Botanical Source

Vicenin-2 (VCN-2), an active constituent of the medicinal herb Ocimum Sanctum Linn or Tulsi, it can effectively induce anti-proliferative, anti-angiogenic and pro-apoptotic effect in CaP cells (PC-3, DU-145 and LNCaP) irrespective of their androgen responsiveness or p53 status;VCN-2 in combination with docetaxel (DTL) synergistically inhibited the growth of prostate tumors in vivo with a greater decrease in the levels of AR, pIGF1R, pAkt, PCNA, cyclin D1, Ki67, CD31, and increase in E-cadherin; it could as a single agent and in combination with DTL in carcinoma of prostate (CaP).

Rhoifolin possesses a variety of significant biological activities including antioxidant, anti-inflammatory, antimicrobial, hepatoprotective and anticancer effects, it may be beneficial for diabetic complications through its enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and GLUT4 translocation. Rhoifolin has a radioprotective effect against radiation-induced decrease of blood platelets and cardiac biochemical lesions in whole body irradiated mice.

Neoruscogenin represents a universal pharmacological tool for RORα research due to its specific selectivity profile versus other nuclear receptors.

Camelliaside B is a natural product from Camellia oleifera Abel.

Gentiopicroside has been developed into a novel traditional Chinese drug named gentiopicroside injection, and it was approved for the treatment of acute jaundice and chronic active hepatitis by SFDA.Gentiopicroside has analgesic, smooth muscle relaxing, antibacterial, and free radical scavenging activities, it exerts anti-inflammatory effects on experimental acute colitis through attenuating the expression levels of TNF-α, IL-1β, IL-6, iNOS and COX-2.

Bacopasaponin C may have antioxidant activity, it also shows anti-leishmanial property.

Coniferin has ATP-dependent transport activity; the extracts of the Balanophora involucrate and trans-Coniferin have anti-oxidation effects; the chromogenic coniferin analog show the exclusive presence of beta-glucosidase activity in the differentiating xylem, similar to peroxidase activity.

Arjungenin shows β-glucuronidase inhibitory activity, it shows antiviral, and anti-inflammatory activities. Arjungenin exhibits moderate antibacterial activity against Staphylococcus aureus, Escherichia coli and Enterococcus faecalis (MICs within a range of 64 and 256 ug/mL). Arjungenin shows significant protection against domoic acid induced toxicity in Caco-2 cell line.

(-)-Gallocatechin gallate has cancer-preventive activities, it can precipitate cholesterol, decreasee osteoclastogenesis at 20 microM.

Harpagoside has anti-inflammatory effects, it blocks lipopolysaccharide (LPS)-induced bone loss in an inflammatory osteoporosis model, and it does not prevent ovariectomy-mediated bone erosion in a postmenopausal osteoporosis model, it may lead to a partial prevention of obesity-induced atherosclerosis by attenuating inflammatory responses. Harpagoside suppresses lipopolysaccharide-induced iNOS and COX-2 expression through inhibition of NF-κB activation. Harpagoside exerts neuroprotection effect and ameliorates learning and memory deficit appears to be associated, at least in part, with up-regulation of brain-derived neurotrophic factor (BDNF) content as well as activating its downstream signaling pathways, e.g., MAPK/PI3K pathways.

10-Deacetyl-7-xylosyl paclitaxel has long been used in Chinese clinics to treat cancer, it may target mitochondrial permeability transition pore (mPTP).

Anemoside B4(AB4) and tetrandrine(Tet) have some reversal effect on resistant to L-OHP in Lo Vo/L-OHP cells, the molecular mechanism of the resistance reverse effect was related to down-regulation of P-gp for AB4 and down-regulation of z DHHC9 for Tet.

Notoginsenoside Fc has perfect anti-platelet aggregatory effect.

(-)-Epicatechin gallate can effectively stimulates osteoblast differentiation, it has antioxidative effect against lipid peroxidation when phospholipid bilayers are exposed to aqueous oxygen radicals.

Neohesperidin is a natural new nutrition sweetener, widely existing in plants of dry citrus peel, which can be derived from extraction; since the sweetness is 1,300-1,500 times greater than that of sugar, neohesperidin are widely used in fruit juices, wines, beverages, bakeries and pharmaceutical formulations, and are particularly suitable for consumption by diabetic patients.

Sinensetin is a polymethoxylated flavonoids in citrus fruit, as a novel antiangiogenesis agent, has potential for anti-carcinogenesis, antitumor, and cardiovascular protective activity.

Chicoric acid, a new compound able to enhance insulin release and glucose uptake, it is a new potential antidiabetic agent carrying both insulin sensitizing and insulin-secreting properties. Chicoric acid has antiobesity effects, it can induce apoptosis in 3T3-L1 preadipocytes through ROS-mediated PI3K/Akt and MAPK signaling pathways. L-Chicoric acid has antiviral activity against HIV-1, which has been attributed to the inhibition of HIV-1 integration.

Phytolaccagenin has promising antifungal activity against ATCC standard cultures of Candida albicans and Cryptococcus neoformans, and against clinical isolates of these fungi, it also shows inhibitory effects on lipopolysaccharide-induced NO production, and haemolytic activities.

Isofraxidin has definite anti-bacterial, anti-oxidant, analgesic,and anti-inflammatory activities, it inhibits expression of MMP-7 and in vitro cell invasion at a non-toxic level through inhibiting ERK1/2 phosphorylation in hepatoma cell lines.Isofraxidin is one possible radio-protector, it can protect leukemia cells from radiation-induced apoptosis via ROS/mitochondria pathway in a p53-independent manner.

Schisantherin A exhibits anti-tussive, sedative, anti-inflammatory, antioxidant, anti-osteoporotic, neuroprotective, cognition enhancing, and cardioprotective activities. Schisantherin A can significantly attenuate Aβ1-42-induced learning and memory impairment and noticeably improve the histopathological changes in the hippocampus. Schisantherin A exhibits neuroprotection against 1-methyl-4-phenylpyridinium ion (MPP(+)) through the regulation of two distinct pathways including increasing CREB-mediated Bcl-2 expression and activating PI3K/Akt survival signaling.

Aconine can inhibit RANKL-induced osteoclast differentiation in RAW264.7 cells by suppressing NF-κB and NFATc1 activation and DC-STAMP expression.

Sarsasapogenin is a steroidal sapogenin, that is the aglycosidic portion of a plant saponin. It is named after sarsaparilla (Smilax sp.), a family of climbing plants found in subtropical regions. It was one of the first sapogenins to be identified, and the first spirostan steroid to be identified as such.  The identification of the spirostan structure, with its ketone spiro acetal functionality, was fundamental in the development of the Marker degradation, which allowed the industrial production of progesterone and other sex hormones from plant steroids.

Astilbin has insecticidal, antioxidant, antibacterial, and anti-inflammatory activities, it may act as an efficient therapeutic agent for arthritis like cyclosporine A but with less toxicity, its mechanism includes a selective suppression on lymphocyte functions via reducing MMP and NO production. Astilbin can exert an early renal protective role to diabetic nephropathy (DN), inhibit production of transforming growth factor-beta1 (TGF-beta1) and connective tissue growth factor (CTGF).Astilbin also alleviates contact hypersensitivity through a unique mechanism involving a negative cytokine regulation through stimulating IL-10, which is distinct from the immunosuppressant cyclosporin A.

Phellodendrine chloride has anti-nephritic activity, may be due to its ability to inhibit the proliferation or the migration of macrophages and cytotoxic T lymphocytes in the glomeruli.

Sesaminol possesses antioxidative activity, can inhibit lipid peroxidation in rat liver and kidney.

Saikosaponin C (SSC) is one of the saikosaponins that are consisted in a Chinese herb, Radix Bupleuri, it yields a potent effect on inducing human umbilical vein endothelial cells (HUVECs) viability and growth, also induces endothelial cells migration and capillary tube formation.

Eupatilinthe has anti-proliferative effect in MCF10A- ras cells, is associated with its blockade of cell cycle progression which appears to be attributable in part to inhibition of ERK1/2 activation.

Afzelin, isolated from Cornus macrophylla, has antibacterial effects on Pseudomonas aeruginosa, its minimum inhibitory concentration (MIC) is 31 μg/mL.

Hydroxy-alpha-sanshool exerts antiobesity and hypolipidemic activities in HFD rats by reducing liver oxidative stress and thus could be considered as a potential candidate drug to cure or prevent obesity and hyperlipidemia. It also has analgesic properties, it activates TRPV1 and TRPA1 in sensory neurons.

Saikosaponin B2(SSb2) is an efficient inhibitor of early entry, including neutralization of virus particles, preventing viral attachment, and inhibiting viral entry/fusion, SSb2 may be of value for development as an antagonist of entry and could be explored as prophylactic treatment during the course of liver transplantation.

3-oxo-Olean-12-en-28-oic acid and kulinone have cytotoxic effects, with IC50 values of 5.6-21.2 μg/mL.

Pinoresinol diglucoside is a putative α-glucosidase inhibiting compound, has antihypertensive activity. It is a heat shock factor 1 inducer, increased expression of HSF1 by a factor of 1.041 at 3 μM.