29 results about "Antimalarial medication" patented technology

Methods of treating malaria comprising administration of compounds of Formula (I′) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. It also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

Provided are methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. Also provided are uses of the compounds of Formula (I), as defined herein, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

The present invention provides methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for the possible inhibition of plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

The invention relates to application of a mir-331-3p inhibitor in preparation of a medicine for inhibiting malaria mosquito transmission, and belongs to the technical field of biological medicine. Aiming at the technical problems that the existing anti-malarial drug mainly acts on the later stage of plasmodium development and is lack of an effective propagation blocker, the invention provides the miR-331-3p inhibitor which is used for blocking the formation of plasmodium oocysts by inhibiting the interaction between microRNA and a mosquito target gene spetzle. Experiments show that the inhibitor can reduce the mosquito infection rate by about 50%, and has the characteristics of high targeting property, simplicity in operation and the like. The invention provides a novel drug development target for blocking malaria transmission, can effectively supplement the prevention and control blind area of the existing anti-malarial drug, and has important application value in the field of mosquito-borne infectious disease control.

To provide a new antimalarial agent that achieves a balance between strong antimalarial activity and low cytotoxicity.SOLUTION: An antimalarial agent comprising an ethanol extract and / or a methanol extract of at least one plant selected from the group consisting of Ficus hispida, Streblus asper, Boerhavia repens, Clerodendrum viscosum, Amaranthus spinosus, and Mussaenda corymbosa.SELECTED DRAWING: None

This invention provides the application of Pulsatilla saponin B4 in the preparation of antimalarial drugs, which can significantly improve weight loss, peripheral blood parasitemia, and survival rate in mice infected with lethal Plasmodium. Its mechanism of action is not to directly kill Plasmodium, but to regulate the host immune system, including activating T / B cell immune responses, upregulating pro-inflammatory factors and interferon signaling pathways, and downregulating Arg1 expression. At the same time, Pulsatilla saponin B4 can alleviate immunopathological damage to organs such as the spleen and liver, restore the homeostasis of the spleen's immune microenvironment, and protect the normal structure of tissues. As a natural product, this compound has the characteristics of multiple targets and low toxicity, and has the dual advantages of anti-infection and immune homeostasis regulation, showing good prospects for clinical application and translation.

Disclosed herein are methods and compositions for treating and / or preventing Plasmodium falciparum malaria by administering a compound that mimics the binding of anti-Plasmodium falciparum Glutamic Acid Rich Protein (PfGARP).

The present application relates to a preparation of a 7,7'-epoxy lignan compound and its application in preparing anti-malaria products, and belongs to the field of traditional Chinese medicine and natural medicine pharmacy. The anti-malaria medicine with the compound as an active ingredient. The present application expands the medicinal value of 7,7'-epoxy lignan compounds in Rhodiola henryi.

The present invention discloses a functionalized isoquinolone and quinolone compounds and an efficient transition-metal-free approach for the synthesis of the same. The invention provides a highly functionalized isoquinolones from the reaction of dimethyl-2-((phenylamino)methylene) malonate with aryne precursors under mild. The reaction proceeds through insertion of aryne into the C−C σ-bond, which offers a novel and practical entry to access a wide range of isoquinolones with enhanced yields. The substrate scope is broad as the process can stands a variety of functional groups and the application of the developed process has been demonstrated in the total synthesis of antimalarial agent SJ000101247. Also, the highly functionalized quinolones are also useful in the synthesis of floxacins based compounds and derivatives e.g. ciprofloxacin, norfloxacin, G003967, etc.

The present invention belongs to the field of biomedical technology, and specifically relates to the application of Lactobacillus murinus driving GABA in the treatment of cerebral malaria in mice. The present invention found significantly enriched Lactobacillus murinus and confirmed that Lactobacillus murinus can produce GABA. Subsequently, in a mouse cerebral malaria model, the effects of Lactobacillus murinus and GABA on improving and treating mouse cerebral malaria were evaluated when Lactobacillus murinus and GABA were used alone or in conjunction with dihydroartemisinin. The results showed that whether used alone or in combination with dihydroartemisinin, the bacteria and its metabolite GABA can effectively improve mouse behavior, immune pathological damage to various organs, reduce parasitemia, and prolong mouse survival. Compared with the use of drugs alone, it can effectively treat mouse cerebral malaria. From the perspective of using probiotics to drive their metabolites to assist antimalarial drugs in the treatment of mouse cerebral malaria, the present invention provides a new solution for the treatment of severe malaria caused by falciparum malaria, especially human cerebral malaria.

The invention discloses an artemisinin compound containing a piperazine side chain or a pharmaceutical salt thereof, and the structural general formula is shown in the specification. The artemisinin compound containing the piperazine side chain and the pharmaceutical salt thereof provided by the invention have a brand-new skeleton structure and better anti-malaria and anti-tumor activity, can be used as an anti-tumor drug and an anti-malarial drug, and can be used as an anti-malarial drug. And more choices can be provided for clinical treatment.

The invention belongs to the field of compound synthesis, and discloses an epsilon-caprolactam compound containing a guanidyl structural unit and preparation and application of the epsilon-caprolactam compound, the chemical structure of the epsilon-caprolactam compound is shown in the specification, and the epsilon-caprolactam compound containing the guanidyl structural unit has good anti-malarial activity and is expected to become a novel drug intermediate. The compound is used for preparing antimalarial drugs. The invention also discloses a preparation method of the epsilon-caprolactam compound containing the guanidyl structural unit. The preparation method of the epsilon-caprolactam compound containing the guanidyl structural unit has the advantages that the raw materials and the catalyst are cheap and easy to obtain; reaction conditions are mild, and operation is simple and convenient; and the method has the advantages of wide substrate universality, high yield for a series of epsilon-caprolactam products containing guanidyl structural units, and the like.

The invention discloses application of a naturally-sourced small molecule compound and a pharmaceutical composition thereof in preparation of antimalarial drugs, and belongs to the technical field of biological medicines. The small molecule compound is PHPP, the CAS number of the small molecule compound is 252205-23-5, and the structure of the small molecule compound is shown in the specification. According to the invention, the small molecule compound PHPP, which is a specific monomer component, is screened from natural products for the first time and is proved to have remarkable anti-malarial activity, and the cognitive blank of the anti-malarial application of the small molecule compound is filled up; the compound not only has an excellent in-vitro anti-malarial effect, but also has no obvious cytotoxicity under an effective concentration and is high in safety; more importantly, when the compound is combined with artemisinin, a remarkable synergistic effect can be generated, a brand new solution is provided for solving the problem of severe artemisinin drug resistance, and candidate lead compounds and combination schemes with wide prospects are provided for developing new-generation antimalarial drugs.

The invention provides a compound containing an artemisinin similar structure and a preparation method and application of the compound, the structural formula of the compound is shown in the formula I. The compound has excellent histone deacetylase inhibitory activity and anti-tumor and anti-malarial activity and can be used for preparing anti-tumor and anti-malarial drugs.

The invention discloses an artemisinin compound containing a 10-bit ether side chain or a pharmaceutical salt thereof, the structural general formula is one of the following structures: the artemisinin compound containing the 10-bit ether side chain provided by the invention has a relatively obvious proliferation inhibition effect on liver cancer HepG2, lung cancer A549, intestinal cancer HCT116, hematologic tumors MV-4-11 and HL-60; the anti-tumor activity of part of the compounds is higher than that of commercially available drugs SAHA and belinostat, and the compounds are expected to be developed into novel anti-tumor drugs. In addition, the performance of a plurality of compounds is superior to the in-vitro antimalarial activity of artemisinin, and the compounds are expected to be developed into novel antimalarial drugs.

The present invention relates to dosing regimen of a new antimalarial drug, as monotherapy or combination therapy.

The invention discloses a method for inducing polarization of macrophages by AKK and / or outer membrane vesicles thereof and application of AKK and / or outer membrane vesicles thereof in preparation of drugs for promoting phagocytosis and infection of erythrocytes by macrophages, and belongs to the technical field of biological medicines. According to the invention, after macrophages are induced by AKK bacteria or OMVs thereof, an M1 polarization phenomenon occurs. Macrophages polarized by M1 generate proinflammatory factors, and meanwhile, erythrocytes infected by plasmodium are subjected to more phagocytosis. Compared with macrophages not polarized by M1, the macrophages polarized by M1 induced by AKK bacteria or AKK-OMVs can swallow more erythrocytes infected by plasmodium under the condition of not using the existing anti-malarial drugs, so that the resistance of plasmodium to the anti-malarial drugs due to long-term use of the anti-malarial drugs is effectively avoided; and a new scheme is provided for clinical malaria treatment.

This invention belongs to the field of drug synthesis and relates to a highly efficient hydrogen-borrowing reaction strategy for the preparation of ferroquinone (FQ). This strategy uses commercially available ferrocene as a starting material, constructs the key precursor ferrocene diol through two-step conversion, and then proceeds through two hydrogen-borrowing reactions, successfully inventing a highly efficient method for the preparation of FQ in four steps with an overall yield of 69%. Compared with previously reported routes, this method shortens the reaction steps, increases the reaction yield (the overall yield of the existing ferroquinone synthesis route in the background art is 39%), is simpler to operate, and is environmentally friendly (the only byproduct in the hydrogen-borrowing reaction is water). It can be widely used, laying a solid foundation for in-depth pharmacological and physiological activity research of FQ, and providing a novel and universal strategy for developing new scaffolds for candidate drug molecules with high activity and high selectivity of FQ derivatives.

The invention discloses a plasmodium falciparum proliferation inhibitor based on raw milk or pasteurized milk source exosomes (RM-EVs / CM-EVs), and the IC50 value of the plasmodium falciparum proliferation inhibitor is as low as 22.91 + / -2.7 mu g / mL and is obviously superior to that of ultrahigh-temperature sterilized milk and milk powder source EVs. The invention provides an extraction method of the EVs and application of the EVs in antimalarial drugs and functional foods, and provides a new natural and efficient choice for malaria prevention and treatment.

The invention shows that a P. falciparum-specific interaction between a PfEMP1 adhesin and the endothelial receptor CD36 modulates sporozoite infectivity. Using a synthetic peptide to leverage this interaction, a robust high-throughput screening method has been developed to identify next-generation prophylactics against this deadly malaria parasite. The synthetic peptide is also used as a prophylactic medicament to prevent P. falciparum infection in a subject.

This invention relates to a 6- O -L-arabinopyranosyl- β The preparation of β-D-glucopyranoside and its application in the preparation of antimalarial products belong to the field of traditional Chinese medicine and natural drug pharmaceuticals. Compound 6- of this invention... O -L-arabinopyranosyl- β This invention relates to an antimalarial drug with β-D-glucopyranoside as the active ingredient. It expands the application of aromatic disaccharide compounds 6- from *Hydrangea macrophylla*. O -L-arabinopyranosyl- β The medicinal value of D-glucopyranoside.

The invention discloses a long-chain non-coding RNA (lncRNA) lnc30 target spot of plasmodium falciparum in an erythrogenous stage and application of the long-chain non-coding RNA (lncRNA) lnc30 target spot, and relates to the technical field of biological medicines. The lnc30 nucleotide sequence is as shown in SEQ ID NO: 1, has the full length of 705nt, is positioned in a plasmodium falciparum cell nucleus, and is specifically and highly expressed in a schizosome stage. Researches find that lnc30 overexpression can significantly enhance the growth advantage of plasmodium falciparum and the ability of merozoite to invade erythrocytes, and participates in regulation of the erythroid stage development process of plasmodium, but after lnc30 is knocked down, plasmodium death may be caused. The key effect of the lnc30 in plasmodium falciparum development is disclosed for the first time, a new molecular tool is provided for antimalarial drug target screening, malaria diagnosis and pathogenesis research, and remarkable scientific value and application prospects are achieved.

This invention provides a sesquiterpene compound, its preparation, and its application. The sesquiterpene compound has a basic 5 / 7 / 3 / 6 / 5 skeleton. Although its structure differs significantly from that of traditional antimalarial drugs (such as artemisinin and quinoline derivatives), it still effectively inhibits the activity of Plasmodium parasites. It can serve as an outstanding new antimalarial drug, bringing good news to malaria patients and providing a new application for sesquiterpene compounds.

The application discloses an AKK and / or outer membrane vesicle thereof induced macrophage polarization method and application thereof in preparation of a medicine for promoting phagocytosis of infected red blood cells by macrophages, and belongs to the technical field of biological medicines. It is found by the application that macrophages are subjected to M1 polarization phenomenon after being induced by AKK bacteria or OMVs thereof. The macrophages subjected to M1 polarization produce proinflammatory factors, and phagocytose more red blood cells infected by Plasmodium. In the absence of existing anti-malaria medicines, compared with macrophages not subjected to M1 polarization, the macrophages subjected to M1 polarization only by AKK bacteria or AKK-OMVs can phagocytose more red blood cells infected by Plasmodium, effectively avoiding the resistance of Plasmodium to anti-malaria medicines caused by long-term use of the anti-malaria medicines, and providing a new scheme for clinical malaria treatment.

The invention relates to a preparation method and application of an ATG5 and DC-SIGN bimolecular condition knockout mouse model, and belongs to the field of gene engineering. A mouse model is knocked out under the bimolecular conditions of ATG5 and DC-SIGN by hybridizing an Atg5f / f CD11c Cre < + > mouse with a Cd209aflox / flox C57BL / 6JGp mouse, and a DC cell of the Atg5f / f Cd209af / f CD11c Cre < + >, and a DC cell of the Atg5f / f Cd209af / f CD11c Cre < + > is knocked out under the bimolecular conditions of the ATG5 and the DC-SIGN. An intraperitoneal injection plasmodium johnsonii infection model is established, plasmodium proliferation is observed, CD4 + T cell response is detected, and the DC function is verified in combination with an in-vitro co-culture experiment. The model enhances DC phagocytosis and antigen presentation capabilities, promotes plasmodium specific CD4 + T cell activation, significantly inhibits plasmodium infection, provides a new target for targeted DC-SIGN-based malaria immunotherapy, and can be used as an antimalarial drug screening tool.

The invention discloses an artemisinin compound or a pharmaceutical salt thereof, the structure of which is shown as follows: the artemisinin compound provided by the invention has a brand new chemical structure, and in-vitro activity screening on solid tumor and hematologic tumor cells shows that most compounds show broad-spectrum and excellent in-vitro anti-tumor activity, so that the artemisinin compound or the pharmaceutical salt thereof can be applied to preparation of antitumor drugs. Wherein the antitumor activity of a plurality of compounds is superior to that of a marketed drug SAHA, and the compounds are expected to be developed into novel antitumor drugs. In addition, a plurality of compounds show in-vitro anti-malarial activity equivalent to that of artemisinin, and are expected to be developed into novel anti-malarial drugs.

The invention discloses an application of an anti-malarial drug primaquine phosphate in preparation of drugs for treating BCR-ABL positive leukemia and breast cancer and a drug combination composition, and discovers that the anti-malarial drug primaquine phosphate has obvious effects of resisting BCR-ABL + leukemia and breast cancer, and has obvious anti-BCR-ABL + leukemia and breast cancer in the cellular level. The PRQ can significantly inhibit the growth of a BCR-ABL + leukemia cell line and an imatinib drug-resistant BCR-ABL + leukemia cell line, significantly inhibit the growth of breast cancer cells and induce ferroptosis of the breast cancer cells, and further researches find that the PRQ can degrade wild or mutant BCR-ABL proteins in a targeted manner. At the patient level, the PRQ is found to be capable of inhibiting the formation ability of primary cell colonies of wild-type or mutant patients with the BCR-ABL + leukemia, and at the animal level, the PRQ is found to have an obvious inhibiting effect on the progress of the BCR-ABL + leukemia.

The invention discloses application of an FABP5 inhibitor in preparation of a medicine for inhibiting growth of plasmodium and an antimalarial medicine combining the FABP5 inhibitor with artemisinin, and relates to the technical field of biological medicine. The novel application of the FABP5 inhibitor in preparation of the medicine for inhibiting the growth of the plasmodium provides a basis for application of the FABP5 inhibitor in preparation of the antimalarial medicine. Meanwhile, the FABP5 inhibitor can be used in combination with artemisinin and derivatives thereof, the antimalarial effect is remarkably enhanced, no obvious toxic or side effect exists, and it is further proved that the FABP5 inhibitor can be used for preparing antimalarial drugs.