scholarly journals Advances in Biosynthesis, Pharmacology, and Pharmacokinetics of Pinocembrin, a Promising Natural Small-Molecule Drug

Molecules ◽  
2019 ◽  
Vol 24 (12) ◽  
pp. 2323 ◽  
Author(s):  
Xiaoling Shen ◽  
Yeju Liu ◽  
Xiaoya Luo ◽  
Zhihong Yang

Pinocembrin is one of the most abundant flavonoids in propolis, and it may also be widely found in a variety of plants. In addition to natural extraction, pinocembrin can be obtained by biosynthesis. Biosynthesis efficiency can be improved by a metabolic engineering strategy and a two-phase pH fermentation strategy. Pinocembrin poses an interest for its remarkable pharmacological activities, such as neuroprotection, anti-oxidation, and anti-inflammation. Studies have shown that pinocembrin works excellently in treating ischemic stroke. Pinocembrin can reduce nerve damage in the ischemic area and reduce mitochondrial dysfunction and the degree of oxidative stress. Given its significant efficacy in cerebral ischemia, pinocembrin has been approved by China Food and Drug Administration (CFDA) as a new treatment drug for ischemic stroke and is currently in progress in phase II clinical trials. Research has shown that pinocembrin can be absorbed rapidly in the body and easily cross the blood–brain barrier. In addition, the absorption/elimination process of pinocembrin occurs rapidly and shows no serious accumulation in the body. Pinocembrin has also been found to play a role in Parkinson’s disease, Alzheimer’s disease, and specific solid tumors, but its mechanisms of action require in-depth studies. In this review, we summarized the latest 10 years of studies on the biosynthesis, pharmacological activities, and pharmacokinetics of pinocembrin, focusing on its effects on certain diseases, aiming to explore its targets, explaining possible mechanisms of action, and finding potential therapeutic applications.

Author(s):  
Ganesh Kumar Y ◽  
Pranitha D ◽  
Phaneendra D ◽  
Madhava Reddy Ch

Various types of conditions exist in the body that causes fever and pain. Drugs that are used to treat fever are called antipyretics, and those are usually prescribed to treat elevated body temperature. But those drugs result in many other side effects like ulcers, perforations, bleedings and obstructions, which make their use questionable and limiting. Medicinal plants are used in the treatment of diseases from the starting of the human race and the process; they had been subjected to rigorous investigations and tests to establish a scientific proof and validation of the various pharmacological activities and their respective mechanisms of action in treating the herbs. Considering the anti-inflammatory properties of the plant, Xylocarpus mekongesis was investigated for its antipyretic activity in yeast method and 3doses out of which 00mg/kg body weight showed a better activity compared to the standard drug and other extracts too. The mechanism of action was similar to the paracetamol action that is inhibition of prostaglandin synthesis.


2020 ◽  
pp. 41-45
Author(s):  
G. R. Kuchava ◽  
E. V. Eliseev ◽  
B. V. Silaev ◽  
D. A. Doroshenko ◽  
Yu. N. Fedulaev

The aim of the study was to assess the course and outcome of cerebral infarction, depending on the age factor and duration of stay in the neuroblock. Materials and methods: a dynamic observation of 494 patients, men and women, aged 38–84 years with acute ischemic stroke of hemispheric localization, which were divided into the three groups depending on age, was performed. Group 1 – younger than 60 years old, group 2–60–70 years old, group 3 – older than 60 years. All patients underwent standard therapy, according to the recommendations for the treatment of ischemic stroke. The patients underwent comprehensive clinical and instrumental monitoring, which included assessment of somatic and neurological status according to the NIH‑NINDS scales at 1st, 3rd, 10th days and at discharge or death; assessment of the level of social adaptation according to the Bartel scale on 1st, 3rd, 10th days and at discharge, clinical and biochemical blood tests, computed tomography of the brain. Assessment of the quality of therapy was carried out according to specially developed maps using methods of statistical correlation analysis. Results: the most pronounced positive dynamics of neurological status was in the 1st group of patients. The regression of neurological deficit in the 2nd group was worse. The minimal dynamics of neurological deficit was in the 3rd group of patients with cerebral stroke. Most often, the death of patients with cerebral stroke occurred from the development of multiple organ disorders. Conclusions: patients over 70 years of age have the greatest risk of death, due to: a decrease in the reactivity of the body, the presence of initially severe concomitant somatic pathology in patients with admission to hospital; accession of secondary somatic and purulent‑septic complications.


2018 ◽  
Vol 24 (14) ◽  
pp. 1533-1550 ◽  
Author(s):  
Jong-Eun Kim ◽  
Ki Won Lee

Skin is a protective organ and the largest of the human body. Due to its pivotal role in aesthetic appearance, skin health has a significant impact on quality of life. Chronic inflammation of the skin often marks the beginning of various skin diseases. Immune-mediated responses serve to protect the body from external insults and require succinct control, and can lead to ongoing cellular damage and various skin conditions if left unchecked. Studies have shown that phytochemicals can alter processes involved in skin inflammation and alleviate the effects of aging, cancer, atopic dermatitis, psoriasis, and vitiligo. Direct molecular targets of some phytochemicals have been identified and their precise mechanisms of action investigated. In this review, we summarize recent findings on the effects of phytochemicals on skin inflammation and the mechanisms of action involved.


2020 ◽  
Author(s):  
Guanghui Xu ◽  
Yuhao Wang ◽  
Hushan Zhang ◽  
Xueke She ◽  
Jianjun Yang

Neuroendocrine neoplasias (NENs) are a heterogeneous group of rare tumors scattered throughout the body. Surgery, locoregional or ablative therapies as well as maintenance treatments are applied in well-differentiated, low-grade NENs, whereas cytotoxic chemotherapy is usually applied in high-grade neuroendocrine carcinomas. However, treatment options for patients with advanced or metastatic NENs are limited. Immunotherapy has provided new treatment approaches for many cancer types, including neuroendocrine tumors, but predictive biomarkers of immune checkpoint inhibitors (ICIs) in the treatment of NENs have not been fully reported. By reviewing the literature and international congress abstracts, we summarize the current knowledge of ICIs, potential predicative biomarkers in the treatment of NENs, implications and efficacy of ICIs as well as biomarkers for NENs of gastroenteropancreatic system, lung NENs and Merkel cell carcinoma in clinical practice.


2021 ◽  
Vol 22 (8) ◽  
pp. 4207
Author(s):  
Nikola Tułowiecka ◽  
Dariusz Kotlęga ◽  
Andrzej Bohatyrewicz ◽  
Małgorzata Szczuko

Introduction: Cardiovascular diseases including stroke are one of the most common causes of death. Their main cause is atherosclerosis and chronic inflammation in the body. An ischemic stroke may occur as a result of the rupture of unstable atherosclerotic plaque. Cardiovascular diseases are associated with uncontrolled inflammation. The inflammatory reaction produces chemical mediators that stimulate the resolution of inflammation. One of these mediators is lipoxins—pro-resolving mediators that are derived from the omega-6 fatty acid family, promoting inflammation relief and supporting tissue regeneration. Aim: The aim of the study was to review the available literature on the therapeutic potential of lipoxins in the context of ischemic stroke. Material and Methods: Articles published up to 31 January 2021 were included in the review. The literature was searched on the basis of PubMed and Embase in terms of the entries: ‘stroke and lipoxin’ and ‘stroke and atherosclerosis’, resulting in over 110 articles in total. Studies that were not in full-text English, letters to the editor, and conference abstracts were excluded. Results: In animal studies, the injection/administration of lipoxin A4 improved the integrity of the blood–brain barrier (BBB), decreased the volume of damage caused by ischemic stroke, and decreased brain edema. In addition, lipoxin A4 inhibited the infiltration of neutrophils and the production of cytokines and pro-inflammatory chemokines, such as interleukin (Il-1β, Il-6, Il-8) and tumor necrosis factor-α (TNF-α). The beneficial effects were also observed after introducing the administration of lipoxin A4 analog—BML-111. BML-111 significantly reduces the size of a stroke and protects the cerebral cortex, possibly by reducing the permeability of the blood–brain barrier. Moreover, more potent than lipoxin A4, it has an anti-inflammatory effect by inhibiting the production of pro-inflammatory cytokines and increasing the amount of anti-inflammatory cytokines. Conclusions: Lipoxins and their analogues may find application in reducing damage caused by stroke and improving the prognosis of patients after ischemic stroke.


Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1214
Author(s):  
Imane Zalegh ◽  
Mohamed Akssira ◽  
Mohammed Bourhia ◽  
Fouad Mellouki ◽  
Naima Rhallabi ◽  
...  

Resistance to drugs is reaching alarming levels and is placing human health at risk. With the lack of new antimicrobials drugs, infectious diseases are becoming harder to treat. Hence, there is an increasing awareness of active phytochemicals with therapeutic functions. The tremendous research interest on the Cistus L. genus includes numerous plants used in traditional medicine by people living around the Mediterranean Sea, also resulted in some interesting discoveries and written literature. This review aimed at gathering scientific literature about Cistus species, describing phytochemical profiles and the various pharmacological activities. We also extensively reviewed the antimicrobial activities, including antiviral, antiparasitic, antifungal, and antibacterial potentials of Essential Oils (EO), raw extracts as well as isolated compounds. Mechanisms of action along with methods used are also investigated in this review. Considering the findings of the Cistus species extracts, this genus offers an adequate reserve of active phytochemicals since many have been used to create drugs. Therefore, this review work can serve society by providing a global view on Cistus L. sp. regarding pharmacological potentials and their chemical profiles.


2001 ◽  
Vol 13 (4) ◽  
pp. 245-249 ◽  
Author(s):  
Jürgen Braun ◽  
Filip de Keyser ◽  
Jan Brandt ◽  
Herman Mielants ◽  
Joachim Sieper ◽  
...  

2017 ◽  
Vol 70 (1) ◽  
pp. 26-33 ◽  
Author(s):  
Joyce A. Nettleton ◽  
Ingeborg A. Brouwer ◽  
Johanna M. Geleijnse ◽  
Gerard Hornstra

At a workshop to update the science linking saturated fatty acid (SAFA) consumption with the risk of coronary heart disease (CHD) and ischemic stroke, invited participants presented data on the consumption and bioavailability of SAFA and their functions in the body and food technology. Epidemiological methods and outcomes were related to the association between SAFA consumption and disease events and mortality. Participants reviewed the effects of SAFA on CHD, causal risk factors, and surrogate risk markers. Higher intakes of SAFA were not associated with higher risks of CHD or stroke apparently, but studies did not take macronutrient replacement into account. Replacing SAFA by cis-polyunsaturated fatty acids was associated with significant CHD risk reduction, which was confirmed by randomized controlled trials. SAFA reduction had little direct effect on stroke risk. Cohort studies suggest that the food matrix and source of SAFA have important health effects.


2017 ◽  
Vol 14 (06) ◽  
pp. 1750063 ◽  
Author(s):  
A. M. Hegab ◽  
S. A. Gutub ◽  
A. Balabel

This paper presents the development of an accurate and robust numerical modeling of instability of an interface separating two-phase system, such as liquid–gas and/or solid–gas systems. The instability of the interface can be refereed to the buoyancy and capillary effects in liquid–gas system. The governing unsteady Navier–Stokes along with the stress balance and kinematic conditions at the interface are solved separately in each fluid using the finite-volume approach for the liquid–gas system and the Hamilton–Jacobi equation for the solid–gas phase. The developed numerical model represents the surface and the body forces as boundary value conditions on the interface. The adapted approaches enable accurate modeling of fluid flows driven by either body or surface forces. The moving interface is tracked and captured using the level set function that initially defined for both fluids in the computational domain. To asses the developed numerical model and its versatility, a selection of different unsteady test cases including oscillation of a capillary wave, sloshing in a rectangular tank, the broken-dam problem involving different density fluids, simulation of air/water flow, and finally the moving interface between the solid and gas phases of solid rocket propellant combustion were examined. The latter case model allowed for the complete coupling between the gas-phase physics, the condensed-phase physics, and the unsteady nonuniform regression of either liquid or the propellant solid surfaces. The propagation of the unsteady nonplanar regression surface is described, using the Essentially-Non-Oscillatory (ENO) scheme with the aid of the level set strategy. The computational results demonstrate a remarkable capability of the developed numerical model to predict the dynamical characteristics of the liquid–gas and solid–gas flows, which is of great importance in many civilian and military industrial and engineering applications.


Stroke ◽  
2012 ◽  
Vol 43 (suppl_1) ◽  
Author(s):  
Tareq Kass-Hout ◽  
Maxim Mokin ◽  
Omar Kass-Hout ◽  
Emad Nourollahzadeh ◽  
David Wack ◽  
...  

Objective: To use the Computed Tomography Perfusion (CTP) parameters at the time of hospital admission, including Cerebral Blood Volume (CBV) and Permeability Surface area product (PS), to identify patients with higher risk to develop hemorrhagic transformation in the setting of acute stroke therapy with intravenous thrombolysis. Methods: Retrospective study that compared admission CTP variables between patients with Hemorrhagic Transformation (HT) acute stroke and those with no hemorrhagic transformation. Both groups received standard of care intravenous thrombolysis with tPA. Twenty patients presented to our stroke center between the years 2007 - 2011 within 3 hours after stroke symptoms onset. All patients underwent two-phase 320 slice CTP which creates CBV and PS measurements. Patients were divided into two groups according to whether or not they had HT on a follow up CT head without contrast, done within 36 hours of the thrombolysis therapy. Clinical, demographic and CTP variables were compared between the HT and non-HT groups using logistic regression analyses. Results: HT developed in 8 (40%) patients. Patients with HT had lower ASPECT score ( P =.03), higher NIHSS on admission ( P= .01) and worse outcome ( P= .04) compared to patients who did not develop HT. Baseline blood flow defects were comparable between the two groups. The mean PS for the HT group was 0.53 mL/min/100g brain tissue, which was significantly higher than that for the non-HT group of 0.04 mL/min/100g brain tissue ( P <.0001). The mean area under the curve was 0.92 (95% CI). The PS threshold of 0.26 mL/min/100g brain tissue had a sensitivity of 80% and a specificity of 92% for detecting patients with high risk of hemorrhagic transformation after intravenous thrombolysis. Conclusions: Admission CTP measurements might be useful to predict patients who are at higher risk to develop hemorrhagic transformation after acute ischemic stroke therapy.


Sign in / Sign up

Export Citation Format

Share Document