Clinical management of severe acute respiratory infection (SARI) when COVID-19 disease is suspected *notes to self

Tanshinone IIa


Pharm:

Antibacterial (Escherichia coli, MIC = 50μg/mL;
Staphylococcus aureus ATCC-25923, MIC = 100μg/mL; Bacillus pyocyaneus ATCC-27853, MIC = 50μg/mL; hemolytic streptococcus, MIC = 12.5μg/mL); antithrombotic; used in treatment of myocardial ischemia and myocardial infarction; acetylcho50 > 140μmol/L, Argentatin A, IC50 = 42.8μmol/L)[4944];
iNOS inhibitor (RAW267.4 cells, LPS-induced, IC50 >50μmol/L)[5032];
anti-inflammatory (NO, IL-1β, IL-6 and TNF-α production inhibitor, suppresses expression of iNOS)[5481];
immunosuppressant InRt = −24%, 20μg/mL, InRt = 35%, 80μg/mL, InRt = 46%, control Dexamethasone, 50μg/mL, InRt = 63%)


Source:
DAN SHEN Salvia miltiorrhiza [SAGE]


Chinese Herbs and Altitude Sickness: Lessons from Hypoxic Pulmonary Hypertension Research

[link to www.sciencemag.org (secure)]

Tanshinone IIA, which mimics the action of acetazolamide (5), achieved its effect by inhibiting hypoxia-induced
Ca2+ responses, although it was endothelium independent and partially mediated by opening Ca2+-activated K+ channels.

Another potent drug for treating HPH is Rhodioloside, one of the active components of R. rosea. Rhodioloside research has benefited from multidisciplinary studies. Similar to treatment with Verapamil, a calcium channel blocker, Rhodioloside inhibited acute hypoxia-induced proliferation of PASMCs in rabbit lung (6), and increased the expression of nitric oxide synthase and inhibited KCl-induced cell contraction in vascular smooth muscle cells (7). Pretreatment with Rhodioloside increased arterial oxygen saturation by 3% in a group of young men acutely exposed to an altitude of 3,658 m (unpublished data). Together, this provides evidence supporting a possible anti-HPH effect of Rhodioloside.
Our ongoing research with R. rosea is focused on mechanistic studies and active-site chemistry using chemically engineered analogues.
Preliminary results demonstrate that one analogue, benzyl galactosidase, has an effect similar to Rhodioloside (8).

Hydroxychloroquine & Salycilic acid & Coronavirus

New study provides key insights into aspirin's disease-fighting abilities

Summary:
A new explanation has been found for how aspirin works in the body to reduce the risk of heart disease and certain cancers. Aspirin's active form, salicylic acid, blocks a protein called HMGB1, which triggers inflammation in damaged tissues. The new findings may explain the disease-preventing effects of a low-dose aspirin regimen and offer hope that more effective aspirin-like drugs may be developed for a wide variety of diseases.

The Klessig group identified two derivatives of salicylic acid, which are far more effective than salicylic acid in blocking HMBG1's pro-inflammatory activities. They synthesized one compound in the lab, while a second was isolated from a licorice plant used as a Chinese medicinal herb .

"We've identified both synthetic and natural derivatives of salicylic acid which are 50 to 1000 times more potent than salicylic acid or aspirin in suppressing the pro-inflammatory activity of extracellular HMGB1," said Klessig, "thereby providing proof of concept that more effective salicylic acid-based drugs are attainable."

[link to www.sciencedaily.com (secure)]

A genome-wide screen for human salicylic acid (SA)-binding proteins reveals targets through which SA may influence development of various diseases

The natural salicylate amoB1 from the medicinal legume Glycyrrhiza foetida (commonly called licorice) also was included in these assays, as it inhibits the disease-associated activity of two previously identified SABPs, HMGB1 and GAPDH, with greater potency than salicylic acid

Pathogenic role of HMGB1 in SARS?

Abstract
High mobility group box 1 protein (HMGB1) is released by necrotic cells or activated macrophages/monocytes, and functions as a late mediator of lethal systemic and local pulmonary inflammation. Passive immunization with anti-HMGB1 antibodies confers significant protection against lethal endotoxemia, sepsis, and acute lung injury, even when antibodies are administered after the onset of these diseases.

[link to www.ncbi.nlm.nih.gov (secure)]

EGCG Epigallocatechin gallate & Quercetin PLUS zinc from

t=2648




more EGCG Epigallocatechin gallate & Quercetin PLUS zinc

EGCG Epigallocatechin gallate & Quercetin PLUS zinc from

t=2648




more EGCG Epigallocatechin gallate & Quercetin PLUS zinc



more EGCG Epigallocatechin gallate & Quercetin PLUS zinc

[link to www.ncbi.nlm.nih.gov (secure)]

SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii

In summary, we have identified quinone-methide triterpene derivatives as novel SARS-CoV 3CLpro inhibitors. The newly identified bioactive compounds with SARS-CoV 3CLpro inhibitory activity in the μM range include celastrol (1), pristimerin (2), tingenone (3) and iguesterin (4). Although all isolated quinone-methide triterpenes has previously been known compounds, this is the first time it has been shown to possess SARS-CoV 3CLpro inhibitory activity.

interleukin-1
---------------



Celastrol
Tripterine

Pharm:
Anti-inflammatory (rat, 0.5mg/kg, strongly inhibits cotton ball granuloma, 0.1~1.0μg/mL, inhibits PGE2 induced by (inhibits activity of interleukin-1 in mus enterocelia macrophages, inhibits production of interleukin-2 in mus splenocyte, reduces synovioblasts to release PGE2 in rbt);
antioxidant (IC50 = 7μmol/L);
immunomodulator (strongly inhibits formation of platelet cell in mus spleen, significantly inhibits mus delayed hypersensitive reaction); immunosuppressant (inhibits reproduction of mus spleen cells caused by PHA, ConA and LPS, inhibits reproduction of lymphocytes);
Spermaticidal (gpg, in vitro);
hypnotic (extends mus sleeping time induced by pentobarbital);
anti-inflammatory (modulator of cytokine network:
inhibits LPS-stimulated IL-1β production on hmn monocytes, mean IC50 = 56nmol/L)[4416];
anti-inflammatory (modulator of cytokine network: decreases and macrophages, IC50 = 30~100nmol/L)[4416];
anti-inflammatory (NO production inhibitor)[4415];
anti-inflammatory (in vitro, NF-κB inhibitor, IC50 = (0.27±0.01)μmol/L;
NO production inhibitor, IC50 = (0.23±0.02)μmol/L; control Aminoguanidine, IC50 = (16.3±0.4)μmol/L)[4604];
cytotoxic (KB, IC50 = (1.6±0.1)μmol/L, control Podophyllotoxin, IC50 =0.014μmol/L)[3969];
antibacterial (Bacillus cereus, MIC = 4.44μmol/L, control Chloramphenicol, MIC = 6.19μmol/L; Staphylococcus epidermidis, MIC = 1.11μmol/L, Chloramphenicol, MIC = 12.38μmol/L; Micrococcus luteus, MIC =4.44μmol/L, Chloramphenicol, MIC = 6.19μmol/L)[3969].

Source:
CU MAO NAN SHE TENG Celastrus strigillosus,
GAO MEI YING BAN Crossopetalum gaumeri (root), (Christmasberry family)
HEI MAN Tripterygium regelii,
LEI GONG TENG Tripterygium wilfordii,
MEI ZHOU NAN SHE TENG Celastrus scandens, (American bittersweet)
NAN SHE TENG GEN Celastrus orbiculatus [Syn. Celastrus articulatus] (root: yield = 0.13%dw) ( Asian bittersweet)





Sinensetin

Pharm:
Antifungal;
cytotoxic (EAC in vitro, 30μg/mL, InRt = 50%);
induces cell differentiation (mus myelocytic leukemia cells, 50μmol/L, growing rate = 62%, 5μmol/L, growing rate = 81%, 50μmol/L and 5μmol/L, activity of macrophages >10%, HL-60 cells, 100μmol/L, growing rate = 50%, 50μmol/L, growing rate = 73%, 50μmol/L, activity of macrophages >25%, 5μmol/L, activity of macrophages = 10%);
antihistamine (inhibits histamine release, basophiles, due to antigen and TPA, IC50 = 44 and 26μmol/L respecttively);
inhibits oxidation of linoleic acid (IC50 = 114μmol/L);
inhibits tissue factor express (induced by hmn interleukin-1 in hyalin leukocyte, IC50 = 10μmol/L); 15-lipoxygenase inhibitor.

Source:
HUA ZHOU YOU Citrus grandis var. tomentosa, (Pomelo)
JIAO GAN Citrus tankan, ( tankan mandarin)
JIU LI XIANG Murraya paniculata [Syn. Chalcas paniculata], (orange jasmine)
JU PI Citrus reticulata, (Mandarin orange)
LONG XU TENG Bauhinia championii,
MAO XU CAO Clerodendranthus spicatus, (Cat's whiskers)
SHENG HONG JI Ageratum conyzoides,
TIAN CHENG Citrus sinensis, (oranges)
ZHI KE Citrus aurantium, (bitter orange)
ZHI SHI Citrus aurantium, (bitter orange
ZONG ZHUANG HUA LI Chenopodium championii. (Goosefoots)

phenylpropanoids






(E)-3-(3,4-Dimethoxyphenyl)-2-propen-1-yl (Z)-2-[(Z)-2-methyl2-butenoyloxymethyl] butenoate

Pharm:

Anti-inflammatory (

NF- B inhibitor,
hmn monocytes,
prevents LPS-induced cytokines (IL-1, IL-6, TNF, IL-8) release and PGE2 synthesis:

unstimulated control:
PGE2 = 0.54pg/mL,
IL-6 = 0.97pg/mL,
IL-1β= 0pg/mL,
TNF-α = 0.02pg/mL,
IL-8 = 3.45pg/mL;

LPS (10ng/mL):
PGE2 = 19.24pg/mL,
IL-6 = 71.42pg/mL,
IL-1β = 3.61pg/mL,
TNF-α = 2.66pg/mL,
IL-8 = 235.18pg/mL;

LPS (10ng/mL +compound 1μg/mL):
PGE2 = 6.58pg/mL,
IL-6 = 52.23pg/mL,
IL-1β = 1.25pg/mL,
TNF-α = 1.18pg/mL,
IL-8 = 158.3pg/mL).


Source: GUAN MU CHAI HU Bupleurum fruticosum (aerial parts)




1-(3,4,5-Trimethoxyphenyl)-2-propenyl 2-(2-methyl-2Z-butenoyloxymethyl)-2Z-butenoate

Pharm:

Anti-inflammatory (
NF- B inhibitor,
hmn monocytes,
prevents LPS-induced cytokines (IL-1, IL-6, TNF, IL-8) release and PGE2 synthesis:

unstimulated control:
PGE2 = 0.54pg/mL,
IL-6 = 0.97pg/mL,
IL-1β= 0pg/mL,
TNF-α = 0.02pg/mL,
IL-8 = 3.45pg/mL;

LPS (10ng/mL):
PGE2 = 19.24pg/mL,
IL-6 = 71.42pg/mL,
IL-1β = 3.61pg/mL,
TNF-α = 2.66pg/mL,
IL-8 = 235.18pg/mL;

LPS (10ng/mL +compound 1μg/mL):
PGE2 = 3.49pg/mL,
IL-6 = 21.94pg/mL,
IL-1β = 0.86pg/mL,
TNF-α = 0.53pg/mL,
IL-8 = 41.78pg/mL).

Source: GUAN MU CHAI HU Bupleurum fruticosum (aerial parts)



--------------------



[link to www.freepatentsonline.com]

Baicalin as a treatment for SARS infection
United States Patent 7605135


The present invention relates to a pharmaceutical composition useful for the treatment of diseases associated with viruses of the order Nidovirales of the family Coronaviradae, such as Severe Acute Respiratory Syndrome (SARS) viruses in humans and other animals. In particular, this invention relates to a naturally occurring compound, namely, baicalin, extracted and purified from the Chinese medicinal plant Scutellaria baicalensis Georgi (Chinese name: Huang Qin), that exhibits potent antiviral activity against members of the order Nidovirales of the family Coronaviradae that infects humans and other animals; in particular, SARS viruses in humans (“hSARS virus”). The invention also relates to a therapeutic method, using pharmaceutical compositions comprising baicalin compounds, for the treatment, amelioration, management or prevention of diseases associated with members of the order Nidovirales of the family Coronaviradae, such as hSARS.


3. SUMMARY OF THE INVENTION
The present invention is based in part on the surprising discovery that the biologically active compound baicalin and its derivatives, extracted and purified from a Chinese medicinal herb Scutellaria baicalensis Georgi (Chinese name: Huang Qin), exhibit potent antiviral activity against strains of coronavirus that infect humans and other animals, particularly at least 10 strains of hSARS virus, which belong to the order Nidovirales of the family Coronaviradae, based on neutralization test and plaque reduction assay.





The Herbal Medicine Sho-saiko-to

[link to en.wikipedia.org (secure)]

[link to cancerres.aacrjournals.org (secure)]

Sho-saiko-to consists of seven crude ingredients extracted from
herbs, i.e.,

Bupleuri radix,
Pinelliae tuber,
Scutellariae radix,
Zizyphi fructus,
Ginseng radix,
Glycyrrhizae radix,
and Zingiberis rhizoma.

Sho-saiko-to is the most popular herbal medicine in Japan

The Herbal Medicine Sho-saiko-to

[link to en.wikipedia.org (secure)]

[link to cancerres.aacrjournals.org (secure)]

Sho-saiko-to consists of seven crude ingredients extracted from
herbs, i.e.,

Bupleuri radix,
Pinelliae tuber,
Scutellariae radix,
Zizyphi fructus,
Ginseng radix,
Glycyrrhizae radix,
and Zingiberis rhizoma.

Sho-saiko-to is the most popular herbal medicine in Japan



Chinese

Xiao Chai Hu Tang (also called XCHT, sho‐sai‐ko‐to, or Minor Bupleurum Decoction),

[link to www.ncbi.nlm.nih.gov (secure)]

Xiao Chai Hu Tang, a Chinese herbal medicine formula


Description of the intervention

Xiao Chai Hu Tang (also called XCHT, sho‐sai‐ko‐to, or Minor Bupleurum Decoction), a herbal formula, was first recorded in the Treatise on Febrile Disease (Shang Han Lun) (Zhang 2005a) in about 280 AD.

The ingredients of Xiao Chai Hu Tang formula are




Chai Hu (Bupleuri Radix, Bupleurum falcatum Linne; approximately 26%),

Ban Xia (Pinelliae Tuber,Pinellia ternata breitenbach; approximately 26%), (Ephedrine source)

Sheng Jiang (Zingiberis Rhizoma, Zingiber officinale roscoe; approximately 10%),

Da Zao (Zizyphi Fructus, Zizyphus jujuba Miller var. inermis Rehder; approximately 10%),

Ren Shen (Ginseng Radix Rubra, Panax ginseng Carl Anton von Meyer; approximately 10%),

Huang Qin (Scutellariae Radix, Scutellaria baicalensis Georgi; approximately 10%),

and Gan Cao (Glycyrrhizae Radix, Glycyrrhiza uralensis Fisher, or Glycyrrhiza glabra Linneá; approximately 10%)

(Zhang 2005a; MHLW 2016) (Note: percentages are authors' calculations)

Judy Mikovits



Thermal stability
Stable at boiling temperature (a typical extraction method)


Standard doses in oral administration in humans baicalin

~1500 mg baicalin (as tablets) [Zui YC, Modern Pharmacy (People's Army Medicinal Press (1999)];
also can be up to ~6000 mg baicalin (calculated from herb, assuming 30 g herb used; the herb may contain up to 20% as baicalin).

Serum level Cmax = 74 μg/mL

Half life

~3 hrs in humans Muto R et al., “The chemical structure of new substance as the metabolite of baicalin and time profiles for the plasma concentration after oral administration of Sho-Saiko-To in human.” Yakugaku Zasshi

Flavonoid Baicalin Inhibits HIV-1 Infection at the Level of Viral Entry

Judy Mikovits


Baicalin (BA) is a flavonoid compound purified from medicinal plant Scutellaria baicalensis Georgi and has been shown to possess anti-inflammatory and anti-HIV-1 activities. In an effort to elucidate the mechanism of the anti-inflammatory effect of BA, we recently found that this flavonoid compound was able to form complexes with selected chemokines and attenuated their capacity to bind and activate receptors on the cell surface. These observations prompted us to investigate whether BA could inhibit HIV-1 infection by interfering with viral entry, a process known to involve interaction between HIV-1 envelope proteins and the cellular CD4 and chemokine receptors. We found that BA at the noncytotoxic concentrations, inhibited both T cell tropic (X4) and monocyte tropic (R5) HIV-1 Env protein mediated fusion with cells expressing CD4/CXCR4 or CD4/CCR5. Furthermore, presence of BA at the initial stage of HIV-1 viral adsorption blocked the replication of HIV-1 early strong stop DNA in cells. Since BA did not inhibit binding of HIV-1 gp120 to CD4, we propose that BA may interfere with the interaction of HIV-1 Env with chemokine coreceptors and block HIV-1 entry of target cells. Therefore, BA can be used as a basis for developing novel anti-HIV-1 agents.

[link to www.researchgate.net (secure)]

[link to www.rebellionresearch.com (secure)]

UVC Radiation

Exposure of SARS virus to UVC radiation for six minutes results in a 400-fold reduction in infectivity. UVA and gamma radiation did not affect infectivity.[12]

Another study of SARS found 1000-fold inactivation from 15 minutes of exposure to UVC.[13]

A study of Ebola virus and MERS virus found that UVC light at >0.1 J/cm^2 reduced infectivity more than 5000-fold in both. Methylene blue plus light at >30 J/cm^2 also reduced infectivity 2000-fold in both.[14]

Far-UVC light (207-222 nm) inactivates bacteria without harm to human skin. It also reduces H1N1 infectivity by 100-fold at low doses: 2 mJ/cm^2.[15]

222-nm far-UVC light applied to a mouse wound where MRSA bacteria had been spread reduced skin bacteria concentrations by >1000-fold, just like 254-nm conventional antimicrobial UV irradiation, but only the 254-nm light increased skin thickness significantly ( a measure of skin damage.)[16]

Isoerubioside B

Pharm:

Enhances fibrinolytic activity;
platelet aggregation inhibitor;
anticoagulant (extends time of coagulation).

Source:

DA SUAN Allium sativum [GARLIC]


-------------


Licochalcone A


Pharm:

Cytotoxic (HT1080 cell line, IC50 = 57.0μmol/L)[4470]; anti-inflammatory (mus, 0.5mg/ear, inhibits edema on ears induced by TPA and arachidonic acid);
antineoplastic (mus, in vitro inhibits TPA-induced 32P combines with phospholipid in HeLa cells, ID50 = 5.3μg/mL; in vivo inhibits papillary epithelioma induced by DMBA and TPA);
anti-HIV (20μg/mL, inhibits HIV-induced formation of giant-cell);
antiallergic (inhibits synthesis of leukotriene in polymorphonuclear neutrocyte);
xanthinoxidase inhibitor (IC50 = 56μmol/L);
antibacterial (Staphylococcus aureus, MIC = 1.95μg/mL;
Bacillus subtilis, MIC = 3.91μg/mL; methicillin-resistant Staphylococcus aureus MIC = 0.01μg/mL); antioxidant (antihemolysis induced by H2O2, free radical scavenger);
anticoagulant (hmn platelet, inhibits formation of COX metabolite TXB2 induced by arachidonic acid, IC50 = 3.9μmol/L;
12(S)-HETE Production inhibitor (IC50 = 82.3μmol/L);
antimalarial(Plasmodium falciparum strain 3D7, Dd2 in vitro; mouse, ip or orl, 3-6d, against P. yoelii plasmodial lethal infection).

Source:

ZHANG GUO GAN CAO Glycyrrhiza inflata, [LICORICE]
HUANG GAN CAO Glycyrrhiza kansuensi [LICORICE]

-----------------


Danshensuan B

Salvianolic acid B

Pharm:

Free radical scavenger;
fibrinolytic function;
increases coronary flow;
antioxidant (inhibits lipid peroxidization strongly, induced by vitamin Cnicotinamide ADP and Fe2+-cysteine in microsome of murine cerebral, hepatic and renal cells);
main component of phenol character acid in Salvia miltiorrhiza.

Source: DAN SHEN Salvia miltiorrhiza [SAGE]

coumarin

Antithrombotic


10, 920, 921, 2102, 2266, 5440, 6700, 7978, 10684,
12420, 15635, 17568, 17978, 18378, 20009, 20121, 20686, 21157,
22497


Allicin - Allium
Alliin - Allium
Baicalein - Skullcap
Dicoumarin - red clover
Fucosterol - Wakame, coconut
Hydroxysafflor yellow A - Carthamus tinctorius [Safflower]
Labiatenic acid/Rosmarinic acid - Mint, Rosemary
Nobiletin - Citrus
Proto-iso-erubioside B - Allium
Quercetin-3-O-neohesperidoside - plum flower/marigold/guava
Skullcapflavone II - skullcap
Soyasaponin A1 - soy
Tanshinone IIa - sage
2,3,5,4'-Tetrahydroxystilbene-2-O-β-D-glucoside - Japanese knotweed
Vincristine - periwinkle
2-Vinyl-1,3-dithia-4-cyclohexene - allium

Thread: Doctors totally understand SarsCov2 mechanism and how to treat it

[link to www.ncbi.nlm.nih.gov (secure)]

Different extraction methods of biologically active components from propolis: a preliminary study


Propolis is widely used in apitherapy, preparations, and food and beverage additives. Various extraction techniques were applied in the extraction of the biologically active constituents of poplar type propolis in order to compare their efficiency. The methods employed were: traditional maceration extraction, ultrasound extraction (UE), and microwave assisted extraction (MAE).

Results
The total amounts of extracted phenolics and flavonoids were determined, and the effectiveness of the methods compared. MAE was very rapid but led to the extraction of a large amount of non-phenolic and non-flavonoid material. UE gave the highest percentage of extracted phenolics.

In the case of ultrasound extraction, the yield of biologically active constituents increases with the time. It is clear that a 30 min sonication should be sufficient to extract the available amount of phenolics and flavonoids.

Oxidative Stress

[link to www.ncbi.nlm.nih.gov (secure)]

Citrus Polyphenol Hesperidin Stimulates Production of Nitric Oxide in Endothelial Cells while Improving Endothelial Function and Reducing Inflammatory Markers in Patients with Metabolic Syndrome


Context:
Hesperidin, a citrus flavonoid, and its metabolite hesperetin may have vascular actions relevant to their health benefits. Molecular and physiological mechanisms of hesperetin actions are unknown.

Objective:
We tested whether hesperetin stimulates production of nitric oxide (NO) from vascular endothelium and evaluated endothelial function in subjects with metabolic syndrome on oral hesperidin therapy.

Design, Setting, and Interventions:
Cellular mechanisms of action of hesperetin were evaluated in bovine aortic endothelial cells (BAEC) in primary culture. A randomized, placebo-controlled, double-blind, crossover trial examined whether oral hesperidin administration (500 mg once daily for 3 wk) improves endothelial function in individuals with metabolic syndrome (n = 24).

Main Outcome Measure:
We measured the difference in brachial artery flow-mediated dilation between placebo and hesperidin treatment periods.

Results:
Treatment of BAEC with hesperetin acutely stimulated phosphorylation of Src, Akt, AMP kinase, and endothelial NO synthase to produce NO; this required generation of H2O2. Increased adhesion of monocytes to BAEC and expression of vascular cell adhesion molecule-1 in response to TNF-α treatment was reduced by pretreatment with hesperetin. In the clinical study, when compared with placebo, hesperidin treatment increased flow-mediated dilation (10.26 ± 1.19 vs. 7.78 ± 0.76%; P = 0.02) and reduced concentrations of circulating inflammatory biomarkers (high-sensitivity C-reactive protein, serum amyloid A protein, soluble E-selectin).

Conclusions:
Novel mechanisms for hesperetin action in endothelial cells inform effects of oral hesperidin treatment to improve endothelial dysfunction and reduce circulating markers of inflammation in our exploratory clinical trial. Hesperetin has vasculoprotective actions that may explain beneficial cardiovascular effects of citrus consumption.


Conclusions
We elucidated novel mechanisms of action for hesperetin to stimulate production of NO in vascular endothelial cells that may oppose atherogenic actions of proinflammatory cytokines. Our clinical translational study rigorously demonstrated daily oral consumption of hesperidin for 3-wk improved endothelial function, reduced circulating biomarkers of inflammation, and favorably altered lipid profiles in subjects with the metabolic syndrome. Cellular and physiological actions of hesperetin may help explain cardiovascular health benefits of citrus fruit consumption.

Vit C / Vit D

H1, H2 receptor antagonists

Inhibits histamine release


Chrysin

anti-inflammatory;
antimicrobial;
cytotoxic (KB, ED50 = 13μg/mL);
induces production of estrin synthetase and cruarin; antihistamine (inhibits histamine release, rat peritoneum mastocyte);
aldose reductase inhibitor (eye inhibitor, prevents COX-2 expression)[4415];
platelet aggregation inhibitor[4415].

Source:

BEI JING YANG Populus beijingensis (bark: content = 0.10%)[5508],
CI GUO SONG Pinus aristata,
DIAN HUANG QIN Scutellaria amoena,
FENG JIAO Apis mellifera ligustica,
HUANG QIN Scutellaria baicalensis,
JIA YANG Populus canadensis (bark: content =
0.10%)[5508],
JIA ZHOU SHAN SONG Pinus monticola,
MAO BAI YANG
Populus tomentosa (bark: content = 0.03%)[5508],

-----

Ciwujianosides

Pharm: Antihistamine (inhibits histamine
release, rat peritoneum giant cells, caused by anti-Ig-E).

Source: CI WU JIA Acanthopanax senticosus [siberian ginseng]

---------------


Ganoderic acid C

Pharm:
Antihistamine (inhibits histamine release, rat mastocyte in vitro, inhibits ConA-reduced histamine release, 0.4μg/mL, InRt = 15%);
cytotoxic (in vitro, HepG2, IC50 = 0.144nmol/L; Hep2,2,15, IC50 = 0.105nmol/L; CCM2, IC50 = 31.3μmol/L; P388, IC50 = 5μmol/L) [3081].

Source: LING ZHI Ganoderma lucidum (dried sporocarp: content scope of 6 origins = 0.106%~0.901%, mean content = 0.472%[5508]).


----------------


Jujubosides

Pharm:

Antihistamine (inhibits histamine release, rat peritoneum oozing cells, caused by antigen-antibody reaction, 100μmol/L, InRt = 30.3%).

Source: SUAN ZAO REN Ziziphus jujuba var. spinosa

-------------------



E-Piceatannol

Pharm:

Antineoplastic;
antifungal;
coronary vasodilator (gpg, ED50 = 13.0μg/heart);
antihistamine (inhibits histamine release, rat);
antioxidant (superoxide anion scavenger, inhibits lipid peroxidization);
antioxidant(superoxide anion scavenger (IC50 = (4.66±0.14)μmol/L, positive control (+)-Catechin, IC50 = (3.67±0.14)μmol/L)[4514];
aromatic L-amino-acid decarboxylase inhibitor (IC50 = 5μmol/L);
lipoxygenase inhibitor (10μmol/L, LTC4 in leukemia basophiles, InRt = 100%, PGD2 formation in leukemia basophiles, InRt = 75%);
monoamine oxidase A inhibitor;
antihypertensive(rat);
plant growth inhibitor;
supertoxic agent.

Source:
CHANG HUA BAN KE YA SHU Vouacapoua macropetala,
FANG JI YE BA QIA Smilax menispermoidea,
MAO CI JIN JI ER Caragana tibetica (stem),
TIAN SHAN DA HUANG Rheum wittrocki, [rhubarb]
OU ZHOU YUN SHAN Picea abies, Pericopsis angolensis,
SI CHUAN CHAN DA HUANG Rheum sp., [rhubarb]
YU DA HUANG Rheum sp [rhubarb]

---------------------


Sandosaponins

Pharm:

Antihistamine (inhibits histamine release, rat peritoneum oozing cells, caused by antigen-antibody reaction, 10μmol/L, InRt = 58.2%).

Source: BAI FAN DOU Phaseolus vulgari [common bean(s)]


---------------------------



6-Shogaol

Pharm:

Antemetic (frog, 100mg/kg);
antihypertensive (rat, 0.5mg/mL iv);
free radical scavenger;
enhances myocardial contractility and raises heart rate (in vitro rat heart, 3.6μmol/L);
antihistamine (inhibits histamine release, rat peritoneal giant cells, caused by calcium);
inhibits mesenteric venous contraction (mus, caused by arterenol and PGF2);
platelet aggregation inhibitor (due to arachidonic acid, in vitro, IC50 = 2.23μmol/L);
inhibits rat skin passive allergy;
5-lipoxygenase inhibitor;
cyclo-oxygenase inhibitor;
prostaglandin biosynthetase inhibitor (IC50 = 1.6μmol/L);
insect antifeedant (termites, 1000mg/L);
irritant;
mutagen (TA100, TA535);
nematocide;
antagonist to body temperature reduction caused by 5-HT (mus, orl, 10mg/kg);
molluscacide (toxic to shellfish);
CYP3A4 inhibitor (IC50 = 77.7μmol/L, control Ketoconazole, IC50 = 0.245μmol/L)[4669];
CYP2D6 inhibitor inactive (IC50 > 100μmol/L, control Quinidine, IC50 = 0.078μmol/L)[4669].

Source:

FANG XIANG JIANG Zingiber aromaticum (rhizome: yield = 0.000047%dw)[4669],
GAN JIANG Zingiber officinale,
SHENG JIANG Zingiber officinale


---------------------------


Sinensetin

Pharm:

Antifungal;
cytotoxic (EAC in vitro, 30μg/mL, InRt = 50%);
induces cell differentiation
antihistamine (inhibits histamine release, basophiles, due to antigen and TPA, IC50 = 44 and 26μmol/L respecttively);
inhibits oxidation of linoleic acid (IC50 = 114μmol/L);
inhibits tissue factor express (induced by hmn interleukin-1 in hyalin leukocyte, IC50 = 10μmol/L);
15-lipoxygenase inhibitor.

Source:

HUA ZHOU YOU Citrus grandis var. tomentosa,
JIAO GAN Citrus tankan,
JIU LI XIANG Murraya paniculata [Syn. Chalcas paniculata],
JU PI Citrus reticulata,
LONG XU TENG Bauhinia championii,
MAO XU CAO Clerodendranthus spicatus,
SHENG HONG JI Ageratum conyzoides,
TIAN CHENG Citrus sinensis,
ZHI KE Citrus aurantium,
ZHI SHI Citrus aurantium,
ZONG ZHUANG HUA LI Chenopodium championii

-----------------------------


Skullcapflavone II


Pharm:

Antineoplastic (ICR mus S180, biotic prolonged rate = 172%);
antithrombotic (1.0mmol/L, inhibits platelet aggregation due to collagen, InRt = 32.5%);
bradykinin antagonist;
cytotoxic (in vitro, L1210 ED50 = 1.5μg/mL);
antihistamine (inhibits histamine release, in vitro, rat peritoneal giant cells, IC50 = 15.0μmol/L);
trypsase inhibitor (IC50 = 18μmol/L);
cytotoxic (LXFL529L hmn large cell lung carcinoma cell line and HL-60, inhibits cell growth at a micromolar range)[5369];
tyrosine kinase inhibitor (tyrosine kinase of EGFR, IC50 > 60μmol/L)[5369].

Source:

DIAN HUANG QIN Scutellaria amoena,
HUANG QIN Scutellaria baicalensis (dried root: mean content = 0.055%[5508),
NIAN MAO HUANG QIN Scutellaria viscidula


---------------


Tracheloside

Pharm:

Activity of trachelogenin:
calcium antagonist (gpg, K+-induced contraction of colon bands, IC50 = 1.1μmol/L);
antihypertensive (spontaneous hypertensive rat, strong and permanent action);
cAMP phosphodiesterase inhibitor (IC50 = 227μmol/L);
antihistamine (inhibits histamine release, rat mastocyte, ConA-reduced histamine release, IC50 = 19μmol/L);
platelet aggregation inhibitor (due to ADP, 0.5mg/mL InRt = 35.4%);
PAF antagonist; smooth muscle relaxant 50 = 2.0μmol/L);
anti-HIV (in vitro, inhibits replication of HIV-1, 0.5μmol/L, InRt to HIV-1 protein p17 and p24 = 60%~70%).

Source:
LUO SHI TENG Trachelospermum jasminoides,
RI BEN LUO SHI Trachelospermum vasiaticum


----------------


Wogonoside

Pharm:

cAMP phosphodiesterase inhibitor (IC50 = 42μmol/L);
antihistamine (rat, inhibits histamine release in peritoneum giant cell, IC50 = 140μmol/L);
liver sialidase inhibitor (mus, 10μg/mL, InRt inhibits leucocyte aggregation in inflammatory exudate);
cytotoxic (LXFL529L hmn large cell lung carcinoma cell line and HL-60, inhibits cell growth at a micromolar range)[5369];
tyrosine kinase inhibitor (tyrosine kinase of EGFR, IC50 > 60μmol/L).

Source:

LIAN QIAO Forsythia suspensa,
CHUAN HUANG QIN Scutellaria hypericifolia,
DIAN HUANG QIN Scutellaria amoena,
HUANG QIN Scutellaria baicalensis (dried root: content scope of 10 samples = 1.07%∼3.24%, mean content = 2.34% ),
NIAN MAO HUANG QIN Scutellaria viscidula

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