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Lotus Leaf Extract

Model: Nuciferine 1% 2% HPLC; 10:1, 20:1 TLC

Lotus Leaf Extract
Latin Name: Nelumbo nucifera Gaertn
Used Part: Leaf
Active ingredient: Nuciferine, Flavonoids, citric acid, oxalate
Specification: Nuciferine 1% 2% HPLC; 10:1, 20:1 TLC
CAS NO. : 475-83-2
Molecular Weight: 295.3755
Molecular Formula: C19H21NO2
Appearance: Brown yellow powder
Particle Size100% through 80 mesh
Function: Help weight loss
ApplicationMedicine, food additive, dietary supplement

Introduction of Lotus Leaf
Medicinally lotus leaves mean the dried leaves of Nelumbo nucifera Gaertn., a plant in the family nymphaeaceae. The harvesting time is usually on summer and autumn because the quality then is the best. Next, they need to be dried in the sun with humidity below 30 percent, remove the petiole, folded into a semicircular shape or folding fan, and then dried thoroughly.

Main chemical constituents in lotus leaf include roemerine, nuciferine, nornuciferine, armepavine, pronuciferine, N-nornuciferine, anonaine, liriodenine, asimilobine, N-norarmepavine, lirinidine, quercetin, leucocyanidin, leucocyanidin, nelunboside, oxalic acid, succinic acid, malic acid, citric acid, tartaric acid, gluconic acid, tannins, and so on.

Nuciferine is an alkaloid found within the plants Nymphaea caerulea and Nelumbo nucifera. It has a profile of action associated with dopamine receptor blockade. It induces sedation, hypothermia, ptosis, and (in higher doses) catalepsy; it inhibits spontaneous motor activity, conditioned avoidance response, amphetamine toxicity and stereotypy. Nuciferine may also potentiate morphine analgesia. The median lethal dose in mice is 289 mg/kg. It is structurally related to apomorphine.

Nuciferine ((R)-1,2- dimethoxyaporphine) is an alkaloid initially isolated from lotus leaf, which is the leaves of Nelumbo nucifera Gaertn. Nuciferine has been reported to show remarkable biological activities, including antioxidant, antimicrobial, anti-HIV, anti-obesity, anti-hyperlipidemic and hypotensive properties. It was also found to stimulate insulin secretion by increasing intracellular calcium and stimulating cAMP responsive pathway, reduce the development of atherosclerosis by inhibiting vascular smooth muscle cell proliferation and migration, inhibit nicotineinduced non-small cell lung cancer progression by reducing the activity of Wnt/β-catenin signaling, restore potassium oxonate-induced hyperuricemia and kidney inflammation. Given these pharmacological properties and salutary effects, nuciferine is a promising drug candidate.

Chemical Composition
Pharmacologically active constituents have been isolated from the seed, leaf, flower, and rhizome. The chemical constituents include alkaloids, steroids, triterpenoids, flavonoids, glycosides, and polyphenols, as well as a variety of minerals. The seeds are rich in protein, amino acids, unsaturated fatty acids, minerals, starch, and tannins. Numerous alkaloids are the major secondary metabolites in the seeds. A description of the chemical composition of the seed polysaccharides is also available.

N -nornuciferine, O -nornuciferine, nuciferine, and roemerine are the 4 main aporphine alkaloids responsible for the pharmacological properties of the plant. Numerous chemical analyses document a number of alkaloids in the leaves. Several flavonoids are located in the leaves and stamens; the stamens contain kaempferol and 7 of its glycosides. The starch in the rhizomes is comparable to maize and potato starch, with a fresh rhizome containing 31.2% starch. Vitamin content includes: thiamine (0.22 mg per 100 g), riboflavin (0.6 mg per 100 g), niacin (2.10 mg per 100 g), and ascorbic acid (1.5 mg per 100 g). An asparagine-like amino acid (2%) has also been isolated in the rhizomes.

Researches on Lotus Leaf
Numerous pharmacologic analyses have been performed on sacred lotus investigating its use as an antioxidant and hepatoprotective, as well as a treatment for diabetes, infectious disease, and hyperlipidemia. Immunomodulatory and psychopharmacologic activity have also been explored.

Antioxidant
Although the mechanism is not completely understood, antioxidant activity may be due to the presence of phenolics, alkaloids, and saponins.

In vitro and animal data
Four different chemical analyses document high antioxidant activity from the rhizome knot. A whole rhizome extract had significant scavenging activity for small carbon-centered radicals. A hydroalcoholic seed extract exhibited strong free radical scavenging activity in rats comparable with that of standard vitamin E treatment at 50 mg/kg. Chemical constituents from the seed pod have lipid auto-oxidative, lipoxygenase, and free radical scavenging activity. Lotus germ oil inhibited lipid peroxidation in mice liver and kidney tissues and blocked autohemolysis of mice red blood cells in a dose-dependent manner. High antioxidant activity was also found in the germ oil in a lipid system (ie, lard peroxidation). The phenolic compounds and tocopherols may contribute to the antioxidant activity of lotus germ oil. A leaf methanol extract exhibited concentration-dependent antioxidant activity against hemoglobin-induced linoleic acid peroxidation, which may be related to its flavonoid content.

Clinical data
No human clinical data are available regarding the antioxidant activity of sacred lotus.

Hepatoprotection
In vitro and animal data
Ethanol seed extracts exhibited hepatoprotective effects against production of serum enzymes and cytotoxicity caused by carbon tetrachloride. The extract also protected against the genotoxic and cytotoxic effects of aflatoxin B1. Armepavine, an active compound in sacred lotus, has antifibrotic effects in rats by activating the anti–NF-kappaB pathway. Armepavine yielded better results compared with silymarin (ie, milk thistle) in reducing certain metabolic parameters in hepatic fibrosis. A dose of 300 and 500 mg/kg of lotus leaf extract in rats was comparable to 100 mg/kg of silymarin against liver-induced injury by carbon tetrachloride. Hepatitis B has been treated with a combination Chinese herbal product containing sacred lotus leaf.

Clinical data
No human clinical data are available regarding the hepatoprotective activity of sacred lotus.

Immunomodulation
In vitro and animal data
A lotus seed ethanol extract inhibited cell-cycle progression, cytokine gene expression, and cell proliferation in human peripheral blood mononuclear cells (PBMCs). ( S )-armepavine from sacred lotus immunomodulatory activity, includes: (1) inhibition of concanavalin A–induced splenocyte proliferation; (2) suppression of cytokine mRNA expression in splenocytes; (3) improved kidney function with reduction of immune complex deposition and glomerular hypercellularity; and (4) reduced autoantibody and T cell-mediated cytokine production in sera.

( S )-armepavine also inhibits interleukin-2 and interferon-gamma transcripts in human PBMCs without direct cytotoxicity. Hydroalcoholic rhizome and seed extracts changed total and differential white blood cell counts, improved phagocytosis, and potentiated immune inflammatory reactions.

Clinical data
No human clinical data are available regarding the immunomodulatory activity of sacred lotus.

Infection
In vitro and animal data
Ethanol seed extracts inhibited herpes simplex virus type 1 (HSV-1) multiplication in HeLa cells without cytotoxicity by inhibiting gene expression of HSV-1. Alkaloids and flavonoids from a 95% ethanol leaf extract had anti-HIV activity. Antifungal activity against Candida albicans and antimalarial activity was found for various leaf constituents with no observed cytotoxicity. Antibacterial activity is documented for rhizome extracts against Staphylococcus aureus , Escherichia coli , Bacillus subtilis , Bacillus pumilis , and Pseudomonus aeruginosa . A rhizome extract had antifungal and antiyeast activity comparable with griseofulvin against 5 different strains of fungi and yeast, including C. albicaus , Aspergillus
niger , Aspergillus fumigatus , and Trichophytum mentagopyhtes .

Clinical data
No human clinical data are available regarding the use of sacred lotus for treating infection.

Effects on lipids and obesity
In vitro and animal data
A Chinese herbal mixture containing sacred lotus reduced serum triglycerides and cholesterol in rats fed a high-fat diet. An ethanol leaf extract stimulated lipolysis in visceral and subcutaneous adipose tissues in mice. The pathway involved the beta-adrenergic receptor mediated in energy expenditure and prevention of diet-induced obesity. The ethanol leaf extract also suppressed body weight gain in mice fed a high-fat diet. A flavonoid-enriched leaf extract reduced blood and liver lipids, lipid peroxidation, release of the liver enzymes AST and ALT, the LDL-C to HDL-C ratio, and lipid accumulation in the liver in a high-fat diet animal model. The effect of the leaf extract on the high-fat–induced lipid metabolic disorder was comparable with results of silymarin and simvastatin treatment. The flavonoids from the leaf extract may exert antiatherogenic properties by inhibiting vascular smooth muscle cell proliferation and migration.

Sacred lotus leaf extract has been used to treat obesity in
China. The effects of the leaf extract on obesity, digestive enzymes, lipid metabolism, and thermogenesis were studied in mice induced with a high-fat diet. The extract inhibited intestinal absorption of carbohydrate and lipid by inhibiting alpha-amylase and lipase; up-regulated lipid metabolism in adipocytes; prevented increases in body weight; and increased thermogenesis. An antiobesity herbal product that included sacred lotus inhibited fat accumulation by down-regulating major transcription factors in the adipogenesis pathway and lipid metabolizing enzymes utilized for accumulation of fat in adipocytes.

Clinical data
No human clinical data are available regarding the effects of sacred lotus on lipids and obesity.

Diabetes
Animal data
An ethanol rhizome extract reduced the blood sugar level of normal rats and glucose-fed hyperglycemic and streptozotocin-induced diabetic rats. In normal rats, the rhizome extract improved glucose tolerance and increased the effectiveness of injected insulin. The activity of the extract was comparable with that of tolbutamide, a sulfonylurea oral hypoglycemic drug, at 73% and 67% in normal and diabetic rats, respectively. Neferine, isolated from the green seed embryo, was comparable with rosiglitazone in enhancing insulin sensitivity and improving fasting blood glucose, triglycerides, and inflammatory cytokines in insulin-resistant rats. The mechanism of action may involve reducing release of tumor necrosis factor-alpha by activating the gamma peroxisome proliferator-activated receptor (PPAR) as well as decreasing insulin compensatory release from pancreatic islet cells. A Chinese herbal formulation decreased abnormal glucose and improved cholesterol, triglycerides, low-density lipoprotein-C (LDL-C), and high-density lipoprotein-C (HDL-C) in rats fed a high-fat diet after 4 weeks of treatment. Potential mechanisms of action include inhibition of intestinal glucosidase, inhibition of lipase, and free radical scavenging activity. 41 Quercetin and glycosides in the leaves may inhibit lens aldose reductase, an enzyme associated with diabetic complications.

Clinical data
No human clinical data are available regarding the use of sacred lotus in diabetes.

Psychopharmacologic activity
In vitro and animal data
The alkaloids asimilobine and lirinidine, isolated from the leaves of sacred lotus, inhibited the contraction of rabbit isolated aorta induced by serotonin. Neferine from lotus seed embryos may have antidepressant activity as indicated by its anti-immobility effects in mice in a forced swimming test. Neferine is a direct 5-hydroxytryptamine (5-HT) 1A receptor agonist and may inhibit 5-HT reuptake or activation of 5-HT metabolism. The antidepressant effect was comparable with that of maprotiline and imipramine. In mice, a methanol rhizome extract may improve learning and memory by enhancing neurogenesis through increased cell proliferation and cell differentiation in the dentate gyrus of the hippocampus. Sacred lotus seed extract improved scopolamine-induced dementia in rats by inhibiting acetylcholinesterase activity and inducing choline acetyltransferase expression. One study documented cholinesterase inhibitory activities from sacred lotus stamen-derived compounds. Methanol seed extracts containing neferine inhibited locomotor activity at 50 mg/kg and elicited potent effects at 100 mg/kg. Neferine induced sedation, hypothermia, antifever effects, and anxiolytic effects comparable with those of diazepam but with a different mechanism. Methanol rhizome extracts also have a minor sedative activity. Leaf extract administered to mice attenuated induced and long-term stress and appeared to have adaptogenic activity comparable with that of diazepam.

Source: https://www.drugs.com/npp/sacred-lotus.html

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