Lupeol, also referred to as fagarsterol, is a very potent antioxidant and anti-inflammatory agent belonging to the triterpene family. Scientists have been studying this triterpene extensively for its several disease combating attributes.
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Lupeol is a member of a group of natural chemical compounds known as triterpenes, which are vital components of the cell membranes of plants. Triterpenes function in the same manner as cholesterol works in the cell membranes of animals. In other words, these compounds aid in maintaining the stability of the bi-layers in plant cells. So far, 25 different clinical researches have studied triterpenes and they have attracted the interest of the scientists as they are capable of lowering the cholesterol levels.
According to estimates by scientists in the West, every day we consume roughly 250 grams of triterpenes, which are mainly obtained from cereals, vegetables, fruits and vegetable oils. It is likely that people inhabiting the Mediterranean region as well as people whose diets typically contain high amounts of olive oil ingest much higher amounts of triterpenes.
Precisely speaking, the natural compound lupeol is found in specific plants, especially growing in the tropical rainforest. In addition, this compound also found in specific foods. Scientists have shown keen interest in lupeol and are currently studying the therapeutic properties of this natural compound. However, since the ongoing studies are just restricted to in vitro as well as animal studies, it is certainly in the initial stage of its discovery. Nevertheless, some studies have found that apparently lupeol possesses anti-cancer and anti-inflammatory properties.
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A triterpenoid that is pharmacologically active, lupeol possesses many potential therapeutic properties. This natural compound can be found in an assortment of plants, which includes Acacia visco, mango and Abronia villosa. In addition lupeol is also present in coffee and dandelion.
The credit for reporting the maiden complete or total synthesis of lupeol is attributed to Gilbert Stork.
When we talk about total synthesis we actually refer to absolute chemical synthesis of any complex molecule, frequently any natural product, from plain precursors that are commercially available. It actually means a process that does not involve the help of any biological process, distinguishing it from partial or semi-synthesis. There can be various target molecules, including organic compounds having theoretical interest, therapeutically significant active ingredients or even natural products. Generally, the intention is to discover a new method of synthesizing a target molecule, which may already have one or more existing synthesis routes. However, occasionally there may not be any existing route and the chemist's objective is to discover a practicable route. There are a number of purposes for total synthesis and one vital purpose is discovering innovative chemical reactions in addition to novel chemical reagents.
The genus Zanthoxylum comprises roughly 250 tree and shrub species belonging to the citrus family. These trees and shrubs have their origin in the sub-tropical and warm temperate regions throughout the world. The heart wood of a number of these species is yellow. Fruits of many of these trees and shrubs are used for making spice such as Sichuan pepper. Sometimes plants belonging to this genus are also used in the form of bonsai trees.
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In folk medicine, the bark of plants belonging to the genus Zanthoxylum has been traditionally used for treating colic, toothache and rheumatism. Zanthoxylum riedelianum is one of the excellent sources of lupeol. It is among the tallest trees found in the lower regions of Peru. It is interesting to note that a plant in the Philippines called Ficus pseudopalma also is a good source of lupeol. This plant has been traditionally used in the form of an herbal remedy for treating diabetes and kidney stones. Now we know that there are assortments of plants that are also good sources of lupeol. These include cucumber, white cabbage, tomato and pepper and fruits like mango, fig, olive, red grapes and strawberry.
Lupeol belongs to pentacyclic triterpenes, which are known for their antioxidant and anti-inflammatory activities. It has been found that lupeol slows down cutaneous toxicity which is brought on by benzoyl peroxide. It addition, it has been found that lupeol controls P13K/Akt and NF-κB pathways, improve alfatoxin B1 brought on by peroxidation hepatic damage, stimulate Fas-mediated apoptotic death prostate cancer cells sensitive to androgen, and also slow down the Ras signalling route. In addition to these benefits, this natural compound has also demonstrated that it possesses the aptitude to put off the consequences of DMBA, which induces DNA alkylation damage in the skin of rodents.
If you are wondering what is Ras and Ras signalling pathway actually, here is an explanation. Basically, Ras is a group of proteins which are related to one another and is found in the cell lineages as well as organs of all animals. All members of Ras protein family are members of a protein class referred to as small GTPase. Within the animal cells, these proteins have a role in transmitting signals, which is also known as cellular signal transduction. In fact, Ras is the perfect member of the proteins belonging to the Ras super family. All of them are linked in 3D structures and they govern the various behaviours of the cells.
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When incoming signals activate or "switch on" Ras, subsequently it activates other proteins. Eventually, these proteins switch on the genes that play a role in cell growth, survival as well as differentiation. Any kind of mutation in Ras genes can result in producing Ras proteins that are permanently activated. Consequently, it may result in unwanted as well as overactive signalling within the cells even when there is no incoming signal.
Since these signals are responsible for the growth as well as division of the cells, eventually overactive Ras signalling may result in the development of cancer. In fact, the 3 Ras genes found in humans are considered to be the most widespread oncogenes in cancers among humans. It has been found that mutations of Ras genes, which activate Ras permanently, are responsible for 20 to 25 percent of all tumours in humans. On the other hand, they are responsible for up to 90 percent of specific types of cancers, for instance pancreatic cancer. This is the reason why scientists are studying Ras inhibitors with a view to find an effective means to treat cancer as well as other ailments caused by permanently active Ras genes.
Ras proteins work like binary molecular switches, which govern the signalling networks between cells. The signal pathways regulated by Ras also control a number of processes like proliferation, actin cytoskeletal integrity, apoptosis, cell adhesion, differentiation, and cell migration. It has been found that in cancers Ras proteins as well as proteins regulated by Ras are often deregulated resulting in enhanced invasion as well as metastasis. On the other hand, it decreases apoptosis.
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Lupeol is known to possess anti-arthritic and anti-inflammatory properties. It is also said to be a potent phytonutrient that may possess the aptitude to alter inflammation and, at the same time, protect cartilage in people suffering from rheumatoid arthritis. Another unique property of lupeol is that it only targets the unhealthy and diseased cells, while leaving the healthy and normal cells untouched.
Since the pre-historic days, people have been using natural products as medicine for treating the diseases afflicting them. Lupeol is a triterpene as well as a phytosterol and is found extensively in many edible vegetables and fruits. Over the last three decades, scientists have undertaken extensive research to examine the therapeutic properties of this natural compound. Their findings have shown that lupeol has many vital pharmacological activities.
Different pre-clinical as well as in vitro studies undertaken on animals have hinted that lupeol possesses the potential to serve as an anti-microbial, anti-inflammatory, anti-invasive, anti-proliferative, anti-protozoal, anti-angiogenic as well as cholesterol lowering agent. Apart from undertaking various in vivo as well as in vitro studies with lupeol, scientists have also examined this natural compound for its medicinal effectiveness in treating other conditions like diabetes, kidney ailments, cardiovascular disease, arthritis and even healing wounds. The findings of these studies have revealed that pharmacologically lupeol is effectual in the treatment of a variety of ailments in pre-clinical situations (in animal models). Moreover, the studies have shown that lupeol is effective in such cases regardless of the routes used to administer this natural compound, including oral, topical, and intravenous as well as intra-peritoneal.
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