- Leonurine derivative and application thereof in preparing medicine for preventing or treating ischemic cerebrovascular diseases
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The invention provides a leonurine derivative and application of the leonurine derivative in preparation of a medicine for preventing or treating ischemic cerebrovascular diseases. The leonurine derivative has a structure as shown in a general formula (I), wherein X is selected from O or NH; Y is selected from any one of natural amino acid, substituted amino acid or amino alcohol; Z is selected from H, proline and any substituted proline. Pharmacological experiments prove that the leonurine derivative provided by the invention has the effects of neuroprotection, cerebral infarction area reduction and animal neurobehavioral scoring, and is good in safety, so that the leonurine derivative has important significance for developing novel medicines for preventing or treating ischemic cerebrovascular diseases.
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- Design, synthesis, and biological evaluation of novel stachydrine derivatives as potent neuroprotective agents for cerebral ischemic stroke
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Stachydrine is a natural product with multiple protective biological activities, including those involved in preventing cancer, ischemia, and cardiovascular disease. However, its use has been limited by low bioavailability and unsatisfactory efficacy. To address this problem, a series of stachydrine derivatives (A1/A2/A3/A4/B1/B2/B3/B4) were designed and synthesized, and biological studies were carried out in vitro and in vivo. When compared with stachydrine, Compound B1 exhibited better neuroprotective effects in vitro, and significantly reduced infarction size in the model of the middle cerebral artery occlusion rat model. Therefore, Compound B1 was selected for further research on ischemic stroke. [Figure not available: see fulltext.].
- Zhang, Liang,Li, Feng,Hou, Chenhui,Zhu, Sifeng,Zhong, Lili,Zhao, Jianchun,Song, Cai,Li, Wenbao
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p. 2529 - 2542
(2020/05/25)
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- METHOD FOR PRODUCING RECOMBINANT PEPTIDE AND RESULTANT PEPTIDE
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PROBLEM TO BE SOLVED: To provide peptides with reproductive- and sexual-function stimulating activity. SOLUTION: The peptides are represented by general formula: A-Thr-Lys-Pro-B-C-D-X (where A is 0, Met, Met(O), Thr, Ala, His, Phe, Lys, or Gly; B is 0, Gly, Asp, Trp, Gln, Asn, Tyr, Pro, or Arg; C is 0, Arg, Phe, Tyr, Gly, His, Pro, or Lys; D is 0, Val, Gly, Tyr, Trp, Phe, or His; and X is OH, OCH3, or NH2; where 0 represents absence of the amino acid residue; provided that if A≠0 then B ≠0 and/or C≠0 and/or D≠0, if B≠0 then C≠0 and/or D≠0, and peptides Phe-Thr-Lys-Pro-Gly, Thr-Lys-Pro-Pro-Arg and Thr-Lys-Pro-Arg-Gly are excluded). SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2020,JPO&INPIT
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Paragraph 0046; 0050; 0051
(2020/01/07)
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- PYRROLIDINE CARBOXAMIDO DERIVATIVES AND METHODS FOR PREPARING AND USING THE SAME
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Pyrrolidine carboxamido derivatives, optical isomers thereof, and salts thereof that are able to prevent, improve, and/or treat inflammatory conditions, including inflammatory bowel disease, and methods for preparing and using the same are provided.
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Page/Page column 55-56
(2017/01/26)
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- Synthesis of cytotoxic cyanobactin, Wewakazole B
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We report herein the synthesis of cytotoxic cyanobactin, Wewakazole B through an efficient solution-phase approach. The key steps of the synthesis are the macrocyclic lactamization of linear dodecapeptide and construction of two hexapeptides with three di
- Nayani, Kiranmai,Anwar Hussaini
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supporting information
p. 1166 - 1169
(2017/03/02)
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- Aggregation propensity of amyloidogenic and elastomeric dipeptides constituents
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This study demonstrates the self-assembly of N- and C-terminal protected dipeptides Phe–Gly and Pro–Gly which were derived from amyloidogenic and elastomeric peptide sequences. These constituents afforded nanostructured supramolecular ensembles through va
- Kumar, Vikas,Krishna, K. Vijaya,Khanna, Shruti,Joshi, Khashti Ballabh
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p. 5369 - 5376
(2016/08/05)
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- Stability of His-Phe-Arg-Trp-Pro-Gly-Pro to Leucine Aminopeptidase, Carboxypeptidase Y, and Rat Nasal Mucus, Blood, and Plasma
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The His-Phe-Arg-Trp-Pro-Gly-Pro [ACTH-(6-9)-PGP] peptide was synthesized. Proteolysis of ACTH-(6-9)-PGP and semax (Met-Glu-His-Phe-Pro-Gly-Pro) in the presence of leucine aminopeptidase and carboxypeptidase Y was studied. If the proteolysis of ACTH-(6-9)-PGP is mainly defined by aminopeptidases, the basic metabolite is Trp-Pro-Gly-Pro. Identification of major metabolites of ACTH-(6-9)PGP when incubated with the enzymes in vitro made it possible to evaluate proteolysis pathways of the peptide and prepare necessary amounts of its metabolites for using them as standards. Kinetics of ACTH-(6-9)PGP degradation in the presence of enzyme systems of nasal mucus, blood, and plasma were also explored. It was found that proteolysis of ACTH-(6-9)-PGP in rat blood and plasma occurs mainly under the effect of enzymes whose action is similar to leucine aminopeptidase.
- Shevchenko,Dulov,Andreeva,Nagaev,Shevchenko,Radilov,Myasoedov
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p. 153 - 161
(2016/04/19)
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- Method for producing a recombinant peptide and resultant peptide
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The invention relates to peptides with the following general formula: [in-line-formulae]A-Thr-Lys-Pro-B-C-D-X, where:[/in-line-formulae] A—0, Met, Met (O), Thr, Ala, His, Phe, Lys, Gly B—0, Gly, Asp, Trp, Gln, Asn, Tyr, Pro, Arg C—0, Arg, Phe, Tyr, Gly, His, Pro, Lys D—0, Val, Gly, Tyr, Trp, Phe, His X—OH, OCH3, NH2, where 0 is no amino acid residue, provided that if A≠0, then B and/or C and/or D≠0, if B≠0, then C and/or D≠0, excluding the peptides Phe-Thr-Lys-Pro-Gly (SEQ ID NO: 1), Thr-Lys-Pro-Pro-Arg (SEQ ID NO: 2), Thr-Lys-Pro-Arg-Gly (SEQ ID NO: 3).
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Page/Page column 157
(2016/09/12)
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- Synthesis, docking and anticancer activity studies of D-proline- incorporated wainunuamide
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D-proline-incorporated wainunuamide - a cyclic octapeptide was synthesized and characterized by FTIR, 1H and 13C NMR and Mass spectral analysis. Molecular docking studies were carried out for the designed cyclic octapeptide and the results showed greater affinity for HPV18-2IOI receptor (HeLa cancer cell line). The synthesized cyclic octapeptide exhibited potent anticancer activity against HeLa cancer cells. Indian Academy of Sciences.
- Himaja,Ranjitha,Mali, Sunil V.
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p. 1049 - 1055
(2013/03/13)
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- Structural-functional study of glycine-and-proline-containing peptides (Glyprolines) as potential neuroprotectors
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A synthetic scheme for preparation of (Gly-Pro) n, (Pro-Gly) n (n = 2, 3), and (Pro-Gly-Pro) n (n = 1, 2) peptides was elaborated. The effect of the synthesized peptides and the Gly-Pro and Pro-Gly dipeptides on survival of cultured cells of PC12 rat pheochromocytoma was studied under the conditions of oxidative stress induced by brief incubation of the cells with hydrogen peroxide. Peptides of the general formula (Gly-Pro) n and the Pro-Gly-Pro peptide at a concentration of 0.2-100 μM were shown to decrease the number of damaged cells. The Gly-Pro peptide was the most active and decreased the number of damaged cells by 49% on average at a concentration of 100 μM.
- Martynova,Andreeva,Klimova,Kirillova, Yu. G.,Shevchenko,Nagaev, I. Yu.,Shram,Shvets,Myasoedov
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experimental part
p. 150 - 156
(2010/04/29)
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- Synthesis of a phenylalanine-rich peptide as potential anthelmintic and cytotoxic agent
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A natural cyclic heptapeptide segetalin D [VIII] was synthesized by coupling of tripeptide unit Boc-Pro-Gly-Leu-OMe [V] with tetrapeptide unit Boc-Ser-Phe-Ala-Phe-OMe [VI] after proper deprotection at carboxyl and amino ends followed by cyclization of linear peptide segment. Structure of VIII was confirmed by spectral and elemental analyses. The newly synthesized cyclopeptide was tested for its antibacterial, antifungal, anthelmintic and cytotoxic activities. Compound VIII showed high cytotoxicity against Dalton's lymphoma ascites (DLA) and Ehrlichis ascites carcinoma (EAC) cell lines with CTC50 values of 7.54 and 13.56 μM. Moreover, VIII exhibited potent anthelmintic activity against earthworms Eudrilus species, Megascoplex konkanensis and Pontoscotex corethruses at a dose of 2 mg/mL.
- Dahiya, Rajiv
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p. 509 - 516
(2008/12/22)
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- Studies on Bitter Peptides from Casein Hydrolyzate. XIV. Bitter Taste of Synthetic Analogs of Octapeptide, Arg-Gly-Pro-Phe-Pro-Ile-Ile-Val, Corresponding to the C-Terminal Portion of β-Casein
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In order to elucidate the relationship between the chemical structure and bitter taste of the C-terminal portion of β-casein, some analogues, in which the phenylalanine residue was substituted by D-phenylalanine, lysine, glycine, glutamic acid or L-pyreny
- Nakatani, Masaru,Nakata, Takashi,Kouge, Katsushige,Okai, Hideo
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p. 438 - 444
(2007/10/02)
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- Compatibility of thioamides with reverse turn features: Synthesis and conformational analysis of two model cyclic pseudopeptides containing thioamides as backbone modifications
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The incorporation of thioamides within the backbone of linear peptides can produce subtle physical changes but have profound effects on biological activities and selectivity. To study the compatibility of thioamides with reverse turns (1←3 and 1]4 hydroge
- Sherman,Spatola
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p. 433 - 441
(2007/10/02)
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- SYNTHESIS OF C-TERMINAL FRAGMENTS OF BOMBESIN AND THEIR ANALOGUES
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With the aim of structural-functional studies in the bombesin series, a number of bombesin fragments and analogues have been synthesized.The synthesis was performed by the carbodiimide method and by the activated-ester method.Fragments with the sequences
- Kuranova, I. L.,Churkina, S. I.,Dyudmirova, V. L.,Filonova, E. B.,Ibatullin, F. M.,et al.
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p. 475 - 484
(2007/10/02)
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- 2'-Nitrobenzhydryl Polystyrene Resin: A New Photosensitive Polymeric Support for Peptide Synthesis
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2'-Nitrobenzhydryl polystyrene resin (NBH-resin) was prepared from the commercially available styrene-divinylbenzene cross-linked polymer by a two-step polymer analogous reaction.This resin was employed as a photolytically cleavable polymeric protective support for carboxyl function in amino acids under neutral conditions.The 2'-nitrobenzhydryl resin possesses good stability in 4 N HCl-dioxane required for the deprotection of the temporary Nα-tert-butyloxycarbonyl protecting group.The advantage of the new resin over the already reported benzhydryl resin is its increased acid stability during the Nα deblocking, which permits the peptide synthesis with the commonly available Boc-amino acids.The applicability of this resin is illustrated with the solid-phase synthesis of some model peptides.
- Ajayaghosh, A.,Pillai, V. N. Rajasekharan
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p. 5714 - 5717
(2007/10/02)
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- The L-Proline Residue as a 'Break-point' in Metal - Peptide Systems
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Results are reported of a potentiometric and spectrophotometric study of the H+ and Cu2+ complexes of the tetrapeptides X-Gly-Gly-Gly, Gly-X-Gly-Gly, Gly-Gly-X-Gly, and Gly-Gly-Gly-X where X is the proline (Pro) and sarcosine (Sar) residue (Gly=glycine).All the tetrapeptides (HL) form the series of complexes , -1L>, -2L>, and -3L> (charges omitted).The ligands Gly-X-Gly-Gly also form the bis-complex, .When inserted in a peptide chain the Pro and Sar residues cannot co-ordinate to Cu2+ through their peptide nitrogens since they do not possess ionizable protons.In addition the Pro residue tends to force the peptide chain to form a 'β-turn' and so adopt a 'bent' conformation.These studies demonstrate the formation of a large chelate ring when tetrapeptides containing Pro (and , to a smaller extent, Sar) in the second or third positions co-ordinate to Cu2+.This ring spans the terminal residues of the peptide chain and locks the peptide into a 'bent' or 'horse-shoe' shaped conformation.Cu2+ could therefore play an important role in activating oligopeptides (e.g. neuropeptides) containing proline.
- Pettit, Leslie D.,Steel, Ian,Formicka-Kozlowska, Grazyna,Tatarowski, Tomasz,Bataille, Michael
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p. 535 - 540
(2007/10/02)
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- PHOSPHONAMIDATE COMPOUNDS
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Phosphonamidates of the formula STR1 wherein X is a substituted or unsubstituted imino or amino acid or ester. These compounds possess angiotensin converting enzyme activity and are thus useful as hypotensive agents.
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