Delving into the Latest Updates on Isoniazid/Piperine/Rifampicin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Risorine

Target

CYP3A x P-gp x RNAP

Action

inhibitors

Mechanism

CYP3A inhibitors(Cytochrome P450 3A inhibitors), P-gp inhibitors(P-glycoprotein 1 inhibitors), RNAP inhibitors(Bacterial DNA-directed RNA polymerase inhibitors)

Therapeutic Areas

Infectious DiseasesRespiratory Diseases

Active Indication

TuberculosisPulmonary Tuberculosis

Inactive Indication-

Originator Organization

Cadila Pharmaceuticals Ltd.

Active Organization

Cadila Pharmaceuticals Ltd.

Zydus Lifesciences Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

India (16 Oct 2009),

Tuberculosis

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC43H58N4O12

InChIKeyJQXXHWHPUNPDRT-ZNQWNCHJSA-N

CAS Registry13292-46-1

View All Structures (3)

The evolving dynamics of drug resistance due to tumor heterogeneity often creates impediments to traditional therapies making it a challenging issue for cancer cure. Breast cancer often faces challenges of current therapeutic interventions owing to its multiple complexities and high drug resistivity， for example against drugs like trastuzumab and tamoxifen. Drug resistance in the majority of breast cancer is often aided by the overtly expressed P-glycoprotein (P-gp) that guides in the rapid drug efflux of chemotherapy drugs. Despite continuous endeavors and ground-breaking achievements in the pursuit of finding better cancer therapeutic avenues, drug resistance is still a menace to hold back. Among newer therapeutic approaches, the application of phytonutrients such as alkaloids to suppress P-gp activity in drug-resistant cancers has found an exciting niche in the arena of alternative cancer therapies. In this work, we would like to present a black pepper alkaloid derivative known as BioPerine-loaded chitosan (CS)-polyethylene glycol (PEG) coated polylactic acid (PLA) hybrid polymeric nanoparticle to improve the bioavailability of BioPerine and its therapeutic efficacy in suppressing P-gp expression in MDA-MB 453 breast cancer cell line. Our findings revealed that the CS-PEG-BioPerine-PLA nanoparticles demonstrated a smooth spherical morphology with an average size of 316 nm, with improved aqueous solubility, and provided sustained BioPerine release. The nanoparticles also enhanced in vitro cytotoxicity and downregulation of P-gp expression in MDA-MB 453 cells compared to the commercial inhibitor verapamil hydrochloride, thus promising a piece of exciting evidence for the development of BioPerine based nano-drug delivery system in combination with traditional therapies as a crucial approach to tackling multi-drug resistance in cancers.

01 Dec 2019·Journal of Experimental & Clinical Cancer ResearchQ1 · MEDICINE

Curcumin C3 complex®/Bioperine® has antineoplastic activity in mesothelioma: an in vitro and in vivo analysis

Q1 · MEDICINE

ArticleOA

Author: Maglione, Vittorio ; Giello, Gerarda ; Filosa, Stefania ; Di Meo, Francesco ; Crispi, Stefania ; Baldi, Alfonso ; Di Pardo, Alba ; Madonna, Michele

BACKGROUNDA major limitation in the treatment for malignant mesothelioma is related to serious side effects caused by chemotherapeutics and to the development of cancer-resistance. Advances in cancer therapies have been reached thanks to the introduction of alternative approaches, such as the use of phytochemicals. Curcumin-C3complex®/Bioperine® is a commercially standardized extract containing a ratio-defined mixture of three curcuminoids and piperine that greatly increase its bioavailability. Interestingly, the anticancer effect of this formulation has been described in different studies and several clinical trials have been started, but to our knowledge none refers to human mesothelioma.METHODSCurcumin-C3complex®/Bioperine® anticancer effect was evaluated in vitro in different human mesothelioma cell lines analysing cell proliferation, colony-forming assay, wound healing assays, invasion assay and FACS analysis. In vivo anticancer properties were analysed in a mesothelioma xenograft mouse model in CD1 Nude mice.RESULTSCurcumin-C3complex®/Bioperine® in vitro induced growth inhibition in all mesothelioma cell lines analysed in a dose- and time-depended manner and reduced self-renewal cell migration and cell invasive ability. Cell death was due to apoptosis. The analysis of the molecular signalling pathway suggested that intrinsic apoptotic pathway is activated by this treatment. This treatment in vivo delayed the growth of the ectopic tumours in a mesothelioma xenograft mouse model.CONCLUSIONSCurcumin-C3complex®/Bioperine® treatment strongly reduces in vitro tumorigenic properties of mesothelioma cells by impairing cellular self-renewal ability, proliferative cell rate and cell migration and delays tumor growth in xenograft mouse model by reducing angiogenesis and increasing apoptosis. Considering that curcumin in vivo synergizes drug effects, its administration to treatment regimen may help to enhance drug therapeutic efficacy in mesothelioma. Our results suggest that implementation of standard pharmacological therapies with novel compounds may pave the way to develop alternative approaches to mesothelioma.

01 Feb 2018·Rejuvenation ResearchQ3 · MEDICINE

Dietary Supplements as Surrogate of Mediterranean Diet in Healthy Smoking Subjects

Q3 · MEDICINE

Article

Author: Di Gaudio, Francesca ; Vasto, Sonya ; Aiello, Anna ; Candore, Giuseppina ; Monastero, Roberto ; Indelicato, Serena ; Italiano, Emilio ; Caruso, Calogero ; Galimberti, Damiano ; Accardi, Giulia ; Barera, Annalisa ; Rizzo, Claudia

The interventions to slow aging, favoring active life expectancy, represent the new perspectives in ageing investigation. Some mechanisms that delay or prevent the onset of aging pathologies have been identified. Between them, a healthy lifestyle seems to reduce many risk factors. In particular, eating habits represent the most concrete, low-cost way to act on aging process. Mediterranean diet has received much attention since its antioxidant and anti-inflammatory effects have been consistently demonstrated. Unfortunately, many people follow a Western diet, poor in phytochemicals that represent the main source of beneficial effects of this dietary pattern. So, supplements administration should be considered, especially in subjects exposed to high level of oxidative stress and inflammation. So, we tested the properties of a commercial food supplement containing a series of plant polyphenols in combination with caffeine, bioperine (black pepper extract), and selenium in smoking healthy volunteers. Fifty participants have been recruited and hematochemical analyses and biochemistry tests have been performed, before and after 60 days of supplement intake. Thirteen subjects dropped out of the study. At the end of the intervention, the variation of inflammatory and oxidant markers has been evaluated, measuring urinary isoprostanes, serum advanced glycation end products, and oxidized low-density lipoproteins. The results showed that this supplement exhibits promising antioxidant and anti-inflammatory responses, especially in women, highlighting the role of supplementation in certain groups of subjects, for the control of oxidative stress as well as inflammatory status. So, its intake should be useful in delaying the onset of age-related diseases.

100 Deals associated with Isoniazid/Piperine/Rifampicin

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	J04AC51	-

R&D Status

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Tuberculosis	India	Cadila Pharmaceuticals Ltd.	16 Oct 2009
Pulmonary Tuberculosis	-	Zydus Lifesciences Ltd.	-

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00113841 (CTgov)	Not Applicable	Multiple Myeloma	42	Curcumin (Curcumin)	qppbxxfzfn(hkdhexdvog) = jtynvdcxsj mdsxnkuoia (tgdzfjwdga, tfusbiwjso - qgektuswgg) View more	-	19 Oct 2011
				Curcumin+Bioperine (Curcumin + Bioperine)	qppbxxfzfn(hkdhexdvog) = hfqmqxdhvx mdsxnkuoia (tgdzfjwdga, rzzcaxjmzo - ljpjjymmxj) View more