Breviscapine: A Review on its Phytochemistry, Pharmacokinetics and Therapeutic Effects

Author(s):  
Luan Wen ◽  
Ting He ◽  
AXiang Yu ◽  
Siqi Sun ◽  
Xiang Li ◽  
...  

Breviscapine is one of the extracts of several flavonoids of Erigeron breviscapus. Scutellarin is the main active component of breviscapine, and the qualitative or quantitative criteria as well. Scutellarin and its analogs share a similar skeleton of the flavonoids. Breviscapine has been widely used in the treatment of cerebral infarction and its sequelae, cerebral thrombus, coronary heart disease (CHD), and angina pectoris. Breviscapine has a broad spectrum of pharmacological activities, such as increasing blood flow, improving microcirculation, dilating blood vessels, decreasing blood viscosity, promoting fibrinolysis, inhibiting platelet aggregation, and thrombosis formation, etc. In addition, breviscapine and its analogs have significant value for drug research and development because of the superiority of those significant bioactivities. Furthermore, an increasing number of pharmacokinetic studies have explored the mechanism of scutellarin and its analogs. To provide a comprehensive understanding of the current research on breviscapine, scutellarin, and the analogs, the structural features, distribution situation, preparation method, content determination method, clinical applications, pharmacological action as well as pharmacokinetics are summarized in the present review.

2020 ◽  
Vol 15 (1) ◽  
Author(s):  
Yang Qi-yue ◽  
Zhang Ting ◽  
He Ya-nan ◽  
Huang Sheng-jie ◽  
Deng Xuan ◽  
...  

Abstract Background Indigo naturalis is a blue dye in ancient, as well as an extensive used traditional Chinese medicine. It has a wide spectrum of pharmacological properties and can be used to treat numerous ailments such as leukemia, psoriasis, and ulcerative colitis. This article aims to expand our understanding of indigo naturalis in terms of its chemical constituents, pharmacological action and clinical applications. Methods We searched PubMed, web of science, CNKI, Google academic, Elsevier and other databases with the key words of “Indigo naturalis”, and reviewed and sorted out the modern research of indigo naturalis based on our research results. Results We outlined the traditional manufacturing process, chemical composition and quality control of indigo naturalis, systematically reviewed traditional applictions, pharmacological activities and mechanism of indigo naturalis, and summarized its clinical trials about treatment of psoriasis, leukemia and ulcerative colitis. Conclusions Indigo naturalis has a variety of pharmacological activities, such as anti-inflammatory, antioxidant, antibacterial, antiviral, immunomodulatory and so on. It has very good clinical effect on psoriasis, leukemia and ulcerative colitis. However, it should be noted that long-term use of indigo naturalis may produce some reversible adverse reactions. In summarize, indigo naturalis is an extremely important drug with great value and potential.


Synlett ◽  
2021 ◽  
Author(s):  
Vinod Kumar

Hydantoin and its analogs such as thiohydantoin and iminohydantoin have received substantial attention both from a chemical and biological point of view. Several compounds of this class have shown useful pharmacological activities such as anticonvulsant, antitumor, antiarrhythmic, herbicidal, and others that lead in some cases to clinical applications. Because of broad-spectrum activities, intensive research efforts have been dedicated in industry and academia to the synthesis and structural modifications of hydantoin and its derivatives. Realizing the importance of hydantoin in organic and medicinal chemistry, we also initiated a research program to successfully design and develop the new routes/methods resulting in the formation of hydantoin, thiohydantoin, and iminohydantoin substituted at different positions particularly at the N-1 position without following protection-deprotection strategy. Given the fact that the combination of two or more pharmacophoric groups may lead to hybrid molecules which result in a mixed mechanism of action on the biological target. We, therefore, further extended the developed strategy for the synthesis of new types of hydantoin-based hybrid molecules by combining hydantoin with a triazole, isoxazoline, and phosphate scaffolds as another pharmacophoric group to exploit diverse biological functions.


Biomedicines ◽  
2021 ◽  
Vol 9 (7) ◽  
pp. 712
Author(s):  
Wei-Yun Lai ◽  
Yen-Jen Chen ◽  
Alvin Kai-Xing Lee ◽  
Yen-Hong Lin ◽  
Yu-Wei Liu ◽  
...  

Worldwide, the number of bone fractures due to traumatic and accidental injuries is increasing exponentially. In fact, repairing critical large bone defects remains challenging due to a high risk of delayed union or even nonunion. Among the many bioceramics available for clinical use, calcium silicate-based (CS) bioceramics have gained popularity due to their good bioactivity and ability to stimulate cell behavior. In order to improve the shortcomings of 3D-printed ceramic scaffolds, which do not easily carry growth factors and do not provide good tissue regeneration effects, the aim of this study was to use a gelatin-coated 3D-printed magnesium-doped calcium silicate (MgCS) scaffold with genipin cross-linking for regulating degradation, improving mechanical properties, and enhancing osteogenesis behavior. In addition, we consider the effects of fibroblast growth factor-2 (FGF-2) loaded into an MgCS scaffold with and without gelatin coating. Furthermore, we cultured the human Wharton jelly-derived mesenchymal stem cells (WJMSC) on the scaffolds and observed the biocompatibility, alkaline phosphatase activity, and osteogenic-related markers. Finally, the in vivo performance was assessed using micro-CT and histological data that revealed that the hybrid bioscaffolds were able to further achieve more effective bone tissue regeneration than has been the case in the past. The above results demonstrated that this type of processing had great potential for future clinical applications and studies and can be used as a potential alternative for future bone tissue engineering research, as well as having good potential for clinical applications.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 628
Author(s):  
Im-Sook Song ◽  
So-Jeong Nam ◽  
Ji-Hyeon Jeon ◽  
Soo-Jin Park ◽  
Min-Koo Choi

We evaluated the bioavailability, liver distribution, and efficacy of silymarin-D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) solid dispersion (silymarin-SD) in rats with acetaminophen-induced hepatotoxicity (APAP) compared with silymarin alone. The solubility of silybin, the major and active component of silymarin, in the silymarin-SD group increased 23-fold compared with the silymarin group. The absorptive permeability of silybin increased by 4.6-fold and its efflux ratio decreased from 5.5 to 0.6 in the presence of TPGS. The results suggested that TPGS functioned as a solubilizing agent and permeation enhancer by inhibiting efflux pump. Thus, silybin concentrations in plasma and liver were increased in the silymarin-SD group and liver distribution increased 3.4-fold after repeated oral administration of silymarin-SD (20 mg/kg as silybin) for five consecutive days compared with that of silymarin alone (20 mg/kg as silybin). Based on higher liver silybin concentrations in the silymarin-SD group, the therapeutic effects of silymarin-SD in hepatotoxic rats were evaluated and compared with silymarin administration only. Elevated alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase levels were significantly decreased by silymarin-SD, silymarin, and TPGS treatments, but these decreases were much higher in silymarin-SD animals than in those treated with silymarin or TPGS. In conclusion, silymarin-SD (20 mg/kg as silybin, three times per day for 5 days) exhibited hepatoprotective properties toward hepatotoxic rats and these properties were superior to silymarin alone, which may be attributed to increased solubility, enhanced intestinal permeability, and increased liver distribution of the silymarin-SD formulation.


2019 ◽  
Vol 43 (27) ◽  
pp. 10763-10773 ◽  
Author(s):  
Maryam Mousavi ◽  
Ali Nakhaei Pour

LaNiO3 and LaNi0.5Co0.5O3 as perovskites were synthesized in magnetized and non-magnetized water and the activity of the catalysts was evaluated in the methane dry reforming reaction with CO2.


2021 ◽  
Vol 11 (7) ◽  
pp. 1024-1030
Author(s):  
Li Zhang ◽  
Miao Xu ◽  
Min Zhu ◽  
Andong Liu ◽  
Fenghua Zhao

Tissue plasminogen activator (rt-PA) is a thrombolytic drug used for the treatment of stroke. However, it has a short half-life and a high risk of complications of cerebral hemorrhage, which complicates its use in clinical applications. In this study, polyethylene glycol and polycaprolactone were used as nano-carriers in the development of new nano-drug-recombinant plasminogen activator modified nanoparticles (PEG-PCL@rt-PA) loaded with rt-PA. Following treatment, the patients received with either conventional nursing or continuous nursing. Compared with traditional treatment and nursing, the nanoparticles had stronger thrombolytic and therapeutic effects, significantly improved the self-care recovery rate of patients, and reduced the occurrence of complications. This new mode of PEG-PCL@rt-PA drug therapy combined with continuous nursing is expected to improve the recovery and survival rates of stroke patients.


Author(s):  
Lav Singh ◽  
Atul K. Upadhyay ◽  
Pooja Dixit ◽  
Arpit Singh ◽  
Divyanshu yadav ◽  
...  

Background: Pinus and other related conifers belonging to family pinaceae are most commonly used medicinal plants in Indian North-western Himalayas. Various parts of these plants including needles are source of several well known alkaloids. Of all the alkaloids, piperidine group is one of important component and hold considerable medicinal importance. Methods: The group of alkaloids was initially identified from genus Piper through which a large variety of piperidine molecules have been extracted. The planar structure of this heterocyclic nucleus enables acetamide groups to be added at various ring configurations. Results: In the area of drug research, the piperidine heterocycle has gained considerable interest. To produce a new therapeutic profile, the broad range of its therapeutic application paved the way for researchers to implant the nucleus from time to time in diversified pharmacophores. Discussion: However, biological functions of piperidine metabolites have been mostly examined on a limited scale and that most of the findings are thus preliminary. We have tried to present different clinical applications of piperidine alkaloids in this study that researchers have already attempted to demystify from time to time. Conclusion: Given the importance of the piperidine nucleus, the study will enable the researcher to produce scaffolds of the highest therapeutic efficacy. We have also illustrated different types of piperidine, its sources in different member of family pinaceae with special emphasis on Pinus.


2019 ◽  
Vol 6 (1) ◽  
pp. 38
Author(s):  
Dian Kurnia ◽  
Prima Happy Ratnapuri

ABSTRAK      Lidah buaya (Aloe vera L.) diketahui mengandung banyak senyawa kimia alami, seperti antrakuinon, asam amino, acemannan, aloesin, glukomanan yang bertanggungjawab memberikan efek teraupetik yang bermanfaat dalam dunia farmasi. Review ini bertujuan untuk memberikan informasi terkait aktivitas farmakologi dan perkembangan produk dari lidah buaya dalam bidang farmasi. Pada Review artikel ini data yang disajikan diperoleh dari literatur online berupa jurnal dan artikel ilmiah publikasi lokal maupun internasional dan literatur offline berupa buku dan ­e-book. Diketahui bahwa lidah buaya memiliki berbagai aktivitas farmakologi yaitu sebagai antiinflamasi, berperan dalam penyembuhan luka, antibakteri, antifungi, antivirus, antioksidan, antikanker, antitumor, antikolesterol, dan antiulcer. Penggunaan lidah buaya dalam produk farmasi juga telah mengalami perkembangan diantaranya yaitu sediaan nano partikel, tablet, suppositoria, gel dan krim.  Kata Kunci— Aloe vera L., Aktivitas farmakologi, Perkembangan produk  ABSTRACT Aloe vera L. contains many natural chemical compounds, such as anthraquinone, amino acids, acemannan, aloesin, glucomannan which are responsible for providing therapeutic effects that are useful in pharmaceutical. The aims of this review is to provide information about pharmacological activities and products development of Aloe vera. In this article review, online and offline literatures were used. Online literature such us journals and articles obtained from local and international, while the offline literature such us books and e-books. It is known that aloe vera has a variety of pharmacological activities, that act as antiinflammatory, wound healing, antibacterial, antifungal, antiviral, antioxidant, anticancer, antitumor, anticholesterol, and antiulcer. Pharmaceutical products of Aloe vera also have been developed such us nanoparticles products, tablets, suppositories, gels and creams.  Keywords— Aloe vera L., Pharmacological activities, Products development


Author(s):  
Bahareh Sadat Yousefsani ◽  
Motahareh Boozari ◽  
Kobra Shirani ◽  
Amirhossein Jamshidi ◽  
Majid Dadmehr

Abstract Objectives Iris germanica L. is a medicinal plant, which has a long history of uses, mainly in medieval Persia and many places worldwide for the management of a wide variety of diseases. In this study, we aimed to review ethnopharmacological applications in addition to phytochemical and pharmacological properties of I. germanica. Key findings Ethnomedical uses of I. germanica have been reported from many countries such as China, Pakistan, India, Iran and Turkey. The medicinal part of I. germanica is the rhizome and the roots. Based on phytochemical investigations, different bioactive compounds, including flavonoids, triterpenes, sterols, phenolics, ceramides and benzoquinones, have been identified in its medicinal parts. Current pharmacological studies represent that the plant possesses several biological and therapeutic effects, including neuroprotective, hypoglycaemic, hypolipidaemic, antimicrobial, antioxidant, antiproliferative, anti-inflammatory, antiplasmodial, antifungal, immunomodulatory, cytotoxic and antimutagenic effects. Summary Although the majority of preclinical studies reported various pharmacological activities of this plant, however, sufficient clinical trials are not currently available. Therefore, to draw a definitive conclusion about the efficacy and therapeutic activities of I. germanica and its bioactive compounds, further clinical and experimental studies are required. Moreover, it is necessary to focus on the pharmacokinetic and safety studies on the extracts of I. germanica.


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