endoplasmic

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

Thapsigargin is a natural product, an inhibitor of sarcoplasmic endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.

Cyclic ADP-ribose (cADPR) is an effective calcium mobilization second messenger synthesized from NAD+ by ADP-ribosyl cyclase. It mainly increases cytosolic calcium through Ryanodine receptor-mediated endoplasmic reticulum release and extracellular influx via the opening of TRPM2 channels.

α-Lipoic Acid (DL-α-Lipoic acid) an octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.

α-Lipoic Acid (Alphalipoic acid) inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes.

Dibutyl phthalate (1,2-Benzenedicarboxylic acid) is a plasticizer, commonly used in industrial manufacturing, that causes cardiac damage by disrupting Ca(2+) transfer from the endoplasmic reticulum to the mitochondria and triggering subsequent cellular death.Dibutyl phthalate induces oxidative damage in the brain of zebrafish.

Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum

ABTL-0812 induces endoplasmic reticulum (ER) stress-mediated autophagy, and with anti-cancer activity.

Cyclopiazonic acid (CPA) is a neurotoxic secondary metabolite (SM) made by A. flavus. Cyclopiazonic acid (CPA) is an endoplasmic reticulum calcium ATPase (Ca2+ATPase; SERCA)nanomolar inhibitor and a potent inducer of cell death in plants.

Tauroursodeoxycholate (TUDCA ,Taurolite) dihydrate is a water-soluble bile acid with endoplasmic reticulum stress inhibitory, mitochondrial stabilizing, and anti-apoptotic effects, which significantly reduces the expression of apoptotic molecules, such as Caspase-3 and Caspase-12, and inhibits ERK, reducing endoplasmic reticulum stress mediated cell death.

D-Glucose 6-phosphate (G6P) is glucose that hydroxyl group on carbon 6 is phosphorylated by hexose kinase and is involved in glycolysis, gluconeogenesis, and the pentose phosphate pathway, as well as being converted to glycogen or starch storage. G6P serves as a substrate for glucose 6-phosphatase in the liver and hexose 6-phosphate dehydrogenase (H6PDH) in the lumen of the endoplasmic reticulum.

1-Deoxymannojirimycin hydrochloride, a selective α1,2-mannosidase inhibitor (IC50: 20 μM), also inhibits HIV-1 strains but exhibits poor antiviral activity.

Xestospongin C ((-)-Xestospongin C) is a selective inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor and also inhibits sarcoplasmic endoplasmic reticulum Ca2+ ATPase (SERCA). It has neuroprotective effects in APP PS1 AD mice, improving cognitive and pathological deficits associated with Alzheimer's disease.

Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum and can be reversibly converted back by the same enzymes. It can also be irreversibly converted to phosphatidylethanolamine by phosphatidylserine decarboxylase in the mitochondria. Phosphatidylserine binds to T cell immunoglobulin mucin type 1 (TIM-1) and TIM-4 receptors as well as brain-specific angiogenesis inhibitor 1 (BAI1), leading to anti-inflammatory and anti-atherosclerotic effects. It is also a cofactor involved in the activation of various signaling pathways through activation of protein kinase C, neutral sphingomyelinase, and c-Raf-1 protein kinase among others. Phosphatidylserine is externalized during apoptosis by scramblases in the plasma membrane as a signal for phagocytes to engulf the cell. Phosphatidylserines (bovine) is a mixture of bovine phosphatidylserines containing fatty acids with variable chain lengths at the sn-1 and sn-2 positions.

Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent calcium mobilization second messenger synthesized from NAD+ by ADP-ribosyl cyclase. It raises cytosolic calcium levels through Ryanodine receptor-mediated release from the endoplasmic reticulum and facilitates extracellular influx via TRPM2 channels [1][2][3].

β-D-Glucopyranosyl abscisate (ABA-GE) is a hydrolyzable conjugate of abscisic acid (ABA) that predominantly accumulates in the vacuole and likely in the endoplasmic reticulum. The deconjugation of β-D-Glucopyranosyl abscisate enables a swift release of free ABA in response to abiotic stress factors such as dehydration and salt stress, playing a crucial role in maintaining ABA homeostasis.

Daphylloside, and asperuloside can be suggested as endoplasmic reticulum stress regulators.

1. Bufotalin (Bufotaline)e is a kind of poisonous secretions of toads.

1. Acetylshikonin exhibits weak cytotoxicity against human umbilical vein endothelial cells (HUVECs) with IC5 of over 2 microM, exhibits the antiangiogenic and antitumorigenic effects by suppressing proliferation and angiogenic factors. 2. Acetylshikonin inhibits the generation of NADPH oxidase complex in the activation of respiratory burst of PMNs, but does not directly inhibit the activity of NADPH oxidase already generated. 3. Certain shikonin derivatives(such as Acetylshikonin) act as modulators of the Nur77-mediated apoptotic pathway and identify a new shikonin-based lead that targets Nur77 for apoptosis induction. 4. Acetylshikonin, shikonin, and alkannin have accelerative effect on the proliferation of granulation tissue in rats. 5. Acetylshikonin has inhibitory effect on the edematous response is due neither to the release of steroid hormones from the adrenal gland nor to the glucocorticoid activity, but probably partly to the suppression of mast cell degranulation and partly to protection of the vasculature from mediator challenge. 6. Acetylshikonin induces apoptosis of hepatitis B virus X protein-expressing human hepatocellular carcinoma cells via endoplasmic reticulum stress.

α-Lipoic Acid (Thioctic acid) sodium, an essential cofactor for mitochondrial enzyme complexes, functions as an antioxidant. It suppresses NF-κB-dependent activation of HIV-1 LTR [1] [2] [3] and induces ER (endoplasmic reticulum) stress-mediated apoptosis in hepatoma cells [4]. Furthermore, when combined with CPUL1 to form the self-assembled nanoaggregate CPUL1-LA NA, α-Lipoic Acid sodium enhances antitumor efficacy compared to CPUL1 alone [5].

Ipomoeassin F, a selective and potent inhibitor of endoplasmic reticulum (ER) protein translocation, targets the Sec61 complex's pore-forming subunit (Sec61α) at the ER membrane. It inhibits the ER membrane translocation of SARS-CoV-2 proteins and blocks the ER translocation of secretory and type I transmembrane proteins (TMPs), without affecting type III TMPs [1] [2] [3].

Demethylcantharidate disodium, an endogenous metabolite, demonstrates significant anticancer efficacy against various cancers by inducing apoptosis in hepatocellular carcinoma cells through endoplasmic reticulum (ER) stress [1].

Celangulin, an insecticidal component derived from Celastrus angulatus, functions by activating calcium channels on the plasma membrane, which leads to an increase in intracellular Ca2+ due to influx from the external environment. Additionally, Celangulin stimulates calcium channels in the endoplasmic reticulum (ER) [1].

Dehydroeffusol (Dehydro Effusol) possesses anti-cancer, anxiolytic and sedative properties. Dehydroeffusol inhibits gastric cancer cell growth and tumorigenicity by selectively inducing tumor-suppressive endoplasmic reticulum stress and a moderate apoptosis.