hiv-1 protease

Ursonic Acid (TOS-BB-0966) belongs to the family of Ursane Triterpenes whose structure is based on the pentacyclic ursane skeleton. It has potential as HIV-1 Protease Inhibitor.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

α-Lipoic Acid (DL-α-Lipoic acid) an octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.

Betulinic acid (ALS-357) is a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase.

Cytochalasin A, a cell-permeable fungal toxin and oxidized derivative of cytochalasin B, is an inhibitor of HIV-1 protease (IC50 = 3 μM). It inhibits actin polymerization, interferes with microtubule assembly by reacting with sulfhydryl groups, and serves as an antibiotic and bactericidal active agent.

Nigranoic acid is a natural product,and inhibits HIV-1 reverse transcriptase.

Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a CNS-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein [Kis: 8.07 nM and 0.45 nM].

1-Deoxymannojirimycin hydrochloride, a selective α1,2-mannosidase inhibitor (IC50: 20 μM), also inhibits HIV-1 strains but exhibits poor antiviral activity.

1. Isosinensetin (6-Demethoxynobiletin) shows antioxidant and HIV-1 protease inhibiting activities.

Liquidambaric lactone, a compound isolated from Euonymus grandiflorus Wall, may exhibit inhibitory activity against HIV-1 reverse transcriptase.

Zingibroside R1 (Ginsenoside Z-R1) has anti-HIV-1 activity.

Escin IA (Escin IA;Aescin IA) is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression[1][2].

Isoescin IA, a triterpenoid saponin isolated from the seeds of Aesculus chinensis, exhibits anti-HIV-1 protease activity.

1,4-Dicaffeoylquinic acid has antioxidant activity.1,4-Dicaffeoylquinic acid is a potent and highly selective class of HIV-1 integrase inhibitors, inhibitsHIV-1 replication in MT-2 cell culture at non-toxic concentrations.

Punicalin exerts anti-inflammatory, antioxidative, and anti-hepatotoxic activities, it shows inhibitory activity on HIV-1 reverse transcriptase in a dose-dependent manner, with an IC50 of 0.11 microg ml (0.14 microM).

Bevirimat (PA-457) is a first-in-class inhibitor of HIV-1 maturation, blocking the cleavage of the Gag capsid (CA) precursor, CA-SPI, to mature CA protein during virion maturation.

Rosamultin has antioxidant, antiinflammatory antinociceptive properties,and has anti-human immunodeficiency virus (HIV) activity.

Absinthin (Absynthin) is a weak HIV-1 protease inhibitor.

L-Chicoric Acid (trans-Caffeoyltartaric acid) has been shown to inhibit hyaluronidase and HIV-1 integrase, and to possess phagoeytosis stimulatory activity in vitro and in vivo and antiviral acitivy. L-Chicoric acid may reduce acute alcohol-induced steatosis in mice through interfering with the induction of iNOS and iNOS-dependent signaling cascades in the liver. 3. L-Chicoric acid inhibited cell viability and induced apoptosis in 3T3-L1 preadipocytes which was characterized by chromatin condensation and poly ADP-ribose-polymerase (PARP) cleavage.

Ganoderic acid GS-1, an extensively oxygenated lanostane-type triterpenoid, exhibits anti-HIV-1 protease activities, displaying an IC50 value of 58 μM [1].

Acetyl-binankadsurin A (compound 5), a lignan obtained from Kadsura longipedunculata, exhibits weak inhibitory effects on HIV-1 protease, demonstrating an IC50 value exceeding 100 μg mL [1].

Protosappanin A (PTA) has anti-oxidative nitrative activities on brain immune and neuroinflammation through regulation of CD14 TLR4-dependent IKK IκB NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

Ganoderiol F has anti-inflammatory, cytotoxic and anti-HIV activity, it inhibits activity of topoisomerases in vitro, and it inhibits human immunodeficiency virus-1 protease with IC(50) values of 20-40 microM. It induced HO-1 expression, activation of the mitogen-activated protein kinase EKR and up-regulation of cyclin-dependent kinase inhibitor p16 and suppressed lipopolysaccharide (LPS)-induced nitric oxide (NO) production.

Ganoderic acid B is a chemical marker in quality control of G. lucidum and related products. Ganoderic acid B-containing herbs has potential influence towards therapeutic window of trifluoperazine.Ganoderic acid B has antinociceptive effect