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α-Glucosidase Inhibitors from the Roots of Codonopsis lanceolata Trautv.

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Codonopsis lanceolata Trautv. is a plant of the Campanulaceae family, which is distributed throughout Korea, Japan and China. C. lanceolata has been cultivated and its roots have been used as food especially in Korea. Other Codonopsis species, C. pilosula and C. tangshen were used as medicine (Tang-Sam) for ulcers, memory improvement and immunostimulating; however, C. lanceolata was treated as an adulterant in Japan and China.1,2) Several studies of the chemical constituents of C. pilosula, C. tangshen and C. ussuriensis have been reported in the literatures.3-6) There are some reports on secondary metabolites of C. lanceolata; on the isolation of triterpenoid, saponin and alkaloid from the roots7-10) and the isolation of flavonoids from the leaves.11) The present report deals with the isolation, structure determination and α-glucosidase inhibition activity of tangshenoside I and adeonsine from the roots of C. lanceolata.
... 8,9 The roots of C. lanceolata have been used in Korea as a crude tonic drug and an edible plant. 10 The aerial parts of C. nervosa are utilised in Tibetan folk medicine to treat arthritis, leprosy, neuralgia, beriberi and hysteria. 11 In addition, roots of some least explored species of Codonopsis including C. cordifolioidea, C. bulleyana, and C. subglobosa are well-known vegetables in south-western China and have been used as food since ancient times. ...
... Phytochemical Studies of the Extracts: From n-hexane anf EtOAc extracts, eleven compounds were isolated. The isolated compounds were identified as (24E,24R)-methylcholesta-5,7,22-trien-3β-ol (ergosterol) (1) [11], (22E,24R)-ethylcholesta-5,7,22-trien-3β-ol (7-dehydroporiferasterol) (2) [11], (22E,24R)-ethylcholesta-7,22-dien-3β,5α,6β-triol (3) [12], (22E,24R)-ethylcholesta-5,22-dien-3-O-β-D-glucopyranoside (poriferasterol glucoside) (4) [13], perlolyrine (5) [14], pyrrolezanthine-6-methyl ether (6) (11) and βadenosine (10) with IC50 of 56.4 μM and 9.3 mM were previously reported [21,22]. The nitrogen containing moiety in compound 5 and 6 may increase their binding affinity with target enzyme and result in lower IC50 values with higher therapeutic efficiency [23]. ...
... The roots of C. lanceolate have been cultivated and used as a food. Other Codonopsis species such as C. pilosula and C. tangshen have been used as medicines (Tang-Sam) for ulcers treatment, memory improvement, and immune stimulation [78,79].Various reports have indicated that the isolated secondary metabolites of C. lanceolata roots e.g., triterpenoid, saponin, and alkaloids, show tangshenoside I and β-adenosine with an IC 50 of 1.4 and 9.3 mM for α-glucosidase inhibition, respectively [80]. It has been demonstrated previously that Lobelia sessilifolia can potently inhibit rice α-glucosidase, and crude extracts and coffee beans can be very specific and potent α-galactosidase inhibitors [81]. ...
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Type-II diabetes mellitus (T2DM) results from a combination of genetic and lifestyle factors, and the prevalence of T2DM is increasing worldwide. Clinically, both α-glucosidase and α-amylase enzymes inhibitors can suppress peaks of postprandial glucose with surplus adverse effects, leading to efforts devoted to urgently seeking new anti-diabetes drugs from natural sources for delayed starch digestion. This review attempts to explore 10 families e.g., Bignoniaceae, Ericaceae, Dryopteridaceae, Campanulaceae, Geraniaceae, Euphorbiaceae, Rubiaceae, Acanthaceae, Rutaceae, and Moraceae as medicinal plants, and folk and herb medicines for lowering blood glucose level, or alternative anti-diabetic natural products. Many natural products have been studied in silico, in vitro, and in vivo assays to restrain hyperglycemia. In addition, natural products, and particularly polyphenols, possess diverse structures for exploring them as inhibitors of α-glucosidase and α-amylase. Interestingly, an in silico discovery approach using natural compounds via virtual screening could directly target α-glucosidase and α-amylase enzymes through Monte Carto molecular modeling. Autodock, MOE-Dock, Biovia Discovery Studio, PyMOL, and Accelrys have been used to discover new candidates as inhibitors or activators. While docking score, binding energy (Kcal/mol), the number of hydrogen bonds, or interactions with critical amino acid residues have been taken into concerning the reliability of software for validation of enzymatic analysis, in vitro cell assay and in vivo animal tests are required to obtain leads, hits, and candidates in drug discovery and development.
... Kai He và cộng sự chứng minh được rằng Codonopsis pilosula có khả năng hạ đường huyết ở chuột bị tiểu đường do streptozotocin bằng việc ức chế tốt enzym α-glucosidase [21]. Suk Whan Jung và cộng sự cũng nghiên cứu trên rễ của Codonopsis lanceolata có chứa 2 hợp chất tangshenoside và β-adenosine có tác dụng ức chế α-glucosidase in vitro yếu với IC50 lần là 1,4 và 9,3 mM [22]. Một số hợp chất được phân lập từ rễ Hồng đảng sâm có tiềm năng điều trị ĐTĐ và các bệnh mắc kèm do stress oxy hóa gây ra. ...
Article
This study aims to evaluate the antioxidant ability and α-glucosidase inhibitory activities of Codonopsisjavanica extract to elucidate its mechanism in the treatment of diabetes type 2. The roots of Codonopsisjavanica were extracted with ethanol solvents and fractionated with n-hexane, ethyl acetate and butanol solvents. The total extract and the fractions were evaluated for free radical scavenging by 2.2-diphenyl-1-picrylhydrazyl method and α-glucosidase inhibitory activity in vitro. The study results show that ethyl acetate fraction from Codonopsisjavanica roots had the strongest antioxidant activity with a value of IC50 of 80.6 ± 2.8 µg/mL and a strong α-glucosidase enzyme inhibitory activity with a value of IC50 of 80.4 ± 5 µg/mL. These data suggest that ethyl acetate fraction from Codonopsisjavanica roots may have potential for the prevention and treatment of diabetes type 2. Keywords Codonopsisjavanica, diabetes type 2, α-glucosidase, antioxidant ability, fraction. 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... 항종 양 효과는 만삼 다당류와 더덕 부탄올 분획물, 사포닌 및 구성 화학성분인 codonoposide, codonoside 1c 등을 대상으로 다양 한 암세포에 대한 증식 억제 및 세포독성 작용전이 등이 보고된 바 있다(Lee et al., 2002; Lee et al., 2005; Kim et al., 2009c; Wang et al. 2011a;Yu et al., 2011;Xin et al., 2012;Xu et al., 2012;Yang et al., 2013). 항당뇨 효과는 만삼 다당류, 더덕 추 출물 및 구성 화학성분인 thangshenoside I, adenoshin을 대상 으로 수행한 결과, 당뇨유발인자를 유의적으로 억제하는 효과 가 밝혀진 바 있다(Shim et al., 2004;Jung et al., 2006;Fu et al., 2008). 간 보호 효과는 더덕 추출물 및 사포닌이 알코올 성 지방간 및 스트레스로 인한 간 손상을 보호하는 것으로 확인 졌으며, 일반더덕 추출물보다 증숙하거나 발효 처리한 더덕에 서 효과가 높은 것으로 나타났다. ...
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The present study was carried out to identify traditional konwledges on Korean Campanulaceae plants and conduct a comprehensive review of them through analyzing phytochemistry and pharmacology of Korean Campanulaceae plants. According to the literature study, the ethnobotanical plants of Korean Campanulacae consisted of a total 18 taxa. Of them, 12 taxa including Platycodon grandiflorus, Adenophora triphylla var. japonica, Codonopsis lanceolata and others have been used as ethnomedicinal plants. These plants have been used for the treatment of 49 diseases such as cold, asthma and postnatal care. Phytochemical studies have identified the constituents present from Korean Campanulaceae (Adenophora, Codonopsis, Platycodon, Campanula and Asyneuma). A wide range of chemical compounds comprised 109 triterpenes, 8 sterols, 4 polyacetylenes, 21 alkaloids, 14 flavonoids, 14 phenolic acids, 11 phenolic glycosides, 8 phenylpropanoids and 22 other compounds. Pharmacological studies of these compounds have demonstrated immuno-stimulating, anti-inflammatory, anti-asthmatic, apophlegmatic and anti-allergic effects. They have also shown antioxidant, estrogenic, anti-diabetic, hepatoprotective, neuroprotective, antinociception and anti-tumor activities, as well as anti-obesity and cardiovascular effects. In light of traditional knowledge and phytochemical and pharmacological studies summarized, uses of Korean Campanulaceae based on traditional knowledge (for the treatment diseases and conditions of respiratory, pregnancy, childbirth, puerperium, genitourinary, circulatory, musculoskeletal and other systems) have been supported by phytochemical and pharmacological studies.
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