• Title/Summary/Keyword: alkaloid screening

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Screening of novel alkaloid inhibitors for vascular endothelial growth factor in cancer cells: an integrated computational approach

  • Shahik, Shah Md.;Salauddin, Asma;Hossain, Md. Shakhawat;Noyon, Sajjad Hossain;Moin, Abu Tayab;Mizan, Shagufta;Raza, Md. Thosif
    • Genomics & Informatics
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    • v.19 no.1
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    • pp.6.1-6.10
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    • 2021
  • Vascular endothelial growth factor (VEGF) is expressed at elevated levels by most cancer cells, which can stimulate vascular endothelial cell growth, survival, proliferation as well as trigger angiogenesis modulated by VEGF and VEGFR (a tyrosine kinase receptor) signaling. The angiogenic effects of the VEGF family are thought to be primarily mediated through the interaction of VEGF with VEGFR-2. Targeting this signaling molecule and its receptor is a novel approach for blocking angiogenesis. In recent years virtual high throughput screening has emerged as a widely accepted powerful technique in the identification of novel and diverse leads. The high resolution X-ray structure of VEGF has paved the way to introduce new small molecular inhibitors by structure-based virtual screening. In this study using different alkaloid molecules as potential novel inhibitors of VEGF, we proposed three alkaloid candidates for inhibiting VEGF and VEGFR mediated angiogenesis. As these three alkaloid compounds exhibited high scoring functions, which also highlights their high binding ability, it is evident that these alkaloids can be taken to further drug development pipelines for use as novel lead compounds to design new and effective drugs against cancer.

Screening of the Alkaloids in Korean Plants (국내 자생 식물의 알칼로이드 검색)

  • Park, Man-Ki;Park, Jeong-Hill;Kim, Yong-Chul;Han, Byung-Hoon;Han, Yong-Nam;Ryu, Jae-Ha;Yoo, Seung-Jo;Kim, Kyoung-Ho
    • Korean Journal of Pharmacognosy
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    • v.20 no.2
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    • pp.83-87
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    • 1989
  • The alkaloids of thirty five Korean plants which belong to Rhamnaceae, Sterculiaceae, Celastracea, Urticaceae and Rubiaceae were screened. Plant was extracted and solvent fractionated to yield ether soluble alkaloidal fraction and butanol soluble fraction. Each fraction was subjected to alkaloidal test by Dragendorff's reaction. The result showed eighteen plants strong positive, fourteen weak and six negative to alkaloidal test.

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The Chemical Screening of Caryophyllaceae Plants (석죽과식물(石竹科植物)의 성분검색(成分檢索))

  • Chung, Dong-Kyu;Kim, Tae-Hee;Lee, Yong-Ran
    • Korean Journal of Pharmacognosy
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    • v.9 no.2
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    • pp.83-88
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    • 1978
  • From phytochemical screening of the seven species of Caryophyllaceae, that is, one species of Melandrium, and Dianthus and Pseudostellaria, two species of Stellaria and Cerastium the following compounds were identified. 1) aldehyde, sugars, other reducing compounds and glycosides from the above mentioned seven species of Caryophyllaceae were identified by thin layer chromatography method and comparison of Rf values with the standard substances. 2) Saponins, steroids and terpenoids showed positive reaction with the Froth testing in all of seven plants. Five species of plant showed positive reaction with Liebermann-Buchard test. 3) Flavonoid and polyphenolic compounds were identified by the spots in TLC-test and chlorogenic acid showed the same Rf values with the standard substances. 4) The spots of alkaloid were shown at Rf=0.68 (Stellaria aquatica) and at Rf=0.71 (Pseudostellaria palibiniana) and at Rf=0.70, and 0.44 (Dianthus sinensis).

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Antitumor constituents in the Achillea species (Achillea 류 생약의 항암 성분 연구)

  • 이강노
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.209-209
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    • 1994
  • 천연자원으로부터 얻어진 항암 또는 세포독성물질로는 주로 alkaloid, lignan, terpenoid, macrolide 등에 속하는 물질들이고 그 중 sesquiterpene lactone계열 화합물에서 세포독성 및 항종양 활성이 있는 물질이 다수 얻어졌으며 그 대부분은 국화과의 식물에서 분리 보고되고 있다. Achillea 속 식물은 국화과에 속하는 다년생초본으로 남한에는 톱풀과 산톱풀 2종만이 자생한다. screening 결과 이 두 식물에는 segquiterpene lactone 화합물과 Peroxide등 다수의 활성성분이 함유되어 있을 것으로 기대되어 본 연구에 착수하였다. 두 식물의 각 분획에 대하여 SNU-1(위암세포주)과 SNU-354(간암세포주)를 이용해 검색한 결과 두 식물 모두 MC ext.와 MeOH ext.에서 현저한 세포독성을 보였으며 현재 MC ext. 로부터 세포독성물질의 분리를 수행하고 있다. EtOAc ext.는 세포독성은 거의 나타내지 않았으나 flavonoid 성분이 다수 존재함을 확인하였으며 면역활성 및 enzyme inhibition등의 활성을 검토하고자 화합물을 분리하였다. 그 결과 톱풀로 부터는 luteolin-7-0-glucoside와 apigenin-7-0-glucoside를 그리고 산톱풀로부터는 luteolin-7-0-glucoside, apigenin-7-0-glucoside, luteolin, apigenin을 분리 확인 동정하였다.

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Immunotoxin using plant toxins for cancer theraphy (식물성 Toxin 류를 이용한 Immunotoxin 연구)

  • 이강춘
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.210-210
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    • 1994
  • 천연자원으로부터 얻어진 항암 또는 세포독성물질로는 주로 alkaloid, lignan, terpenoid, macrolide 등에 속하는 물질들이고 그 중 sesquiterpene lactone계열 화합물에서 세포독성 및 항종양 활성이 있는 물질이 다수 얻어졌으며 그 대부분은 국화과의 식물에서 분리 보고되고 있다. Achillea 속 식물은 국화과에 속하는 다년생초본으로 남한에는 톱풀과 산톱풀 2종만이 자생한다. screening 결과 이 두 식물에는 segquiterpene lactone 화합물과 Peroxide등 다수의 활성성분이 함유되어 있을 것으로 기대되어 본 연구에 착수하였다. 두 식물의 각 분획에 대하여 SNU-1(위암세포주)과 SNU-354(간암세포주)를 이용해 검색한 결과 두 식물 모두 MC ext.와 MeOH ext.에서 현저한 세포독성을 보였으며 현재 MC ext. 로부터 세포독성물질의 분리를 수행하고 있다. EtOAc ext.는 세포독성은 거의 나타내지 않았으나 flavonoid 성분이 다수 존재함을 확인하였으며 면역활성 및 enzyme inhibition등의 활성을 검토하고자 화합물을 분리하였다. 그 결과 톱풀로 부터는 luteolin-7-0-glucoside와 apigenin-7-0-glucoside를 그리고 산톱풀로부터는 luteolin-7-0-glucoside, apigenin-7-0-glucoside, luteolin, apigenin을 분리 확인 동정하였다.

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Differential Rapid Screening of Phytochemicals by Leaf Spray Mass Spectrometry

  • Muller, Thomas;Cooks, R. Graham
    • Bulletin of the Korean Chemical Society
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    • v.35 no.3
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    • pp.919-924
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    • 2014
  • Ambient ionization can be achieved by generating an electrospray directly from plant tissue ("leaf spray"). The resulting mass spectra are characteristic of ionizable phytochemicals in the plant material. By subtracting the leaf spray spectra recorded from the petals of two hibiscus species H. moscheutos and H. syriacus one gains rapid access to the metabolites that differ most in the two petals. One such compound was identified as the sambubioside of quercitin (or delphinidin) while others are known flavones. Major interest centered on a $C_{19}H_{29}NO_5$ compound that occurs only in the large H. moscheutos bloom. Attempts were made to characterize this compound by mass spectrometry alone as a test of such an approach. This showed that the compound is an alkaloid, assigned to the polyhydroxylated pyrrolidine class, and bound via a $C_3$ hydrocarbon unit to a monoterpene.

Design, Syntheses and Biological Evaluations of Nonpeptidic Caspase 3 Inhibitors

  • Kim, Eun-Sook;Yoo, Sung-Eun;Yi, Kyu-Yang;Lee, Sun-Kyung;Noh, Jae-Sung;Jung, Yong-Sam;Kim, Eun-Hee;Jeong, Nak-Chul
    • Bulletin of the Korean Chemical Society
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    • v.23 no.7
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    • pp.1003-1010
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    • 2002
  • Caspase 3, a member of cysteine protease family, is well known as a major apoptosis effector and is involved in cell death as a result of ischemic diseases such as stroke and myocardial infarction, therefore the inhibition of caspase 3 may protect those apoptotic cell damages. During the high-throughput screening of the compounds from the Korea Chemical Bank, berberine derivatives (A and B), an isoquinoline alkaloid, have been identified as potential inhibitors for caspase 3. Based on this finding we carried out molecular modeling study to identify the pharmacophoric elements of berberine structure which interact with a substrate-recognition binding site of caspase 3 and came up with several novel scaffolds. In this report, we will discuss the molecular modeling, syntheses and the enzyme inhibitory activities of these novel compounds.

Physico-phytochemical Evaluation of Raw Material and CO2 extract of Fruits of Terminalia chebula

  • Chandil, Shachi;Bamoriya, Harikishan
    • CELLMED
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    • v.12 no.1
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    • pp.4.1-4.13
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    • 2022
  • The present communication attempts to evaluate the physicochemical and preliminary phytochemical studies on the fruit of Terminalia chebula Retz. Combretaceae family. Haritaki is one of the most celebrated herbs in the Indian traditional medicine system, Ayurveda. Terminalia chebula is known to exhibit different properties like anticancer, anti-inflammatory, anti-protozoal, antimicrobial, antioxidant, hepato and renal protective activities, and in the management of metabolic syndrome. As there is no detailed standardisation work reported on fruit, the physicochemical parameters, preliminary phytochemical constants, heavy metals, analysis are carried out. The phytochemical screening indicated the presence Tannin, Alkaloid, Phenol, Carbohydrate, Steroids, Protein and Resin compounds in CO2 extract of Haritaki. The present investigation will helpful in assessing the quality and purity of a crude drug. Thus, the study provides facts that CO2 extract of Haritaki contains medicinally important bioactive phytochemical compounds which justifies the use of plant species as conventional medicine for treatment of many diseases.