Tripyolide-nucleic acid aptamer derivatives, a preparation method and use thereof are shown. The structure of the triptolide-nucleic acid aptamer derivatives is as shown by formula I, wherein the definitions of R.sub.1-R.sub.7, G, A, B, M, Z and X are described. The present invention uses a nucleic acid aptamer and triptolide or modified compounds thereof as the starting materials, and introduces a linking group A at the C-14 hydroxyl group, epoxy groups and five-membered ring lactones in triptolide, then connects it to a nucleic acid aptamer B, and obtains the triptolide-nucleic acid aptamer derivatives. The triptolide-nucleic acid aptamer derivatives of the present invention have the characteristics of good targeting, a high anti-cancer activity, low toxicity and side effects, good water solubility and high bioavailability, and the preparation method of the present invention is scientific and reasonable and has a controllable quality and good repeatability, and is thereby suitable for production.

The present invention relates to a combination product comprising a limonoid compound (or a pharmaceutically acceptable derivative, ester, stereoisomer, salt or prodrug thereof), and a biguanide compound (e.g., metformin, metformin hydrochloride, buformin, and phenformin). The present invention further relates to a use of the combination product for prevention and/or treatment of a disease associated with diabetes, for lipid-lowering and weight-loss, and the like.

The present application discloses derivatives of hydroxysteroids, pharmaceutically acceptable salts, stereoisomers or tautomers thereof. The compounds and compositions described herein can be used in therapy.

Provided herein is a compound of Formula (I-I), or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I), and methods of using the compounds, e.g. in the treatment of CNS-related disorders. ##STR00001##

This disclosure provides triptolide-conjugates, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, as well methods of using such compounds in the treatment of conditions/diseases, such as those relating to cancer, immunomodulation and/or inflammation.

Estrane-based and androstane-based aminosteroid derivatives are described herein. More specifically, the following piperazinyl-steroid compounds of Formula I, Formula II, Formula III, and Formula IV are described. The compounds display cytotoxicity on a variety of cancer cell lines. A process for producing the compounds and their use in the manufacture of pharmaceutical formulations and/or combinations is also disclosed. ##STR00001##

The present disclosure provides for a synthetic strategy to incorporate a C12α-hydroxy group from the methylene (—CH2-) in a steroid backbone, combining synthetic chemistry and enzymology techniques to develop a selective inhibitor for cytochrome P450 8B1, and developing a selective P450 8B1 inhibitor, which can be used as a tool to study P450 8B1 and treat health issues.

A steroidal piperidone derivative, a synthesis method, and a use thereof are provided. The steroidal piperidone derivative has a chemical structure shown in general formula (1) or general formula (2), where R is any one selected from the group consisting of alkyl, phenyl, substituted phenyl, and a heterocycle. In the synthesis method of the steroidal piperidone derivative, dehydroepiandrosterone (DHEA) is used as a basic raw material to prepare the steroidal piperidone derivative of the present disclosure through a series of reactions. A product prepared by the synthesis method has a high yield and is easily separated, and thus the synthesis method is the optimal method for preparing the steroidal piperidone derivative of the present disclosure. The present steroidal piperidone derivative exhibits prominent toxic activity against sucking pests, such as aphids, spider mites, rice planthoppers, and B. tabaci, and can be used for the control of a plant pest. ##STR00001##

A triptolide derivative, a preparation method therefor, and a method for use thereof are described. The triptolide derivative has the structure as shown in general formula I, and the definition of each substituent is as described in the description and claims. The triptolide derivative has improved immunosuppressive activity and anti-tumor activity, low toxicity and high safety, thus having good development and application prospects. ##STR00001##

Disclosed are novel compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.