Fong, Harry H.S.;Tan, Ghee Teng;Zhang, Hong Jie;Tamez, Pamela;Aydogmus, Zeynep;Chien, Nguyen Quyet;Franzblau, Scott G.;Gyllenhaal, Charlotte;Regalado, Jacinto C.;Hung, Nguyen Van;Hoang, Vu Dinh;Hiep, Nguyen Tien;Xuan, Le Thi;Hai, Nong Van;Cuong, Nguyen Manh;Bich, Truong Quang;Loc, Phan Ke;Vu, Bui Minh;Southavong, Boun Hoong
    • Natural Product Sciences
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    • v.8 no.1
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    • pp.1-15
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    • 2002
  • An International Cooperative Biodiversity Group (ICBG) program based at the University of Illinois at Chicago initiated its activities in 1998, with the following specific objectives: (a) inventory and conservation of of plants of Cuc Phuong National Park in Vietnam and of medicinal plants of Laos; (b) drug discovery (and development) based on plants of Vietnam and Laos; and (c) economic development of communities participating in the ICBG project both in Vietnam and Laos. Member-institutions and an industrial partner of this ICBG are bound by a Memorandum of Agreement that recognizes property and intellectual property rights, prior informed consent for access to genetic resources and to indigenous knowledge, the sharing of benefits that may arise from the drug discovery effort, and the provision of short-term and long-term benefits to host country institutions and communities. The drug discovery effort is targeted to the search for agents for therapies against malaria (antimalarial assay of plant extracts, using Plasmodium falciparum clones), AIDS (anti-HIV-l activity using HOG.R5 reporter cell line (through transactivation of the green fluorescent protein/GFP gene), cancer (screening of plant extracts in 6 human tumor cell lines - KB, Col-2, LU-l, LNCaP, HUVEC, hTert-RPEl), tuberculosis (screening of extracts in the microplate Alamar Blue assay against Mycobacterium tuberculosis $H_{37}Ra\;and\;H_{37}Rv),$ all performed at UIC, and CNS-related diseases (with special focus on Alzheimer's disease, pain and rheumatoid arthritis, and asthma), peformed at Glaxo Smith Kline (UK). Source plants were selected based on two approaches: biodiversity-based (plants of Cuc Phuong National Park) and ethnobotany-based (medicinal plants of Cuc Phuong National Park in Vietnam and medicinal plants of Laos). At mc, as of July, 2001, active leads had been identified in the anti-HIV, anticancer, antimalarial, and anti- TB assay, after the screening of more than 800 extracts. At least 25 biologically active compounds have been isolated, 13 of which are new with anti-HIV activity, and 3 also new with antimalarial activity. At GSK of 21 plant samples with a history of use to treat CNS-related diseases tested to date, a number showed activity against one or more of the CNS assay targets used, but no new compounds have been isolated. The results of the drug discovery effort to date indicate that tropical plant diversity of Vietnam and Laos unquestionably harbors biologically active chemical entities, which, through further research, may eventually yield candidates for drug development. Although the substantial monetary benefit of the drug discovery process (royalties) is a long way off, the UIC ICBG program provides direct and real-term benefits to host country institutions and communities.