Osthole 98% (Capsules) – Product Details

7-methoxy-8-(3-methyl-2-butenyl)-2H-1-benzopyran-2-one , which is also called Osthole or Osthol commonly abbreviated as OST, is a natural coumarin that was first made from the Cnidium plant. It has a chemical formula C15H16O3 and a total molecular weight(molecular mass) of 244.28. 

The mature fruit of Cnidium monnieri (Fructus cnidii), which is often used in Traditional Chinese Medicine (TCM) clinics, has a lot of Osthole. It is also found in many other medicinal plants, such as Angelica, Archangelica, Citrus, and Clausena.

Most of the health benefits of Fructus cnidii are thought to come from one of its main bioactive components, Osthole, which is thought to strengthen the immune system, improve male function, relieve rheumatic pain, and get rid of dampness. Recent studies suggest that Osthole has anti-inflammatory, anti-cancer, and immune-modulating properties.

Since multiple bioactivities of Osthole have been found, it would be good to develop Osthole and its derivatives as possible multitarget drugs. So, it’s important to look at a summary of the pharmacological and biological research on this coumarin in order to understand how it works and what all of its different functions are.[R]

Experiments done in vitro and in vivo have shown that Osthole has many pharmacological effects, such as neuroprotective, osteogenic, immunomodulatory, anticancer, hepatoprotective, cardiovascular protective, and antimicrobial effects.

Also, pharmacokinetic studies showed that the body quickly and effectively takes in and uses Osthole. Also, the mechanisms of Osthole’s many pharmacological effects are likely related to its ability to change the levels of cyclic adenosine monophosphate (cAMP) and cyclic adenosine monophosphate (cGMP), though some of these mechanisms are still not clear. [R]

Osthole 98%
CAS Number	484-12-8
Molar Mass	244.29
Chemical Formula	C15H16O3
IUPAC Name	7-Methoxy-8-(3-methylbut-2-en-1-yl)-2H-1-benzopyran-2-one

How Does Osthole Work?

Data on Osthole has been shown to control a number of signaling pathways, which in turn control a number of apoptosis-related proteins, cell cycle regulators, protein kinases, transcriptional factors, cytokines, and growth receptors linked to inflammation, proliferation, and a number of other diseases. Osthole is known to stop cancer cells from growing and spreading by stopping the cell cycle and causing them to die. [R] 

Osthole Research

Numerous animal and human studies have been conducted on the potential application of Osthole. In order to study the pharmacological properties of Osthole, researchers need to prepare stock solutions with different concentrations of the compound. This requires precise measurements of Osthole solubility and accurate calculations of the required volume of the solution. Below follows some of the relevant findings:

Osthole on Nootropic and Neuroprotective Effect

 Osthole controls the activity of ion channels and G protein-coupled receptors (GPCRs), which affects how neurons and neuroendocrine glands work. There was evidence that Osthole mediated inhibition of the L-type Ca2+ is responsible for the regulation of neuronal activity in mouse neurons. [R]

It is important to take into account that this study is done in an animal model, thus further research should be done to prove its effectiveness as a treatment to neuroprotective disorders.

Osthole on Osteogenic Activity

One of the most promising therapeutic effects of Osthole is its ability to change the shape of bones. In vitro studies have shown that Osthole and coumarin extract from FC increased the number and changed the shape of osteoblasts while decreasing the number and activity of osteoclasts.

This tipped the balance in favor of bone remodeling and increased bone density, making Osthole a possible treatment for osteoporosis.

 [R]

Osthole on Immunomodulation and Anti-Inflammatory Activity

 In the late 1990s, a German research team reported for the first time that Osthole inhibits 5-lipoxygenase (5-LO) and cyclooxygenase- (COX-) 1. Both enzymes are essential to the inflammatory process, and inhibition of COX has been shown to alleviate pain and inflammatory symptoms.

Whereas, 5-LO is a target for pharmaceutical intervention in a variety of diseases other than inflammatory diseases, such as cardiovascular disease, cancer, and osteoporosis.

In cell culture, Osthole inhibited enzymes including inducible nitric oxide synthase (iNOS), mitogen-activated protein kinases (MAPK), and COX-2 to suppress the immune response of lipopolysaccharide-stimulated macrophages. [R]

Osthole on Anticancer Effect

 The molecular mechanism of Osthole’s anticancer effect remains unknown. Combinatory effects on carcinogenesis and tumor progression are highly probable. Osthole may modulate the PI3K/Akt signaling pathway, resulting in G2/M cell cycle arrest and apoptosis in lung cancer A549 cells.

By inhibiting the c-Met/Akt/mTOR pathway, FASN, which is highly expressed in many solid tumors, is downregulated in HER2-overexpressing breast cancer cells. Osthole also normalized plasma alanine aminotransferase (ALT), which has been demonstrated to be an HCC prevention strategy.

In addition, Osthole inhibited the invasion and transition of cancer cells by inhibiting MMP-2 and MMP-9, which were induced by a series of inflammatory factors. Due to its ability to inhibit histone deacetylase, Osthole has also been shown to be a promising cancer treatment agent.[R]

Although several studies showed the promising effect of Osthole it is still recommended for further research to prove its effectiveness. 

Osthole on Hepatoprotective Effect and Benefits on Metabolic Diseases

The liver is one of the vital organs that serves as a center for nutrient metabolism and waste elimination. Osthole provides protection against hepatitis. It inhibited hepatitis B virus (HBV) secretion in cell culture  and prevented hepatitis in mice induced by concanavalin A or an anti-Fas antibody.[R]

This study was conducted in animals, so more research is needed to prove its efficacy in hepatoprotective effect 

Osthole on Vasorelaxant Properties and Cardiovascular Benefits

Osthole has a protective effect on the cardiovascular system. Vascular disease, including atherosclerosis, vein graft occlusion, and restenosis after angioplasty, is characterized by abnormal vascular smooth muscle cell proliferation, whereas osthole treatment selectively inhibits the proliferation of these vascular smooth muscle cells.

Due to its Ca2+-channel antagonistic effect and upregulation of cGMP in vascular smooth muscle, osthole demonstrated vasorelaxant properties.

Osthole has a relaxant effect not only on blood vessels, but also on other tissues such as isolated rodent ileum and taeniae coli ; trachea ; and corpus cavernosum, which partially explains the long history of using FC as a herbal treatment for male sexual dysfunction.[R]

Although Osthole gives a promising result, more research is still suggested to prove its vasorelaxant properties and cardiovascular benefits

Osthole on Antimicrobial and Antiparasitic Effect

 Osthole has antifungal effects on a variety of fungal species. Experimental evidences showed that Osthole inhibited hypha growth of Fusarium graminearum, a parasite found on common weeds and cereal crops, through glucose starvation , and controlled powdery mildew caused by Sphaerotheca fuliginea via inhibiting spore germination and mycelia growth.

Osthole derivatives had a curative effect on Phytophthora capsici-caused pepper blight. Additional antibacterial activities against both gram-positive and gram-negative bacteria have been reported.[R] 

How Osthole is prepared for research use? (Prepare Stock Solution)

Osthole is a natural compound found in many herbs and plants. It has been used in traditional Chinese medicine as herbal extract for centuries and is now gaining popularity in modern medicine as dietary supplement. Preparing stock solutions of Osthole is an important step in its use as a medicine or supplement.

Some article provide a guide to preparing stock solutions of Osthole, including the batch-specific molecular weight, how to use the dilution calculator calculate the necessary dilution , how to calculate molar mass of Osthole and solvent volumes required. 

Osthole (concentration required with purity 99.5% as determined by high-performance liquid chromatography) was isolated from the fruit of C. monnieri using purification methods.

By dissolving Osthole in dimethyl sulfoxide (DMSO), a stock solution was created and this chemical compound should be stored at 4 °C until use. Dilution required as necessary. [R]

 FAQs

Is OSTHOLE safe?

In addition to a lack of consistent evidence of direct benefits, the potential long-term effects of OSTHOLE are also unknown. Purerawz sells OSTHOLE for research purposes(lab supply) only.

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