34 results about "C21 steroid" patented technology

The invention discloses a furan skeleton included 2H-pyrazole hydroxamic acid C21 steroid saponin aglycone derivative and a preparation method and an application thereof. The structure of the derivative is shown as the formula VIII (img file = 'DDA 000709386530000011. TIF' wi= '882' he= '498' / ), R1 is selected from H and CH3; R2 is selected from H and F. The derivative has an apparent inhibiting effect on human breast cancer cells (MCF-7), cervical cancer cells (HeLa), lung carcinoma cells (A549) and hepatoma carcinoma cells (HepG2), and cytotoxicity equivalent to or higher than positive control drugs Celecoxib is presented to human kidney epithelial cells (293T), and the derivative can be applied to preparation of antitumor drugs.

The invention discloses a pyrazoline hydroxamic acid C21 steroid saponin aglycone derivative containing a naphthalene skeleton, a preparation method of the derivative and an application of the derivative in preparing an anti-tumor drug. The C21 steroid saponin aglycone derivative has a structural formula as shown as Formula IX as shown in the specification, wherein R1 is selected from H or CH3; R2 is selected from H or CH3; R3 is selected from H or CH3; and R4 is selected from H or CH3. The derivative has the advantages of better bioactivity, higher selectivity, lower toxicity and the like. The derivative has an obvious inhibiting effect on human breast cancer cells, cervical cancer cells, lung cancer cells and liver cancer cells.

The invention provides a Radix Radix C21 steroid extract, a preparation method and application thereof. The dried cane of dill radix is ​​extracted with 0-100% ethanol solution, and the C21 steroid of dill radix is ​​separated by the method of macroporous adsorption resin and decolorization resin, wherein the weight percentage of C21 steroid is 50-95%. The obtained radish C21 steroid extract has been proved by pharmacological activity studies to have the effect of reversing tumor multidrug resistance, and can be used to prepare tumor cell multidrug resistance reversing agent.

The invention discloses a furan skeleton-containing dihydropyrazolsulfanilamide C21 steroid sapogenin derivative, and a preparation method and an application thereof. The structure of the furan skeleton-containing dihydropyrazolsulfanilamide C21 steroid sapogenin derivative is represented by formula VII shown in the specification; and in the formula VII, R1 is selected from H and CH3, and R2 is selected from H and F. The derivative has an obvious inhibition effect on human breast cancer cells (MCF-7), cervical carcinoma cells (HeLa), lung cancer cells (A549) and liver cancer cells (HepG2), has same or better cytotoxicity on human renal epithelial cells (293T) than positive control drug Celecoxib, and can be used to prepare antitumor drugs.

The invention belongs to the field of medicines or health care products, and in particular relates to the use of C. citronella C21 steroids in the preparation of IDO inhibitors. The present invention finds through the research that salivaside C, salivaside D, salivaside O, salivaside P, salivaside Q, salivaside R, salivaside S, salivaside M and salivaside N The inhibitory activity to intracellular IDO is better than that of the positive control drug 1-methyltryptophan (1-MT) to the inhibitory activity of intracellular IDO, has significant IDO inhibitory activity, and can be used for the treatment of cancer, albino Alzheimer's disease, autoimmune disease, ankylosing spondylitis, bacterial infection, cataracts, mood disorder, depression, or anxiety.

Belonging to the field of natural pharmaceutical chemistry, the invention discloses a C21 steroid Asclepiasterol, a preparation method and application thereof in preparation of a tumor multidrug resistance reversal agent. The structural formula of C21 steroid Asclepiasterol is shown as the specification. The Asclepiasterol involved in the invention has low cytotoxicity, but can significantly increase the accumulation degree of antitumor drugs in drug resistant cells, can enhance the effect of antitumor drugs in inducing drug resistant cell apoptosis, and can be applied in combination with antitumor drugs to significantly inhibit the formation rate of drug resistant tumor cell colonies and obviously decline the expression level of P-gp in two drug resistant cell lines without lowering drug resistant gene expression, thus suggesting that Asclepiasterol probably affects P-gp expression at the level of transcription and translation and has a unique mechanism of action. Therefore, compared with the existing tumor multidrug resistance reversal agents, the C21 steroid Asclepiasterol provided by the invention has high reversal activity and low toxicity, and is in accordance with the high efficiency and low toxicity characteristics of antitumor drugs.

The invention discloses the use of C21 steroid glycoside in pharmacy, wherein the systematic test shows that C21 steroid glycocide has low toxic and side effect, but has unique effect for treating psychogenia diseases with depression state, in particular for depression.

The invention provides a Xu Changqing C21 steroid transformation product and its application in the preparation of a multidrug resistance reversal agent for tumor cells. The weight percentage of C21 steroid aglycone in the transformation product is greater than or equal to 90%, which can reverse the multidrug resistance of human gastric cancer. Drug-resistant cells, multidrug-resistant cells of human colon cancer, and multidrug-resistant cells of human lung cancer are resistant to commonly used clinical drugs paclitaxel, doxorubicin, 5-fluorouracil, and cisplatin, and also provide preparation of Xu Changqing's C21 steroid transformation product The method and the preparation method are simple and convenient. The Xu Changqing C21 steroid transformation product of the present invention is used in combination with antineoplastic drugs in clinic to improve the curative effect of chemotherapy and has broad application prospects.

The invention belongs to the field of medicines or health products and particularly relates to Periploca forrestii C21 steroides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors. Researches herein discover that both periplocoside L and periplocoside H have better intracellular IDO inhibitory activity than a positive control 1-MT (1-methyl-tryptophan), have significant IDO inhibitoryactivity, and are suitable for treating cancers, Alzheimer's disease, autoimmune diseases, ankylosing spondylitis, bacterial infections, cataract, mood disorders, and depression or anxiety.

The invention relates to a C21 steroid saponin compound in marsdenia tenacissima stem, and applications thereof in preparation of medicines used for preventing and treating lung cancer. It is shown bybiological experiments that the C21 steroid saponin compound in marsdenia tenacissima stem is capable of inhibiting tumor cell migration, maintaining tumor cells at G0 / G1 phases, and releasing Cytochrome c through up-regulating of Bax and down-regulating of Bcl-2 expression, activating Caspase 3 and Caspase 9 to induce tumor cell apoptosis, and is capable of activating caspase 8 at the same time,and inducing cell apoptosis through death receptor pathway. The C21 steroid saponin compound is capable of inhibiting tumor cell migration and invading through down-regulating of MMP-2 and MMP-9 protein expression, the effect is obvious, and lung cancer preventing and treating effect is achieved.

The present invention relates to a pharmaceutical composition for the treatment, prevention and / or treatment of neurodegenerative diseases. On the one hand, its active ingredient C21 steroidal saponin can significantly reduce the production of β-amyloid in N2a-APP695 cells and increase excessive Aβ amyloid. Protein clearance rate; on the other hand, it promotes the proliferation of neuronal cells, and has a protective effect on neurotransmitters such as glutamate-induced neuronal cytotoxicity caused by the excessive accumulation of Aβ amyloid, thereby comprehensively playing a role in the treatment of neurodegenerative diseases. effect. Therefore, it has a good application prospect in the preparation of Aβ amyloid formation inhibitors and neuroprotective agents, and drugs for preventing or treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's disease and the like.

The invention belongs to the technical field of medicines, and relates to the preparation of C21 steroid compounds in Tengguanteng and its application in the field of preventing and treating osteoporosis. The present invention discloses a C21 steroid compound of formulas (I) and (II) and salts thereof, R1-R5 as described in the description and claims. The compound of the present invention has good effect of preventing and treating osteoporosis, and can be combined with a pharmaceutically acceptable carrier to prepare clinically acceptable medicine for treating osteoporosis.

The invention belongs to the field of medicines or health products and particularly relates to Periploca forrestii C21 steroides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors. Researches herein discover that both periplocoside G and periplocoside I have better intracellular IDO inhibitory activity than a positive control 1-MT (1-methyl-tryptophan), have significant IDO inhibitoryactivity, and are suitable for treating cancers, Alzheimer's disease, autoimmune diseases, ankylosing spondylitis, bacterial infections, cataract, mood disorders, and depression or anxiety.

The invention relates to a C21 steroidal saponin compound and its application in the preparation of anti-lung cancer drugs. Biological experiment results show that the compound can inhibit tumor cell migration and keep it in G0 / G1 phase. In addition, tumor cell apoptosis can be induced by up-regulating Bax and down-regulating the expression of Bcl-2, thereby releasing Cytochrome c, and finally activating Caspase 3 and Caspase 9. It can also activate caspase 8 and induce apoptosis through the death receptor pathway. The compound of the present invention can inhibit the migration and invasion of tumor cells by down-regulating the expression of MMP-2 and MMP-9 proteins, the effect is remarkable, and the anti-lung cancer effect is achieved.