scholarly journals Solubility and Bioavailability Enhancement of Oridonin: A Review

Molecules ◽  
2020 ◽  
Vol 25 (2) ◽  
pp. 332 ◽  
Author(s):  
Yuanyuan Zhang ◽  
Shaohua Wang ◽  
Mengmeng Dai ◽  
Jijuan Nai ◽  
Liqiao Zhu ◽  
...  

Oridonin (ORI), an ent-kaurene tetracyclic diterpenoid compound, is isolated from Chinese herb Rabdosia rubescens with various biological and pharmacological activities including anti-tumor, anti-microbial and anti-inflammatory effects. However, the clinical application of ORI is limited due to its low solubility and poor bioavailability. In order to overcome these shortcomings, many strategies have been explored such as structural modification, new dosage form, etc. This review provides a detailed discussion on the research progress to increase the solubility and bioavailability of ORI.

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 51
Author(s):  
Huili Shao ◽  
Bingqian Li ◽  
Huan Li ◽  
Lei Gao ◽  
Chao Zhang ◽  
...  

Toad venom contains a large number of bufadienolides, which have a variety of pharmacological activities, including antitumor, cardiovascular, anti-inflammatory, analgesic and immunomodulatory effects.. The strong antitumor effect of bufadienolides has attracted considerable attention in recent years, but the clinical application of bufadienolides is limited due to their low solubility and poor bioavailability. In order to overcome these shortcomings, many strategies have been explored, such as structural modification, solid dispersion, cyclodextrin inclusion, microemulsion and nanodrug delivery systems, etc. In this review, we have tried to summarize the pharmacological activities and structure–activity relationship of bufadienolides. Furthermore, the strategies for solubility and bioavailability enhancement of bufadienolides also are discussed. This review can provide a basis for further study on bufadienolides.


2022 ◽  
Vol 2022 ◽  
pp. 1-11
Author(s):  
Zhe Li ◽  
Tingting Zhao ◽  
Jiaxin Li ◽  
Qingying Yu ◽  
Yu Feng ◽  
...  

Natural products have antitumor, anti-inflammatory, antioxidant, and other pharmacological activities and are an important source of drugs for prevention and treatment of various diseases. However, the inherent defects of natural products in physiological media such as poor solubility and stability and short biological half-life limit their clinical application. In recent years, more and more attention has been paid to the science of drug delivery by nanoscale materials. A large number of in vitro and in vivo studies have further confirmed the efficacy and safety of nanomedicine based on natural products in preclinical models of various diseases. In this review, we summarized the achievements of nanomaterials in improving the efficacy of natural products, introduced the research progress in several key fields of natural product-based nanomedicine in medical application, and discussed the challenges and prospects of clinical transformation of nanomedicine.


2016 ◽  
Vol 7 (1) ◽  
pp. 355-363 ◽  
Author(s):  
Hongming Lv ◽  
Wenzhi Ren ◽  
Yuwei Zheng ◽  
Lidong Wang ◽  
Gejin Lu ◽  
...  

Tenuigenin (TNG), isolated from the root of the Chinese herb Polygala tenuifolia, possesses various biological and pharmacological activities, including anti-oxidation and anti-inflammation activities.


2019 ◽  
Vol 25 (6) ◽  
pp. 715-728 ◽  
Author(s):  
Hai-Yue Lan ◽  
Bin Zhao ◽  
Yu-Li Shen ◽  
Xiao-Qin Li ◽  
Su-Juan Wang ◽  
...  

Momordica cochinchinensis (Lour.) Spreng (M. cochinchinensis) is a deciduous vine that grows in Southeast Asia. It is known as gac in Vietnam and as Red Melon in English. Gac is reputed to be extremely benificial for health and has been widely used as food and folk medicine in Southeast Asia. In China, the seed of M. cochinchinensis (Chinese name: Mu biezi) is used as traditional Chinese medicine (TCM) for the treatment of various diseases. More than 60 chemical constituents have been isolated from M. cochinchinensis. Modern pharmacological studies and clinical practice demonstrate that some chemical constituents of M. cochinchinensis possess wide pharmacological activities, such as anti-tumor, anti-oxidation, anti-inflammatory, etc. This paper reviews the phytochemistry, pharmacological activities, toxicity, and clinical application of M. cochinchinensis, aiming to bring new insights into further research and application of this ancient herb.


2019 ◽  
Vol 19 (16) ◽  
pp. 1298-1368 ◽  
Author(s):  
Ankit Jain ◽  
Poonam Piplani

: Triazole is a valuable platform in medicinal chemistry, possessing assorted pharmacological properties, which could play a major role in the common mechanisms associated with various disorders like cancer, infections, inflammation, convulsions, oxidative stress and neurodegeneration. Structural modification of this scaffold could be helpful in the generation of new therapeutically useful agents. Although research endeavors are moving towards the growth of synthetic analogs of triazole, there is still a lot of scope to achieve drug discovery break-through in this area. Upcoming therapeutic prospective of this moiety has captured the attention of medicinal chemists to synthesize novel triazole derivatives. The authors amalgamated the chemistry, synthetic strategies and detailed pharmacological activities of the triazole nucleus in the present review. Information regarding the marketed triazole derivatives has also been incorporated. The objective of the review is to provide insights to designing and synthesizing novel triazole derivatives with advanced and unexplored pharmacological implications.


2020 ◽  
Vol 15 (7) ◽  
pp. 559-569 ◽  
Author(s):  
Zhen Chang ◽  
Youhan Wang ◽  
Chang Liu ◽  
Wanli Smith ◽  
Lingbo Kong

Macrophages M2 polarization have been taken as an anti-inflammatory progression during inflammation. Natural plant-derived products, with potential therapeutic and preventive activities against inflammatory diseases, have received increasing attention in recent years because of their whole regulative effects and specific pharmacological activities. However, the molecular mechanisms about how different kinds of natural compounds regulate macrophages polarization still unclear. Therefore, in the current review, we summarized the detailed research progress on the active compounds derived from herbal plants with regulating effects on macrophages, especially M2 polarization. These natural occurring compounds including flavonoids, terpenoids, glycosides, lignans, coumarins, alkaloids, polyphenols and quinones. In addition, we extensively discussed the cellular mechanisms underlying the M2 polarization for each compound, which could provide potential therapeutic strategies aiming macrophages M2 polarization.


2021 ◽  
Vol 16 (2) ◽  
pp. 229-240
Author(s):  
Manisha P. More ◽  
Anuja S. Motule ◽  
Prajakta N. Dongare ◽  
Prerna A. Patinge ◽  
Rahul D. Jawarkar ◽  
...  

In the present review, we are highlighted various pharmacognostic and pharmacological aspects of the different parts of plant Ginkgo biloba. Leaves are mainly potential source of phytochemical constituents. The plant encompasses variety of pharmacological activities namely antioxidant, hypolipidemic, antibacterial, etc. The pharmacological profile of plant is mainly attributed to the presence of chemicals such as Ginkgolide A, Ginkgolide B, Ginkgolide C, Bilobalide, Ginkgotoxin, ginkgolides and bilobalide are the major constituents. The pills with the highest concentration of plant extract (100 mg) allow the intake of the highest antioxidants concentration. It is also used along with 5-flurouracil in cancer treatment. There is need to explore more activities of the plant.


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