Last update 01 Nov 2024

phospholipase

Last update 01 Nov 2024

Basic Info

Synonyms-

Introduction-

Drugs associated with phospholipase

CT-2584

Target

phospholipase

Mechanism

phospholipase inhibitors

Active Org.-

Originator Org.

CTI BioPharma Corp.

Active Indication-

Inactive Indication

Castration-Resistant Prostatic Cancer [+5]

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

SC-101c

Target

phospholipase

Mechanism

phospholipase inhibitors

Active Org.-

Originator Org.

Scotia

Active Indication-

Inactive Indication

Cachexia

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Sch-53823

Target

phospholipase

Mechanism

phospholipase inhibitors

Active Org.-

Originator Org.

Schering-Plough Research Institute

Active Indication-

Inactive Indication

Infectious Diseases [+1]

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with phospholipase

NCT00004026 / TerminatedPhase 2

A Phase II Study of CT-2584 Mesylate in Patients With Hormone Refractory Prostate Cancer

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die. CT-2584 may stop the growth of prostate cancer by stopping blood flow to the tumor.
PURPOSE: Randomized phase II trial to study the effectiveness of CT-2584 in treating patients who have metastatic prostate cancer that has not responded to previous therapy.

Start Date01 Dec 1998

Sponsor / Collaborator

CTI BioPharma Corp.

100 Clinical Results associated with phospholipase

100 Translational Medicine associated with phospholipase

0 Patents (Medical) associated with phospholipase

1,220

Literatures (Medical) associated with phospholipase

01 Dec 2024·Journal of Ethnopharmacology

Anti-inflammatory and antiophidic effects of extract of Hymenaea eriogyne benth and structure-activity relationship prediction of the major markers in silico

Article

Author: Cavalcanti, Felipe França ; Torres-Rêgo, Manoela ; Lucas Tenório, Camylla Janiele ; de Sousa Ferreira, Sarah ; Assunção Ferreira, Magda Rhayanny ; Roberto da Costa Rodrigues, José ; de Freitas Fernandes-Pedrosa, Matheus ; Lira Soares, Luiz Alberto ; Daniele-Silva, Alessandra ; Pontes da Silva, Diana

ETHNOPHARMACOLOGICAL RELEVANCEHymenaea eriogyne Benth (Fabaceae) is popularly known as "Jatobá". Despite its use in folk medicine to treat inflammatory disorders, there are no descriptions that show its anti-inflammatory potential.AIM OF THE STUDYIn this sense, this study aimed to evaluate the anti-inflammatory and antivenom action of bark and leaves extract of H. eriogyne.MATERIALS AND METHODSThe in vivo anti-inflammatory activity was conducted by carrageenan-induced paw edema and zymosan-induced air pouch models, evaluating the edematogenic effect, leukocyte migration, protein concentration, levels of pro-inflammatory cytokines, malondialdehyde (MDA) and myeloperoxidase (MPO) activity. The antivenom potential was investigated in vitro on the enzymatic action (proteolytic, phospholipase and hyaluronidase) of Bothrops brazili and B. leucurus venom, as well as in vivo on the paw edema model induced by B. leucurus. Furthermore, the influence of its markers (astilbin and rutin) on MPO activity was investigated in silico. For molecular docking, AutodockVina, Biovia Discovery Studio, and Chimera 1.16 software were used.RESULTSThe extracts and bark and leaves of H. eriogyne revealed a high anti-inflammatory effect, with a reduction in all inflammatory parameters evaluated. The bark extract showed superior results when compared to the leaf extract, suggesting the influence of the astilbin concentration, higher in the bark, on the anti-inflammatory action. In addition, only the H. eriogyne bark extract was able to reduce MDA, indicating an associated antioxidant effect. Regarding the in vitro antivenom action, the extracts (bark and leaves) revealed the ability to inhibit the proteolytic, phospholipase and hyaluronidase action of both bothropic venom, with a greater effect against B. leucurus venom. In vivo, extracts from the bark and leaves of H. eriogyne (50-200 mg/kg) showed antiedematogenic activity, reducing the release of MPO and pro-inflammatory cytokines, indicating the presence of bioactive components useful in controlling the inflammatory process induced by the venom. In the in silico assays, astilbin and rutin showed reversible interactions of 9 possible positions and orientations towards MPO, with affinities of -9.5 and -10.4 kcal/mol and interactions with Phe407, Gln91, His95 and Arg239, important active pockets of MPO. Rutin demonstrated more effective types of interactions with MPO.CONCLUSIONThis approach reveals for the first time the anti-inflammatory action of H. eriogyne bark and leaf extracts in vivo, as well as its antiophidic potential. Moreover, the distinct effect of pharmacogens as antioxidant agents and distinct effect of astilbin and rutin under MPO sheds light on the different anti-inflammatory mechanisms of bioactive compounds present in H. eriogyne extracts, with high potential for the prospection of new pharmacological agents.

01 Nov 2024·Indian Journal of Medical Microbiology

Vulvovaginal candidiasis in pregnant women attending a tertiary care centre in North-Eastern India

Article

Author: Roy, Mahuya ; Majumdar, Tapan ; Ray, Jayanta

BACKGROUNDCandida colonisation in vagina was found to be 20 %, rising to 30 % during pregnancy. According to studies, the prevalence of VVC during pregnancy is higher than healthy women. During pregnancy, candidal colonisation increases, both symptomatic and asymptomatic. However, the difference between strains causing symptomatic infection and those that cause asymptomatic infection is unknown.OBJECTIVEThis study aimed to compare the virulence factors of Candida VVC isolates from symptomatic and asymptomatic pregnant women.METHODSThe study included 120 pregnant women- 60 symptomatic and 60 asymptomatic, who presented to the Obstetrics and Gynaecology Outpatient Department with vaginitis symptoms. High vaginal swabs from the patient and used for gram stain, direct wet mount, pH detection and fungal culture in SDA with and without antibiotics. Germ tube tests, growth in CMA, and HiCrome Candida Differential Agar were used to identify yeast colonies grown in culture. The isolates were then examined for virulence factors like biofilm formation, phospholipase, coagulase, and hemolysin. Antifungal susceptibility was determined using E-test.RESULTSThe current study reveals a high prevalence of Vulvovaginal Candidiasis in pregnant women(35 %). Asymptomatic patients had lower proportion of VVC than symptomatic patients. Non albicans Candida(NAC) outnumbered Candida albicans. Although Candida albicans growth was predominant in asymptomatic patients. Virulence studies revealed that Candida spp. isolated from symptomatic patients expressed a higher proportion of virulence factors. Besides NAC has higher proportion of expressing virulence factors than Candida albicans and has higher propensity to cause infection especially in symptomatic pregnant women. Antifungal susceptibility testing shows Itraconazole to be most sensitive for VVC treatment but Candida albicans was most susceptible to fluconazole while NAC had the least.CONCLUSIONSThe study emphasizes the importance of routine screening of symptomatic pregnant women for VVC, as syndromic treatment will increase antifungal resistance, particularly in NAC.

18 Oct 2024·Molecular biology reports

Exploring the potential therapeutic benefits of 7-methoxy coumarin for neuropathy pain: an in vivo, in vitro, and in silico approach.

Article

Author: Parthasarathy, Parameswari Royapuram ; Karthikeyan, R ; Venkataraman, Sowmyalakshmi ; Shanmugasundaram, Jaikumar ; Cheriyan, Binoy Varghese ; Ramakrishnan, Prakash ; Ramasamy, Kavitha ; Roy, Anitha

BACK GROUND7-Methoxycoumarin (7-MC) is well recognized for its anti-inflammatory and anti-nociceptive actions. Its capacity to lessen neuropathic pain hasn't been documented yet. Hence the impact of 7-MC on vincristine-induced peripheral neuropathic pain in rodents was investigated. The investigation also looked at the impact of 7-MC in reducing neuropathic pain via voltage-gated calcium channels and phospholipase enzyme inhibition using pertinent in vitro and in silico methods.METHODS AND RESULTSVincristine (0.1 mg/kg, i.p., daily) was administered continuously for 7 days to induce peripheral neuropathic pain in mice, with cold allodynia and thermal hyperalgesia and evaluated on the 8th day using the acetone bubble test and hot water tail immersion test. In order to derive the mechanistic approach for ameliorating neuropathic pain, the role of 7-MC in the inhibition of the phospholipase enzyme, gene expression studies on voltage-gated calcium channels using mouse BV2 microglial cells and in silico studies for its calcium channel binding affinity were also performed. The test compounds reduced vincristine-induced cold allodynia and thermal hyperalgesia in mice in a dose-dependent experiments. In vitro studies on phospholipase inhibition by 7-MC showed an IC₅₀ of 27.08 µg/ml and down-regulated the gene expression of calcium channels in the BV2 microglial cell line. In silico docking scores for 7-MCwere higher than the standard drug gabapentin.CONCLUSIONThe compound 7-MC has shown promise in alleviating vincristine-induced peripheral neuropathicin mice. Studies conducted in parallel, both in silico and in vitro have demonstrated that 7-MC effectively reduces neuropathic pain. This pain reduction is achieved through two mechanisms: inhibiting the phospholipase enzyme and blocking voltage-gated calcium channels.

Analysis

Perform a panoramic analysis of this field.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis

phospholipase

Basic Info

Related

Analysis