Synthesis of the New Furo[3,2-h]isoquinoline Alkaloid, TMC-120B from Aspergillus ustus.

: Berberine, as a representative isoquinoline alkaloid, exhibits significant hypolipidemic activity in both animal models and clinical trials. Recently, a large number of studies on the lipid-lowering mechanism of berberine and studies for improving its hypolipidemic activity have been reported, but for the most part, they have been either incomplete or not comprehensive. In addition, there have been a few specific reviews on the lipid-reducing effect of berberine. In this paper, the physicochemical properties, the lipid-lowering mechanism, and studies of the modification of berberine all are discussed to promote the development of berberine as a lipid-lowering agent. Subsequently, this paper provides some insights into the deficiencies of berberine in the study of lipid-lowering drug, and based on the situation, some proposals are put forward.

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Berberine nanoencapsulation attenuates hallmarks of scoplomine induced Alzheimer's-like disease in rats

Current Clinical Pharmacology ◽

10.2174/1574884715666200628112844 ◽

2020 ◽

Vol 15 ◽

Author(s):

Samar R. Saleh ◽

Mariam M. Abady ◽

Mohammed Nofal ◽

Nashwa W. Yassa ◽

Mohamed S. Abdel-latif ◽

...

Keyword(s):

Oxidative Stress ◽

Histopathological Examination ◽

Memory Function ◽

Amyloid Β ◽

Active Pharmaceutical Ingredient ◽

Isoquinoline Alkaloid ◽

Drug Uptake ◽

Male Rats ◽

Morris Water Maze Test ◽

Neuroprotective Effects

Background: Berberine (BBR), an isoquinoline alkaloid, acts as a multipotent active pharmaceutical ingredient to counteract several types of dementia based on its numerous pharmacological actions including antioxidant, antiinflammatory, cholesterol-lowering effect, and inhibition of Aβ production and AChE. However, BBR suffers from poor absorption, bioavailability and brain drug uptake. The present study is directed for the formulation and characterization of Chitosan BBR-nanoparticles (BBR-NPs) as well as the estimation of its neuroprotective effects against scopolamine induced cognitive impairments. Methods: BBR-NPs were formulated using ionic gelation method and tripolyphosphate was chosen as a cross linker. Nanoparticles size, zeta potential, encapsulation efficiency and releasing profile were estimated. To investigate the neuroprotective effects, adult fifty six Wistar male rats were randomly distributed into: three control groups, received saline, polyethylene glycol or chitosan- NPs respectively; induced group, received scopolamine (2 mg/ kg, i.p.) and three treated groups were orally administrated BBR (50 mg/ kg), BBR- NP (7 mg/ kg) and donepezil (2.25 mg/ kg, as positive control) followed by scopolamine injection after 40 min, daily for 4 weeks. Morris water maze test, oxidative stress parameters, cholinergic and amyloid-β processing intermediates as well as neuroplasticity markers and histopathological examination were assessed. Results: Our results showed that BBR- NPs were better than BBR and donepezil as BBR- NPs were powerful inhibitory ligands toward AChE and Aβ42 formation and significantly down regulated Tau, iNOS and BACE gene expression in rats’ hippocampus. BBR-NPs administration, at 1/6 of BBR therapeutic recommended dose, significantly improved learning and memory function. This could be accredited to the diminution of oxidative stress and amyloid-β toxicity in addition to the improvement of the neuroplasticity markers. Conclusions: The enhancing effect of BBR- NPs could be related to the enhancing of its bioavailability, absorption and brain drug uptake which need more investigation in future work.

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Mechanism Involved in Fortification by Berberine in CDDP-Induced Nephrotoxicity

Current Molecular Pharmacology ◽

10.2174/1874467213666200220142202 ◽

2020 ◽

Vol 13 (4) ◽

pp. 342-352 ◽

Cited By ~ 1

Author(s):

Vipin K. Verma ◽

Salma Malik ◽

Ekta Mutneja ◽

Anil K. Sahu ◽

Kumari Rupashi ◽

...

Keyword(s):

Oxidative Stress ◽

Renal Tissue ◽

Isoquinoline Alkaloid ◽

Experimental Models ◽

Beclin 1 ◽

Control Treatment ◽

Control Group ◽

Treatment Groups ◽

Single Intraperitoneal Injection ◽

Male Wistar Rats

Background: The activation of Nrf2/HO-1 pathway has been shown to protect against cisplatin- induced nephrotoxicity by reducing oxidative stress. Berberine (Ber), an isoquinoline alkaloid, has demonstrated antioxidant, anti-inflammatory and anti-apoptotic activities in various experimental models. Aim: To check the effect of Ber on cisplatin-induced nephrotoxicity and to explore the involved mechanism. Methods: Adult male Wistar rats were divided into 6 groups: Normal, cisplatin-control, treatment groups and per se group. Normal saline and Ber (20, 40 and 80 mg/kg; p.o.) was administered to rats for 10 days. A single intraperitoneal injection of cisplatin (8 mg/kg) was injected on 7th day to induced nephrotoxicity. On 10th day, rats were sacrificed, the kidney was removed and stored for the estimation of various parameters. Results: As compared to cisplatin-control group, Ber pretreatment improved renal function system and preserved renal architecture. It also diminished oxidative stress by upregulating the expression of Nrf2/HO-1 proteins. In addition, Ber attenuated the cisplatin mediated inflammation and apoptosis. Furthermore, it also reduced the phosphorylation of p38/JNK and PARP/Beclin-1 expression in the kidney. Conclusion: Ber attenuated renal injury by activating Nrf2/HO-1 and inhibiting JNK/p38MAPKs/ PARP/Beclin-1 expression which prevented oxidative stress, inflammation, apoptosis and autophagy in renal tissue.

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Berberine elevates cardiolipin in heart of offspring from mouse dams with high fat diet-induced gestational diabetes mellitus

Scientific Reports ◽

10.1038/s41598-021-95353-4 ◽

2021 ◽

Vol 11 (1) ◽

Author(s):

Laura K. Cole ◽

Genevieve C. Sparagna ◽

Marilyne Vandel ◽

Bo Xiang ◽

Vernon W. Dolinsky ◽

...

Keyword(s):

Diabetes Mellitus ◽

Gestational Diabetes ◽

Gestational Diabetes Mellitus ◽

Mitochondrial Function ◽

High Fat Diet ◽

Fatty Acid Uptake ◽

Isoquinoline Alkaloid ◽

Acid Uptake ◽

High Fat ◽

Low Fat

AbstractBerberine (BBR) is an isoquinoline alkaloid from plants known to improve cardiac mitochondrial function in gestational diabetes mellitus (GDM) offspring but the mechanism is poorly understood. We examined the role of the mitochondrial phospholipid cardiolipin (CL) in mediating this cardiac improvement. C57BL/6 female mice were fed either a Lean-inducing low-fat diet or a GDM-inducing high-fat diet for 6 weeks prior to breeding. Lean and GDM-exposed male offspring were randomly assigned a low-fat, high-fat, or high-fat diet containing BBR at weaning for 12 weeks. The content of CL was elevated in the heart of GDM offspring fed a high fat diet containing BBR. The increase in total cardiac CL was due to significant increases in the most abundant and functionally important CL species, tetralinoleoyl-CL and this correlated with an increase in the expression of the CL remodeling enzyme tafazzin. Additionally, BBR treatment increased expression of cardiac enzymes involved in fatty acid uptake and oxidation and electron transport chain subunits in high fat diet fed GDM offspring. Thus, dietary BBR protection from cardiac dysfunction in GDM exposed offspring involves improvement in mitochondrial function mediated through increased synthesis of CL.

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Micromycetes-resistant colored cotton is promising material to reduce mycotoxins amounts in textiles

E3S Web of Conferences ◽

10.1051/e3sconf/202016406015 ◽

2020 ◽

Vol 164 ◽

pp. 06015

Author(s):

Kseniia Illarionova ◽

Sergey Grigoryev

Keyword(s):

Upland Cotton ◽

Federal District ◽

Cotton Fibers ◽

Rhizopus Nigricans ◽

Aspergillus Ustus ◽

Cotton Plants ◽

Colored Cotton ◽

Penicillium Aurantiogriseum ◽

The Mean ◽

White Cotton

The aim of research was to characterize epiphyte micromycetes observed on variable cotton fibers accessions, to estimate the range of fiber destruction and select cotton, which were the most resistant to fungus damage. The accessions of differently colored Upland Cotton varieties (Gossypium hirsutum L.) evaluated: eleven cotton of natural green, twelve – of brown and eleven of conventional white color. Cotton plants have been grown in Sothern Federal District, RF. The fiber samples for the study were placed into a thermostat in sterile Petri dishes on moistened filter paper in order to stimulate the development of mycelium or sporulation of fungi naturally occurred on fibers. Incubation carried out in a thermostat at a +24-28 °C, humidity of 90-100% and exposed for 28 days. The samples examined with a microscope or binocular magnifier. Aspergillus ustus (Bainier), A. fumigatus Fresen., A. niger v. Tiegh., A. flavus Link, Penicillium aurantiogriseum Dierckx, P. notatum Westling, Rhizopus nigricans Ehrenb. and Alternaria alternata (Fuier) Keissler were detected. Compared with exposed white, accession of green and brown colors were significantly resistant to fungus. The mean of destruction (K) of white cotton varied up to 0.95, but colored accessions not exceeded 0.3 (initial destruction of the surface, not affecting internal fiber’s structure).

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