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Status:
US Previously Marketed
Source:
Oleic Acid U.S.P.
(1921)
Source URL:
First marketed in 1921
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Elaidic acid is the 9-trans isomer of oleic acid. It is a monounsaturated trans-fatty acid, which can be found in partially hydrogenated cooking oils. It was revealed, that elaidic acid inhibits HHT and HETE formation in human platelets incubated with arachidonic acid. Also was shown, that trans oleic acid increased plasma CETP activity, which increases low-density lipoprotein (LDL) cholesterol and decreases high-density lipoprotein (HDL).
Status:
Possibly Marketed Outside US
First approved in 2023
Source:
sugar management gummies by XIAN CHIANG COMPANY LIMITED
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Berberine, an alkaloid isolated from Rhizoma Coptidis, is known to have a wide array of therapeutic effects including antimicrobial, antineoplastic, and hepatoprotective effects. It is found in several plants including European barberry, goldenseal, goldthread, Oregon grape, phellodendron, and tree tumeric. Berberine seems to slightly reduce blood sugar levels in people with diabetes. Berberine might lower blood pressure. Berberine is possibly safe for most adults for short-term use when taken by mouth or applied to the skin.
Status:
Possibly Marketed Outside US
Source:
Dexinling by Shenzhen Deyintang Biotechnology Co., Ltd.
(2022)
Source URL:
First approved in 2022
Source:
Dexinling by Shenzhen Deyintang Biotechnology Co., Ltd.
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Sesamin is a naturally occurring compound found in sesame oil and in the bark and fruit of certain plant species. SESAMIN, (±)- is a racemic dl-form. The dl-form is also known as fagarol, and may be isolated from the bark of various fagara species. Sesamin, either as the d-form or the dl-form, has now been found to possess psychotropic activity, i.e., administration of appropriate dosages to a human or animal subject elicits a psychotropic response. Sesamin is catered to be a nutritional supplement that confers antioxidant and antiinflammatory effects (if touting its health properties) or possibly being an estrogen receptor modulator and fat burner (if targeting athletes or persons wishing to lose weight).
Sesamin has a few mechanisms, and when looking at it holistically it can be summed up as a fatty acid metabolism modifier. It appears to inhibit an enzyme known as delta-5-desaturase (Δ5-desaturase) which is a rate-limiting enzyme in fatty acid metabolism; inhibiting this enzyme results in lower levels of both eicosapentaenoic acid (EPA, one of the two fish oil fatty acids) as well as arachidonic acid, and this mechanism appears to be relevant following oral ingestion. The other main mechanism is inhibiting a process known as Tocopherol-ω-hydroxylation, which is the rate-limiting step in the metabolism of Vitamin E; by inhibiting this enzyme, sesamin causes a relative increase of vitamin E in the body but particularly those of the gamma subset (γ-tocopherol and γ-tocotrienol) and this mechanism has also been confirmed to be active following oral ingestion. Sesamin is a potent and specific inhibitor of delta 5 desaturases in polyunsaturated fatty acid biosynthesis. Sesamin inhibits particular CYP3A enzymes that are involved in vitamin E metabolism, where the enzyme initially ω-hydroxylates vitamin E (required step) and then the rest of vitamin E is subject to fat oxidation. By inhibiting this step, sesamin causes an increase in circulating and organ concentrations of vitamin E. Sesamin is thought to have PPARα activating potential in the liver, but it is uncertain how much practical relevance this has in humans due to this being a mechanism that differs between species.
Status:
Possibly Marketed Outside US
Source:
Ultra Brightening Serum by Ultraceuticals US, LLC
(2021)
Source URL:
First approved in 2021
Source:
Ultra Brightening Serum by Ultraceuticals US, LLC
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Hydroxyresveratrol (Oxyresveratrol) is a major active compound in the heartwood of Artocarpus lacucha. It was first isolated from the heartwood of Artocarpus lakoocha, and has also been found in various plants, including Smilax China, Morus alba, Varatrum nigrum, Scirpus maritinus, and Maclura pomifera. Oxyresveratrol, an aglycone of mulberroside A, has been produced by microbial biotransformation or enzymatic hydrolysis of a glycosylated stilbene mulberroside A, which is one of the major compounds of the roots of M. alba.
Oxyresveratrol plays an important role in anti-tyrosinase, antioxidant, anti-inflammatory, antiviral and neuroprotective properties. There are many A. lacucha commercial products available on the market for skin whitening and anti-aging effects. OxyResvenox™ is the registered trademark of Oxyresveratrol from Sabinsa. Oxyresveratrol is an analog of Resveratrol and is of synthetic origin. The hydroxystilbene compounds including oxyresveratrol and resveratrol showed the potent inhibitory effect on tyrosinase activity. Oxyresveratrol is also naturally present in Morus alba L., Morus bombycis. Oxyresveratrol exhibits a potent inhibitory effect on dopa oxidase activity of tyrosinase
which catalyzes rate-limiting steps of melanin biosynthesis. Oxyresveratrol showed superoxide scavenging effects with the IC50 values 3.81 ± 0.5 uM,
Oxyresveratrol exhibited a DPPH free radical scavenging effect (IC50 = 23.4 ± 1.5 uM).
Oxyresveratrol also showed hepatoprotective effects with EC50 values 32.3 ± 2.62 uM, on
tacrine-induced cytotoxicity in human liver-derived Hep G2 cells. Oxyresveratrol significantly inhibited LPS-evoked nuclear translocation of NF-kappaB and
cyclooxygenase-2 (COX-2) activity in RAW 264.7 cells.
The results suggest that the anti-inflammatory properties of oxyresveratrol might be
correlated with inhibition of the iNOS expression through down-regulation of NF-kappaB
binding activity and significant inhibition of COX-2 activity. Oxyresveratrol revealed a dose-dependent neuroprotective effect in an in vivo stroke model.
This may prove to be beneficial for a therapeutic strategy to limit brain injury in acute brain ischemia.
Status:
Possibly Marketed Outside US
Source:
21 CFR 333A
(2020)
Source URL:
First approved in 2020
Source:
21 CFR 333A
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Dimethyl succinate is the inactive analog of dimethyl fumarate. Dimethyl succinate has a pleasant, ethereal, winey odor and a fruity, winey, and burning flavor. It is used in foods as a flavoring ingredient. Dimethyl succinate was found at increased concentrations in the culture medium of the lung cancer cell line A549 and in the urine of mice implanted with A549 cells. Dimethyl succinate could be used to prolong the insulinotropic action of GLP-1 in the treatment of type-2 diabetes and it may represent a novel therapeutic approach in endotoxemia and multiple-organ failure.
Status:
Possibly Marketed Outside US
First approved in 2016
Source:
M020
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Uric acid, generated from the metabolism of purines, has proven and emerging roles in human disease. Humans produce large quantities of uric acid. Excess serum accumulation of uric acid can lead to a type of arthritis known as gout. Hyperuricemia may increase risk factors for cardiovascular disease. High serum uric acid was associated with higher risk of type 2 diabetes and other diseases.
Status:
Possibly Marketed Outside US
First approved in 2014
Source:
21 CFR 352
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Palmitoleic acid, commonly known as omega-7, is a rare monounsatured fatty acid, which was generally reported to benefit the skin in promoting epithelialisation, and certain gynaecological problems (vaginal mycoses). Until now, sea buckthorn (Hippophae rhamnoides), a shrub widely found in Europe and Asia, and macadamia nuts have been the principal sources. Palmitoleic acid (PMA) has anti-inflammatory and antidiabetic activities. Palmitoleic acid is a gap junction uncoupler.
Status:
Possibly Marketed Outside US
Source:
21 CFR 352
(2013)
Source URL:
First approved in 2013
Source:
21 CFR 352
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Methylinositol is a natural product in the family of inositols. It is found in many foods as well as pine tree bark. Methylinositol is found naturally in many foods and is commercially available as an approved food supplement. Methylinositol can mediate insulin action to improve glycemic control and insulin sensitivity in patients with type 2 diabetes mellitus, especially in patients with insulin resistance. It plays a positive role in regulating insulin-mediated glucose uptake in the liver through translocation and activation of the PI3K/Akt signaling pathway. The compound also modulates gamma-secretase to reduce A-betta production while sparing cleavage of the gamma-secretase substrate Notch. Methylinositol improves cognitive function and memory deficits in preclinical models of Alzheimer's disease (AD) neuropathology. Methylinositol was will tolerated in the population of AD subjects of varying age and severity. No serious adverse effects were detected in clinical trials. Many plant-derived compounds have excellent therapeutic potential against various human ailments. It was shown, that methylinositol mitigates tumor growth by modulating interleukins and hormones and induces apoptosis in rat breast carcinogenesis through inhibition of NF-κB.
Status:
Possibly Marketed Outside US
First approved in 2011
Source:
21 CFR 352
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Resveratrol, a natural non-flavonoid polyphenol, exhibits a wide range of beneficial properties as an anticancer agent, a platelet anti-aggregation agent, and an antioxidant, as well as its anti-aging, anti-inflammatory, antiallergenic. This compound is in phase III clinical trials in combination with carboxymethyl-β-glucan for improving nasal symptoms in children with pollen-induced allergic rhinitis. Also in phase III clinical trial in the treatment of painful knee osteoarthritis and in type 2 diabetic patients. It has been demonstrated that resveratrol may prevent type 2 diabetic by targeting Sirtuin type 1 (SIRT1), indicating that SIRT1 may be a novel therapeutic target for diabetes prevention.
Status:
Possibly Marketed Outside US
First approved in 2011
Source:
EnLyte by Jaymac Pharma
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Pyridoxal phosphate (PLP, pyridoxal 5'-phosphate, P5P) is a coenzyme, the active form of vitamin B6. Pyridoxal 5′-phosphate (PLP) is used as a cofactor for a wide range of enzymes including mitochondrial cysteine desulfurase, cystathionine γ-synthase (CGS), ornithine 4,5-aminomutase (OAM), and d-serine dehydratase. The versatility of PLP arises from its ability to covalently bind the substrate, and then to act as an electrophilic catalyst, thereby stabilizing different types of carbanionic reaction intermediates. PLP acts as a coenzyme in all transamination reactions, in various beta-elimination reactions, in the condensation reaction in heme synthesis.