Kev Pom Zoo Rau Sesamolin: Physicochemical Properties, Pharmacological Activities, Thiab Kev Tshawb Fawb Yav Tom Ntej
Mar 25, 2022
Hu rau: Audrey Hu Whatsapp / hp: 0086 13880143964 Email:audrey.hu@wecistanche.com
Reny Rosalina 1 thiab Natthida Weerapreeyakul 2,3,*
1 Graduate School (Biomedical Sciences Program), Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand; renyrosalina@kkumail.com
2 Division of Pharmaceutical Chemistry, Kws Qhia Ntawv ntawm Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand
3 Human High Performance and Health Promotion Research Institute, Khon Kaen University, Khon Kaen 40002, Thaib teb
Abstract
Cov noob noob hnav muaj nplua nuj nyob hauv cov ntsiab lus lignan thiab tau paub zoo txog lawv cov txiaj ntsig kev noj qab haus huv. Tsis zoo li lwm cov sesame lignan tebchaw (piv txwv li, sesamin thiab sesamol), txoj kev tshawb fawb ntawm pharmacological kev ua ntawm sesamolin tsis tau tshawb pom dav. Qhov kev tshuaj xyuas no, yog li ntawd, sau cov ntaub ntawv ntsig txog sesamolin cov tshuaj ua haujlwm, thiab cov txheej txheem ntawm kev ua. Tsis tas li ntawd, kev cuam tshuam ntawm nws cov khoom physicochemical ntawm cov tshuaj pharmacological kuj tau tham txog. Sesamolin muaj cov tshuaj tiv thaiv neuroprotective tiv thaiv hypoxia-induced reactive oxygen hom (ROS) thiab oxidative kev nyuaj siab nyob rau hauv neuron hlwb los ntawm kev txo cov ROS thiab inhibiting apoptosis. Hauv kev mob qog noj ntshav ntawm daim tawv nqaij, sesamolin nthuav tawm cov tshuaj tiv thaiv melanogenesis los ntawm kev cuam tshuam rau kev qhia ntawm cov enzymes melanogenic. Cov tshuaj tiv thaiv mob qog noj ntshav ntawm sesamolin raws li kev tiv thaiv kev loj hlob thiab inhibition ntawm kev tsiv teb tsaws tau pom nyob rau hauv tib neeg cov kab mob qog noj ntshav. Tsis tas li ntawd, kev kho mob nrog sesamolin tuaj yeem txhawb lub cev tiv thaiv kab mob txhawm rau txhim kho cov haujlwm cytolytic los tua Burkitt's lymphoma hlwb. Txawm li cas los xij, qhov tshuaj lom thiab kev nyab xeeb ntawm sesamolin tsis tau tshaj tawm. Thiab kuj tseem muaj cov ntaub ntawv tsawg dua ntawm kev sim kawm hauv vivo. Qhov txwv aqueous solubility ntawm sesamolin dhau los ua qhov teeb meem tseem ceeb, uas cuam tshuam rau nws cov tshuaj pharmacological hauv kev sim hauv vitro thiab kev kho mob zoo. Yog li ntawd, kev txhim kho solubility yog xav tau rau kev tshawb nrhiav ntxiv thiab kev txiav txim siab ntawm nws cov kev ua haujlwm pharmacological. Txij li thaum muaj tsawg dua cov ntaub ntawv kawm txog qhov teeb meem no, nws tuaj yeem dhau los ua qhov kev tshawb fawb yav tom ntej.
Ntsiab lus: sesamolin; sesame lignan; Sesamum indicum L.; pharmacological kev ua; physicochemical zog; physicochemical kev txhim kho
1 Kev Taw Qhia
Sesamolin yog cov feem ntau paub furfural lignan cais los ntawm cov noob ntawm Sesamum Indicum L. [1,2]. Noob yog thawj zaug cog rau 4000 xyoo dhau los thiab yog li suav hais tias yog ib qho ntawm cov qoob loo qub tshaj plaws los tsim cov roj [3]. Tag nrho txhua xyoo kev tsim cov noob hnav hauv ntiaj teb yog kwv yees li 5,532,000 metric tons (MT), nrog 50 feem pua ntawm Asia thiab 30 feem pua ntawm Africa [4]. Cov noob noob hnav muaj 50 feem pua roj, 25 feem pua ntawm cov protein, thiab cov seem yog cov suab thaj, noo noo, fibers, thiab minerals, thiab feem ntau ntawm cov noob hnav lignans muaj xws li sesamolin, sesamin, sesamol, thiab sesamol muaj nyob rau hauv cov noob hnav thiab cov roj [5 ,6] ib.
Cov txiaj ntsig kev noj qab haus huv ntawm cov noob hnav tau txais txiaj ntsig zoo los ntawm nws cov ntsiab lus lignans xws li sesamin, sesamol, thiab sesamolin. Ob peb qhov kev tshuaj xyuas tsis ntev los no tau nthuav tawm cov tshuaj pharmacological ntawm cov roj noob hnav hauv vitro thiab hauv vivo thwmsim; Qee tus ntawm lawv kuj nyiam tsom mus rau cov tshuaj pharmacological ntawm sesame lignans tebchaw xws li sesamol lossis sesamin [7–10]. Sesamolin, ib qho ntawm cov noob qoob loo lignan tseem ceeb, tau tshaj tawm tias muaj cov tshuaj tiv thaiv kab mob antioxidant, neuroprotective, thiab kev tiv thaiv kab mob. Txawm li cas los xij, daim ntawv tshaj tawm hais txog kev tshawb nrhiav hauv kev ua haujlwm pharmacological ntawm sesamolin yog txwv.
Nrog rau cov kev ua ub no, ntau daim ntawv tshaj tawm qhia txog cov kev txwv physicochemical ntawm sesamolin uas tuaj yeem yog qhov tsis zoo ntawm lawv cov tshuaj pharmacological. Sesamolin muaj kev txwv dej-solubility uas ua rau nws raug cais raws li chav kawm II hauv Biopharmaceutic Classification System, uas yog chav kawm rau cov dej solubility tsawg thiab muaj cov permeability siab. Cov khoom sib xyaw ua ke ntawm cov chav kawm no xav tau kev txhim kho physicochemical zog, tshwj xeeb tshaj yog cov solubility profile, los txhim kho nws cov nyhuv pharmacological thiab tsim los ua tus neeg sib tw tshuaj [11,12]. Qhov teeb meem no yuav dhau los ua qhov teeb meem tseem ceeb rau kev tshawb fawb sesamolin cov tshuaj pharmacological, tab sis qhov no tuaj yeem dhau los ua kev tshawb fawb los txhim kho cov khoom siv hluav taws xob ntawm sesamolin txhawm rau txhim kho cov nyhuv kho. Yog li, qhov kev tshuaj xyuas no nthuav tawm cov ntsiab lus ntawm cov ntaub ntawv ntawm cov kev tshawb fawb tshiab tsis ntev los no ntawm sesamolin hais txog qhov loj, kev txheeb xyuas, thiab kev ua kom huv huv, cov khoom siv lub cev, thiab kev ua haujlwm tshuaj ntawm sesamolin nrog nws cov txheej txheem ntawm kev ua. Tsis tas li ntawd, kev txwv tsis pub muaj feem cuam tshuam txog cov khoom siv physicochemical ntawm sesamolin thiab cov kev tshawb fawb yav tom ntej hauv Fifield cuam tshuam kuj tau tshuaj xyuas.
suab puam cistanche cov txiaj ntsig
2. Tau thiab Sesamolin Cov ntsiab lus hauv Noob Noob
Sesame (Sesamum indicum L.), ntawm tsev neeg Pedaliaceae, yog lub hauv paus loj ntawm sesamolin thiab lwm yam lignan tebchaw nrog rau sesamin, sesamol, sesamol, sesamolinol, thiab glycosylated-lignans. Txawm hais tias lwm cov sesame lignans xws li sesamin tau tshaj tawm tias raug cais tawm ntawm lwm hom nroj tsuag xws li Piper sp., Virola sp., Magnolia sp., thiab Camellia sp., tsis ntev los no qhia tau hais tias tsis muaj ntawv ceeb toom ntawm sesamolin tau cais los ntawm lwm cov tsev neeg cog qoob loo. Sesamum. Txawm li cas los xij, lwm hom Sesamum xws li S. angustifolium, S. alatum, S. radiatum, S. angolense Welw., S. calcium Welw., thiab S. orientale var. malabaricum Nar. tau tshaj tawm tias kuj muaj sesamolin hauv me me [1,7,13]. Ntau qhov kev tshawb fawb tau tshaj tawm tias cov ntsiab lus sesamolin hauv cov noob hnav feem ntau muaj nyob ntawm 0.2–4.3 mg / g qhuav noob raws li qhia hauv Table 1.
Feem ntau, sesamolin cov ntsiab lus qis dua sesamin, thaum sesamol yog qhov tsawg tshaj plaws ntawm peb lignins. Txawm li cas los xij, cov ntsiab lus ntawm lignan nyob rau hauv cov noob qoob loo sib txawv yuav txawv. Ntau yam xws li ntau yam, xim ntawm cov noob, thaj chaw, thiab kev loj hlob ntawm kev cog qoob loo tuaj yeem cuam tshuam cov phytoconstituents hauv cov noob hnav. Kauslim dub sesame cultivars muaj cov ntsiab lus sesamolin ntau dua sesamin, tab sis qhov nruab nrab lignan ntsiab lus ntawm Kauslim dawb sesame yog siab dua. Txoj kev tshawb no tseem pom tau tias cov ntsiab lus lignan sib txawv heev ntawm ob lub xyoo qoob loo (2009 thiab 2010), qhia tias ib puag ncig kev ntxhov siab thiab agronomic tej yam kev mob cuam tshuam rau cov ntsiab lus lignan [14]. Nyob rau hauv sib piv rau cov kev tshawb pom, Indian dub sesame cultivars muaj siab tshaj plaws tag nrho cov ntsiab lus lignan, thiab sesame cultivars dawb muaj cov ntsiab lus siab sesamol. Ib siab tag nrho cov ntsiab lus lignan hauv cov noob hnav dub kuj tau tshaj tawm los ntawm Shi li al. nyob rau hauv sesame noob cultivated nyob rau hauv Tuam Tshoj [15,16]. Kev tshawb fawb hauv thaj av thiab kev yug me nyuam ntawm cov noob hnav los ntawm Thaib teb tau pom ntau yam ntawm cov ntsiab lus sesamolin, ntawm 0-2.25 mg / g. Landrace sesame noob, Maehongsong, muaj qib ntawm sesamolin ntau dua sesamin.
Txawm li cas los xij, cov kab yug tsiaj A7250-8 thiab A7251-7 (BR) tsis muaj sesamolin [17]. Sesamolin cov ntsiab lus hauv cov roj noob hnav tuaj yeem cuam tshuam los ntawm cov txheej txheem roj. Roj ua technologies feem ntau muaj ob txoj kev sib txawv. Thawj yog thaum cov noob tau ci, thiab qhov thib ob yog thaum cov roj crude yog refined. Yog li, muaj qee yam khoom siv roj ntau yam raws li cov roj ua haujlwm, (1) cov roj kub kub nias (HPSO), thiab cov roj noob hnav me me (SMSO) siv cov noob roasted, (2) cov roj txias txias (CPSO) siv cov noob uas tsis yog ci, thiab (3) cov roj txiv roj ua kom zoo (RSO) siv cov noob roasted lossis tsis-roasted tom qab los ntawm kev ua kom zoo. Roasted sesame noob roj (HPSO thiab SMSO) muaj qib sesamolin qis dua li ntawm CPSO (unroasted noob). Cov txheej txheem roasting ntawm cov noob hnav tuaj yeem ua rau oxidation ntawm sesamolin hloov mus rau hauv sesamol, ua rau cov ntsiab lus sesamolin tsawg. Lub caij no, sesamolin tuaj yeem tawg mus rau hauv sesamol thaum lub sij hawm bleaching. Yog li, sesamolin qis kuj tau pom hauv RSO [15,18].
cistanche kho mob raum
3. Sesamolin cais, txiav txim siab, thiab purification txoj kev
Sesamolin thiab lwm cov tshuaj hauv cov noob hnav tuaj yeem txheeb xyuas qhov zoo thiab muaj nuj nqis siv ntau yam kev sib cais ua raws li cov txheej txheem spectroscopy rau kev tshuaj xyuas. Ua ntej txheeb xyuas cov tebchaw hauv cov noob hnav lossis cov qauv roj, kev npaj ua ntej txhawm rau tshem tawm cov kev cuam tshuam kev sib txuas thiab mloog zoo rau cov lignans. Ntau txoj kev rho tawm xws li cov khoom siv-theem extraction thiab kua-kua extraction tau zoo-paub txoj hauv kev rau lub hom phiaj no. Cov txheej txheem rho tawm siv cov khoom sorbents graphene oxide thiab hydroxylated ferrous ferric oxide (Fe3O4) tau ua tiav rau kev npaj cov roj noob hnav ua ntej kev txiav txim siab sesamolin, sesamin, thiab sesamol siv cov kua chromatography (HPLC) ua haujlwm siab 85-93 feem pua rov qab [20 ]. Ultrasonic-pab kua-kua micro-extraction siv sib sib zog nqus eutectic hnyav (DES) muaj li ntawm choline chloride thiab p-cresol nrog kev pab los ntawm sonication rau noob hnav roj extraction muab siab extraction efficiency rau polar thiab nonpolar lignans [21].
Ntawm kev sib cais thiab kev txheeb xyuas siv cov txheej txheem chromatography, HPLC siv ultraviolet (UV / VIS) detector, photodiode array (PDA) detector, los yog fluorescent detector yog txoj kev siv dav tshaj plaws rau kev sib cais thiab kom muaj nuj nqis ntawm cov tebchaw vim nws qhov rhiab heev [7,15, 17, 22, 23] ib. Tsis tas li ntawd, nyias txheej chromatography (TLC), roj chromatography (GC) ua ke nrog ib pawg spectrometer (MS) muab kev sib cais zoo thiab kev txiav txim siab txhim khu kev qha. Xwb, kev siv cov txheej txheem nyias nyias chromatography (HPTLC) muaj qhov kev txiav txim siab sai thiab raug nqi ntawm lignan tebchaw hauv cov noob hnav piv rau HPLC, uas yog suav tias yog txoj kev siv sijhawm. Tsis ntev los no, HPTLC txoj kev siv cov kuab tshuaj tsis zoo ua rau pom kev sib piv nrog HPLC-DAD [19,24]. Tsis ntev los no, Ze-infrared spectroscopy (NIRS) analytical txheej txheem ua ke nrog cov chemometric tsom xam tau muab kev txiav txim siab tsis muaj kev puas tsuaj, nrawm, thiab eco-friendly compound. NIRS tau ua tiav qhov kev kwv yees ntawm cov sesamolin thiab sesamin hauv cov noob hnav ze ze rau cov txiaj ntsig ntawm HPLC cov txheej txheem [25,26].
Sesamolin can be purified from sesame seeds or oil extracts by various chromatography methods such as silica gel column, counter-current chromatography, preparative HPLC, and centrifugal partition chromatography. The other methods are crystallization and resin absorption. The silica gel column, followed by semi-preparative HPLC, success-Molecules 2021, 26, 5849 4 of 16 fully separated sesamolin and sesamin from sesame oils with high purity (>97 feem pua ), tab sis tsis tshua muaj txiaj ntsig [23,27]. Reshma thiab cov neeg ua haujlwm sib koom ua ke siv crystallization los cais cov noob hnav roj lignan ua tiav qhov ntau (54 feem pua yield) thiab 94.4 feem pua purity ntawm sesamolin [28].
Separation and purification of sesamolin and sesamin from sesame seeds using the Countercurrent chromatography (CCC) method by employing petroleum ether (60−90 ◦C), ethyl acetate, methanol, and water 1:0.4:1:0.5 (v/v) as solvents system successfully obtained sesamolin with 64% recovery and 98% purity [29]. Hamman also found the separation of sesamolin and sesamin from sesame oil qualitatively when using CCC following with GC/MS method to separate many vegetable oils minor lipids components [30]. Most problems in compound isolation from plant oils samples were the removal of the triacylglycerol, which was>90 feem pua hauv cov roj ua ntej cov txheej txheem sib cais los txhawb cov hom phiaj sib txuas. Txhawm rau ua tiav lub hom phiaj no Gournet thiab cov neeg ua haujlwm sib koom ua ke siv resin nqus XAD-4 raws li cov kauj ruam ua ntej kom tau txais qhov sib tov yuav luag tsis pub muaj suab thaj thiab polar lipids tom qab ntawd siv Fast Centrifugal Partition Chromatography (FCPC) los cais cov lignan Cheebtsam hauv cov noob noob hnav. cov extract [2].
Los ntawm kev siv Centrifugal Partition Chromatography (CPC), sesamolin nrog 93 feem pua purity tau ntse cais los ntawm cov noob hnav noob extracts thiab txoj kev no tuaj yeem siv nrog ntau tus qauv, uas tsis tau tshaj tawm yav dhau los [31]. Hauv tsab ntawv ceeb toom tsis ntev los no, Michailidish et al. kuj tau ntse cais cov sesamin thiab sesamolin nyob rau hauv sesame roj nrog siab yield thiab siab purity siv centrifugal partition extraction (CPE), tom qab los ntawm centrifugal partition chromatography (CPC) siv biphasic solvents system n-hexane / ethyl acetate / ethanol / dej nyob rau hauv qhov kev faib ua feem ntawm 2:3:3:2 (v/v/v/v) [32].
neuroprotective teebmeem ntawm cistanche echinacoside
4. Physicochemical Properties ntawm Sesamolin
Sesamolin muaj cov mis mos molecular C20 H 18O7, thiab nws cov qauv tshuaj muaj nyob rau hauv daim duab 1. Sesamolin yog nyob rau hauv ib pawg ntawm lignan tebchaw tsim los ntawm kev sib koom ua ke ntawm ob phenylpropanoids txuas nrog lub hauv paus carbon ntawm lawv propyl sab. Lub xub ntiag ntawm methylene dioxyphenoxy moieties los yog nws cov metabolite los ntawm - phenolic hydroxyl pawg - tej zaum yuav yog lub luag hauj lwm rau ntau yam lom lom ua si ntawm sesamolin [8]. Txawm li cas los xij, tsis muaj kev tshawb fawb qhia txog cov qauv-kev sib raug zoo ntawm sesamolin txog cov pab pawg ua haujlwm twg yog cov tshuaj pharmacophores rau nws cov haujlwm lom neeg.
Cov khoom physicochemical ntawm sesamolin tau sau tseg nyob rau hauv Table 2. Cov khoom tseem ceeb physicochemical uas cuam tshuam rau pharmacokinetic thiab pharmacodynamic cwj pwm ntawm cov tebchaw yog solubility, lipophilicity, hydrogen bond donors (HBD's), hydrogen bond acceptors (HBAs), thiab topological polar deg cheeb tsam ( TPSA), Sesamolin muaj dej-solubility tsawg dua 0.1 mg/mL uas yog suav hais tias yog insoluble hauv dej. Aqueous solubility yog ib qho cuab yeej tseem ceeb rau bioactive compounds vim tias nws tuaj yeem cuam tshuam kev ua haujlwm hauv vitro thiab hauv vivo kev soj ntsuam, txawm tias nyob rau theem kho mob. Nyob rau theem kev sim hauv vitro, feem ntau ntawm cov kev sim hauv vitro siv qhov nruab nrab aqueous, tshwj xeeb tshaj yog thaum siv cov qauv ntawm tes. Cov tshuaj ntsuam xyuas yuav tsum tau yaj tag nrho hauv qhov nruab nrab ntawm qhov kho kom haum kom ntsuas nws cov tshuaj pharmacological. Tsis tas li ntawd, hauv daim duab 1. Sesamolin molecular qauv. Cov khoom physicochemical ntawm sesamolin tau sau tseg nyob rau hauv Table 2. Cov khoom tseem ceeb physicochemical uas cuam tshuam rau pharmacokinetic thiab pharmacodynamic cwj pwm ntawm cov tebchaw yog solubility, lipophilicity, hydrogen bond donors (HBD's), hydrogen bond acceptors (HBAs), thiab topological polar deg cheeb tsam ( TPSA), Sesamolin muaj dej-solubility tsawg dua 0.1 mg/mL uas yog suav hais tias yuav insoluble hauv dej. Aqueous solubility yog ib qho cuab yeej tseem ceeb rau bioactive compounds vim tias nws tuaj yeem cuam tshuam kev ua haujlwm hauv vitro thiab hauv vivo kev soj ntsuam, txawm tias nyob rau theem kho mob. Nyob rau theem kev sim hauv vitro, feem ntau ntawm cov kev sim hauv vitro siv qhov nruab nrab aqueous, tshwj xeeb tshaj yog thaum siv cov qauv ntawm tes. Cov tshuaj ntsuam xyuas yuav tsum tau yaj tag nrho hauv qhov nruab nrab ntawm qhov kho kom haum kom ntsuas nws cov tshuaj pharmacological. Tsis tas li ntawd, nyob rau hauv vivo assay, lub compound yuav tsum tau khaws cia nyob rau hauv ib tug tshwj xeeb concentration nyob rau hauv lub aqueous mob nyob rau hauv thiaj li yuav muab zoo faib ntawm cov hlab ntsha thiab muab siab bioavailability los muab cov pharmacological nyhuv ntawm lub hom phiaj [33]
Lub hav zoov ntawm hydrogen bond donors (HBD's) thiab hydrogen bond acceptors (HBAs) hauv cov qauv sib xyaw ua rau nws cov dej solubility, membrane absorption, thiab ligand-receptor kev sib cuam tshuam [34]. Sesamolin muaj tsawg dua 5 HBD thiab 2 txog 16 HBA uas yog tus naj npawb zoo tshaj plaws rau kev nqus cov membrane thiab muab kev sib cuam tshuam txaus los ntawm hydrogen daim ntawv cog lus raws li Lipinski txoj cai ntawm tsib. Qib ntawm lipophilicity ntawm cov compound yog qhia raws li qhov sib faib coefficient (log P) thiab nws cov khoom tseem ceeb uas txhais tau tias qhov nqus ntawm phospholipid bilayer. Sesamolin muaj log P tus nqi 3. A degree ntawm lipophilicity tus nqi tsawg tshaj li 5 yog tsim nyog rau lub compound kom muaj txaus txaus nqus mus rau hauv daim nyias nyias cell. Qhov chaw polar nto (PSA) ntawm bioactive compound yuav tsum tau khi nrog feem ntau ntawm cov hom phiaj receptors. Qhov chaw polar nto (PSA) ntawm bioactive compound txiav txim siab nws nqus. PSA siab yuav nce solubility hauv dej, tab sis tus nqi PSA ntau dua 140 Å yuav txo cov tshuaj muaj peev xwm permeate hlwb. PSA ntawm sesamolin yog 64.6 Å, yog li nws raug suav hais tias muaj qhov zoo permeability [35–37].
cistanche echinacoside:anti-apoptosis
5. Pharmacological Activities
5.1. Antioxidant Kev Ua Haujlwm
Noob noob taum paub zoo tias muaj kev ua haujlwm siab antioxidant. Hloov chaw ntawm tus kheej cov nyhuv ntawm lignan tebchaw, cov nyhuv synergistic ntawm tocopherol thiab lignans cov ntsiab lus hauv cov noob hnav ua rau cov tshuaj antioxidant ntawm cov noob hnav [8]. Sesamolin pom muaj kev ua haujlwm antioxidant tsawg hauv ntau yam hauv vitro kev sim. Sesamolin tau pom tias muaj kev ua kom muaj zog antioxidant tsawg dua li sesamol raws li kev tshem tawm muaj peev xwm tiv thaiv DPPH radical thiab superoxide-dawb radical [38,39], ferrous txo lub peev xwm (FRAP), oxygen radical absorbance peev (ORAC), -carotene-bleaching assay, thiab inhibition ntawm linoleic acid peroxidation [40]. Txawm li cas los xij, tom kawg ob qhov teebmeem antioxidant tau siab dua sesamin [40].
Kev ua haujlwm antioxidant tsawg ntawm sesamolin hauv vitro tuaj yeem yog vim tsis muaj phenolic hydroxyl pab pawg, cov khoom siv hluav taws xob zoo rau cov dawb radicals. Lub tshuab ua haujlwm ntawm cov kev ua haujlwm ntawm hydrogen atoms (DTFT) . Yog li ntawd, sesamolin tau kwv yees kom muaj lub peev xwm tsis muaj zog antioxidant dua li sesamin, uas tuaj yeem pub ob allylic hydrogens, thiab sesamol, uas muaj phenolic hydroxyl pawg [41]. Txawm hais tias muaj kev ua haujlwm tsis muaj zog antioxidant hauv lub cev hauv vitro, ntau qhov kev tshawb fawb tau tshaj tawm txog kev ua haujlwm antioxidant ntawm sesamolin hauv vivo. Sesamolin tsis inhibit lipid peroxidation kev ua haujlwm ntawm nas lub siab microsomes induced los ntawm ADP-Fe2 ntxiv / NADPH hauv vitro. Sesamolin tau pom tias inhibit lipid peroxidation ntawm nas daim siab thiab lub raum tom qab pub mis nrog ib qho extract uas muaj 1 feem pua sesamolin. Qhov kev ua no tau npaj los ntawm kev hloov pauv metabolic ntawm sesamolin rau hauv ob lub cev metabolites, sesamolinol thiab sesamol [42]. Kev ua haujlwm antioxidant ntawm sesamolin hauv vivo tau txais kev txhawb nqa los ntawm lwm txoj kev tshawb fawb. Sesamolin muaj cov nyhuv inhibitory los ntawm tib lub microsomal system nyob rau hauv lub cev siv nas lub siab microsomes thiab cumene hydroperoxide (CumOOH) / Fe2 plus -ADP-NADPH, tab sis tsis nyob rau hauv lub non-enzymatic system uas muaj nas daim siab mitochondria thiab Fe2 ntxiv -ascorbate [43] ]. Txoj kev tshawb no kuj tau qhia txog kev sib koom ua ke ntawm ib tus neeg lignans suav nrog sesamolin, sesamin, thiab sesamol nrog -tocopherol lossis tocotrienol tsim cov nyhuv inhibitory ntau dua hauv ob qho tib si lipid peroxidation systems [43].
5.2. Antimicrobial Activity
Sesamolin muaj cov tshuaj tua kab mob tiv thaiv kab mob Bacillus cereus, Staphylococcus aureus, thiab Pseudomonas aeruginosa nrog 61, 62, thiab 53 feem pua kev loj hlob inhibition ntawm 2 mg / mL [40].
5.3. Kev Ua Haujlwm Neuroprotective
Pathphysiology ntawm cov kab mob neurodegenerative feem ntau cuam tshuam nrog kev hloov pauv biochemical ntawm biomolecules Cheebtsam hauv cov hlwb neuronal induced los ntawm oxidative kev nyuaj siab. Nws tau qhia los ntawm ntau lub cim ntawm cov pa oxygen reactive (ROS) xws li hydrogen peroxide, superoxide, thiab hydroxyl dawb radicals vim qhov tsis sib xws ntawm ROS thiab antioxidants ua rau biomolecules puas tsuaj [44]. Qhov tseeb yog, lub hlwb, uas yog ib qho tseem ceeb ntawm lub hauv nruab nrab lub paj hlwb (CNS) yog heev yooj yim rau oxidative kev nyuaj siab [45]. Kev txo qis ntawm ROS tuaj yeem yog lub hom phiaj rau kev tiv thaiv kab mob neurodegenerative thiab kho. Txij li thaum ROS tuaj yeem raug khawb thiab txo qis los ntawm cov tshuaj tua kab mob antioxidant, cov tebchaw uas muaj cov tshuaj tiv thaiv antioxidant tuaj yeem yog cov neeg sawv cev zoo rau kev tiv thaiv thiab kho cov kab mob neurodegenerative.
Ntau qhov kev tshawb fawb tau soj ntsuam cov txiaj ntsig ntawm sesamolin ntawm kev tiv thaiv kev ua haujlwm hauv cov hlwb neuronal. Sesamolin ua tau zoo tiv thaiv murine BV-2 microglial hlwb los ntawm hypoxia-induced cell tuag thiab hydrogen peroxide-induced cell raug mob [46,47]. Hypoxia rau 1 h induced 35 feem pua ntawm tes tuag nyob rau hauv pab pawg neeg tsis kho. Sesamolin 50 µM tau ua tiav cov txiaj ntsig ntawm tes mus rau 96 feem pua, tom qab ntawd txo qis LDH tso tawm los ntawm 24 feem pua. Ntxiv mus, sesamolin scavenged 25 feem pua ntawm hypoxia-induced ROS hauv hlwb. Hypoxia-induced ROS tuaj yeem qhib cov teeb liab hloov txoj hauv kev rau kev tuag ntawm tes, suav nrog cov xov tooj hluav taws xob hluav taws xob tswj hwm cov protein kinases (ERK1/2), c-Jun NH2-terminal kinase (JNK), thiab p38 Mitogen-activated protein kinases (MAPK ). Txoj kev tshawb no tau lees paub tias MAPK cascades tau inhibited los ntawm sesamolin los ntawm kev tiv thaiv phosphorylation ntawm JNK, p38 MAPKs, thiab caspase{21}} qhia hauv BV-2 hlwb ntawm 10 min hypoxia. Siv cov hlwb sib txawv, txoj kev tshawb fawb hauv kev tiv thaiv cov nyhuv ntawm sesamolin kuj tau tshaj tawm los ntawm Hou hauv nas pheochromocytoma (PC12), thiab nas thawj cortical hlwb [48]. Lawv pom tias sesamolin txo qis LDH tso tawm hauv qab hypoxia, uas cuam tshuam nrog inhibition ntawm MAPKs thiab caspase-3. Tsis tas li ntawd, hypoxia-induced apoptotic-zoo li cell tuag, raws li kuaj pom los ntawm fluorescent DNA-binding dye nyob rau hauv kab lis kev cai cortical hlwb, tau txo qis heev tom qab kev kho mob nrog 50 µM sesamolin.
Raws li ROS, kev ua kom lub hlwb microglial yuav tso tawm nitric oxide (NO), uas overproduction tuaj yeem ua rau muaj mob rau cov neurons. Kev hloov pauv ntawm inducible-NO synthase (iNOS) genes hauv microglia tswj NO tiam hauv microglial los ntawm kev txhawb nqa ntawm lipopolysaccharide (LPS) uas ua kom muaj kev sib koom ua ke ntawm intracellular signaling txoj hauv kev nrog tyrosine kinases, MAPK thiab NF-kB kho cov noob qhia. Qhov kev txhawb nqa no ua rau kev tso tawm ntawm cov qog necrosis (TNF- ) thiab txhawb kev tuag neuron. Cov kev tshawb fawb hauv vitro uas siv sesamolin los inhibit NO-induced los ntawm LPS tau lees paub tias sesamolin txo qis cov cim LPS-induced NO nyob rau hauv murine microglial cell kab BV-2 thiab nas thawj microglial hlwb los ntawm kev txo qis LPS-induced. p38 PAB [49]. Cov teebmeem neuroprotective ntawm sesamolin tau ua hauv vivo siv gerbils. Ua ntej focal cerebral ischemia induction, cov gerbils tau hais lus nrog purified sesamin los yog cov roj noob hnav roj uas muaj 90 feem pua sesamin thiab 10 feem pua sesamolin 20 mg / kg / hnub rau 4 hnub.
Sesamin thiab sesame extract uas muaj sesamolin txo qis infarct ntau thiab tsawg ntawm gerbil hlwb nyob rau hauv cerebral ischemia los ntawm 56 feem pua thiab 49 feem pua, raws li (p < 0.05).="" txawm="" li="" cas="" los="" xij,="" cov="" txheej="" txheem="" ntawm="" vivo="" neuroprotection="" tsis="" tau="" nkag="" siab="" [50].="" cov="" kab="" mob="" neurodegenerative,="" tshwj="" xeeb="" tshaj="" yog="" alzheimer's="" disease="" (ad)="" qhia="" txog="" kev="" sib="" sau="" ntawm="" cov="" proteins="" xws="" li="" extracellular="" amyloid="" plaques="" (a)="" thiab="" neurofibrillary="" tangles="" (nft)="" hauv="" lub="" hlwb.="" sesamolin="" cov="" kev="" tiv="" thaiv="" tiv="" thaiv="" toxicity="" ntawm="" a="" tau="" raug="" soj="" ntsuam="" siv="" cov="" kab="" mob="" cab="" (caenorhabditis="" elegans)="" cov="" qauv,="" uas="" qhia="" txog="" tib="" neeg="" a="" ntu="" hauv="" lub="" cev="" phab="" ntsa="" cov="" leeg="" thiab="" tau="" ua="" rau="" tus="" tuag="" tes="" tuag="" taw.="" tsis="" tas="" li="" ntawd,="" qhov="" tso="" nyiaj="" ntawm="" a="" hauv="" cov="" neurons="" ua="" rau="" txo="" qis="" ntawm="" tus="" cwj="" pwm="" chemotaxis.="" sesamolin="" ntawm="" ib="" qho="" concentration="" ntawm="" 100="" μg="" ml="" qhia="" tau="" tias="" muaj="" kev="" cuam="" tshuam="" loj="" ntawm="" kev="" tuag="" tes="" tuag="" taw="" los="" ntawm="" 1.83="" h="" hauv="" cov="" kab="" mob="" transgenic.="" tus="" nqi="" no="" siab="" dua="" li="" ntawm="" ginkgo="" biloba="" nplooj="" extract.="" ntxiv="" mus,="" kev="" tshawb="" fawb="" txog="" kev="" tiv="" thaiv="" ntawm="" sesamolin="" tiv="" thaiv="" a="" toxicity="" nyob="" rau="" hauv="" cov="" hlwb="" neuronal="" siv="" c.="" elegans="" cl2355="" uas="" qhia="" neuronal="" a="" tau="" pom="" tias="" tus="" cwj="" pwm="" chemotaxis="" tau="" zoo="" dua="" piv="" rau="" cov="" pab="" pawg="" tsis="" kho="">
5.4. Antimelanogenesis
Melanogenesis yog txheej txheem ntawm melanin ntau lawm tshwm sim nyob rau hauv tib neeg daim tawv nqaij raws li photoprotection los ntawm UV raug, tab sis kuj ua rau pigmentation nyob rau hauv daim tawv nqaij, raws li melanin yog xim av tsaus. Yog li ntawd, nws yuav txo qhov kev zoo nkauj ntawm daim tawv nqaij. Melanogenesis muaj kev cuam tshuam ntawm keratinocytes thiab melanocytes. Cov txheej txheem pib thaum keratinocytes raug UV los ntawm lub hnub ci thiab txuas ntxiv ua rau cov noob pro-opiomelanin, ua rau lub cim ntawm -melanocyte-stimulating hormone (-MSH). -MSH ces khi nrog melanocortin -1 receptor (MC1R) ntawm melanocytes. Qhov kev koom tes no ua rau txoj kev taw qhia ntawm cyclic adenosine monophosphate (CAMP) thiab ua rau kev ua kom muaj protein ntau Kinase-A (PKA). Cov kev taw qhia txuas ntxiv nrog kev tswj hwm ntawm cAMP cov lus teb cov ntsiab lus-binding (CREB) cov ntsiab lus hloov pauv protein, tom qab ntawd txhawb nqa microphthalmia-sociated transcription factor (MITF), uas ua rau muaj kev hloov pauv ntawm cov protein tyrosinase, TRP-1, thiab TRP{{ 11}}, uas koom nrog hauv melanin synthesis. Biochemical synthesis ntawm melanin tshwm sim hauv melanosomes pib los ntawm hydroxylation ntawm tyrosine mus rau 3, 4-dihydroxyphenylalanine (L-DOPA), tom qab ntawd oxidation rau o-dopaquinone, ces dopachrome yog catalyzed los ntawm tyrosinase. Thaum kawg, eumelanin tsim (xim av tsaus) tshwm sim los ntawm enzymatic transformation ntawm dopachrome los ntawm TRP{16}} thiab TRP{17}} [52,53].
Kev tiv thaiv UV tiv thaiv kev ua haujlwm ntawm melanogenesis thiab tshuaj pleev thaiv hnub ua haujlwm ntawm sesamolin tau raug soj ntsuam nyob rau hauv kev sib piv rau cov neeg ua haujlwm zoo tsim depigmenting, kojic acid, thiab -arbutin. Txoj kev tshawb no tau lees paub tias sesamolin muaj cov tshuaj pleev thaiv hnub ua haujlwm los ntawm feem ntau nqus UVB thiab nthuav tawm 4-fold absorbance siab dua kojic acid thiab -arbutin. Txawm hais tias sesamolin pom tias tsis tshua muaj inhibition hauv nceb tyrosinase, ib qho tseem ceeb enzyme hauv melanogenesis, nws pom tias muaj inhibition siab txog li 50 feem pua ntawm cov cellular tyrosinase ntawm ib tug concentration ntawm 50 µg / mL piv nrog kojic acid thiab -arbutin yam tsis muaj toxicity nyob rau hauv noncancerous Vero thiab melanoma. SK-MEL2 kab ntawm tes. Sesamolin ntawm 25 µg / mL txo cov ntsiab lus melanin hauv SK-MEL2 hlwb. Western blot assay tau pom tias sesamolin txo qis kev qhia ntawm tyrosinase, TRP-1, thiab TRP-2 hauv SK-MEL2 cell kab. Txoj kev tshawb no qhia tias sesamolin tuaj yeem inhibit melanin synthesis ntawm ob theem; (1) tiv thaiv los ntawm UV hluav taws xob, lub melanin inducer, los ntawm cov tshuaj pleev thaiv hnub muaj nuj nqi, thiab (2) downregulated lub melanogenic protein tyrosinase, TRP{19}}, thiab TRP-2 [54].
Cov kev ua los tiv thaiv tyrosinase ntawm sesamolin kuj tau tshaj tawm los ntawm Michaildish raws li inhibition ntawm nceb tyrosinase kev ua hauv vitro. Cov txiaj ntsig tau pom tias sesamolin tau ua haujlwm nruab nrab los tiv thaiv tyrosinase ntawm 500 µM thiab tsis muaj zog ntawm 100 thiab 25 µM [32]. Sesamolin kuj pom tias muaj kev tiv thaiv melanogenesis hauv cov qog nqaij hlav cancer ntawm daim tawv nqaij (B16F10). Txoj kev tshawb no pom tau hais tias sesamolin inhibited qhov kev qhia ntawm melanogenesis-txog mRNA theem, nrog rau cov proteins xws li tyrosinase thiab TRP-1 thiab TRP-2 ntawm qhov concentration ntawm 50 µM [55]. Daim duab 3 qhia cov ntsiab lus ntawm cov txheej txheem ntawm sesamolin inhibition ntawm melanin ntau lawm. Molecules 2021, 26, x FOR PEER REVIEW 8 of 16 UV tiv thaiv cov nyhuv thiab kev tiv thaiv melanogenesis thiab cov tshuaj pleev thaiv hnub ua haujlwm ntawm sesamolin tau raug tshuaj xyuas piv rau cov tshuaj depigmenting uas tsim tau zoo, kojic acid, thiab -arbutin. Txoj kev tshawb no tau lees paub tias sesamolin muaj cov tshuaj pleev thaiv hnub ua haujlwm los ntawm kev nqus UVB feem ntau thiab nthuav tawm 4-fold absorbance siab dua kojic acid thiab -arbutin. Txawm hais tias sesamolin pom tias tsis tshua muaj inhibition hauv nceb tyrosinase, ib qho tseem ceeb enzyme hauv melanogenesis, nws pom tias muaj inhibition siab txog li 50 feem pua ntawm cov cellular tyrosinase ntawm ib tug concentration ntawm 50 µg / mL piv nrog kojic acid thiab -arbutin yam tsis muaj toxicity nyob rau hauv noncancerous Vero thiab melanoma. SK-MEL2 kab ntawm tes. Sesamolin ntawm 25 µg / mL txo cov ntsiab lus melanin hauv SK-MEL2 hlwb.
Western blot assay tau pom tias sesamolin tau txo qis kev qhia ntawm tyrosinase, TRP-1, thiab TRP-2 hauv SK-MEL2 cell kab. Txoj kev tshawb no qhia tias sesamolin tuaj yeem inhibit melanin synthesis ntawm ob theem; (1) tiv thaiv los ntawm UV hluav taws xob, lub melanin inducer, los ntawm cov tshuaj pleev thaiv hnub muaj nuj nqi, thiab (2) txo qis melanogenic protein tyrosinase, TRP-1, thiab TRP-2 [54]. Cov kev ua los tiv thaiv tyrosinase ntawm sesamolin kuj tau tshaj tawm los ntawm Michaildish raws li inhibition ntawm nceb tyrosinase kev ua hauv vitro. Cov txiaj ntsig tau pom tias sesamolin tau ua haujlwm nruab nrab los tiv thaiv tyrosinase ntawm 500 µΜ thiab tsis muaj zog ntawm 100 thiab 25 µΜ [32]. Sesamolin kuj pom tias muaj kev tiv thaiv melanogenesis hauv cov qog nqaij hlav cancer ntawm daim tawv nqaij (B16F10). Txoj kev tshawb no tau ua pov thawj tias sesamolin inhibited qhov kev qhia ntawm melanogenesis ntsig txog mRNA qib, nrog rau cov proteins xws li tyrosinase thiab TRP{18}} thiab TRP-2 ntawm qhov concentration ntawm 50 µΜ [55]. Daim duab 3 qhia cov ntsiab lus ntawm cov txheej txheem ntawm sesamolin inhibition ntawm melanin ntau lawm.
5.5. Anticancer Activity
Sesamolin pom kev loj hlob inhibition thiab apoptosis induction nyob rau hauv tib neeg lymphoid leukemia (Molt 4B) hlwb. Antiproliferation yog ib qho concentration-dependent yam nrog IC90 ntawm 90 µM. Sesamolin-induced apoptosis yog qhia los ntawm kev hloov pauv ntawm morphological, DNA fragmentation, thiab tsim ntawm apoptotic lub cev tom qab 3 hnub ntawm kev kho mob nrog 90 µM sesamolin. Thaum piv nrog lwm cov tshuaj nyob rau hauv cov roj noob hnav, episesamin, thiab sesamol los ntawm lwm cov kev tshawb fawb, kev loj hlob inhibition ntawm sesamolin tau zoo dua. Txawm li cas los xij, txoj kev tshawb no tsis tau nthuav tawm cov ncauj lus ntxaws ntxaws ntawm apoptosis induction txoj hauv kev lossis DNA fragmentation [56].
Cov txiaj ntsig ntawm sesamolin ntawm kev ua haujlwm inhibition proliferative kuj tau soj ntsuam tawm tsam tib neeg txoj hnyuv HCT116. Antiproliferation raws li kev soj ntsuam MTT tau pom tias sesamolin cuam tshuam qhov kev loj hlob ntawm lub sijhawm thiab cuam tshuam kev muaj peev xwm tsiv teb tsaws. Kev loj hlob, kev sib txawv, thiab apoptosis ntawm cov qog nqaij hlav qog noj ntshav tau tswj hwm los ntawm Janus kinase 2 (JAK2) teeb liab hloov pauv thiab activator transcription- 3 (STAT3) qhia txoj hauv kev. Sesamolin 20 µM txo qis qhov qhia ntawm p-JAK2 / STAT3 qhia los ntawm kev txo qis ntawm p-JAK2 / STAT3 band ntawm sab hnub poob blot. Sesamolin thiab AG490 (ib qho kev tswj zoo) tau pom muaj kev sib koom ua ke. Lawv qhov sib xyaw ua ke tau txo qis kev qhia ntawm p-STAT3. Cancer cell migration yog ib qho kev npaj rau metastasis, thiab nws cuam tshuam nrog kev tswj hwm ntawm MMP 1, 2, thiab 9.
Txoj kev tshawb no tau pom tias sesamolin txo qis MMP cov lus qhia hauv HCT116 thaum tshawb xyuas los ntawm qRT-PCR. Sesamolin yog ib qho muaj peev xwm tiv thaiv kab mob rau cov kab mob qog noj ntshav los ntawm inhibiting kev ua haujlwm ntawm JAK2 / STAT3 txoj hauv kev thiab tiv thaiv cell invasion ntawm inhibition ntawm IL-6-induced qhia ntawm MMPs [57]. Lwm txoj kev tshawb nrhiav sesamolin rau nws cov tshuaj tiv thaiv kab mob hauv cov ntshav qog noj ntshav Burkitt's lymphoma hlwb, Raji los ntawm kev txhim kho NK cell lysis kev ua haujlwm [58,59]. NK cell yog ib lub cev tiv thaiv kab mob uas muaj peev xwm txheeb xyuas thiab paub qhov txawv ntawm cov qog nqaij hlav thiab cov qog nqaij hlav ntau dua li tua cov qog hlwb. Kev tua neeg (cytolysis) yog tshwm sim los ntawm kev ua kom cov receptors hauv NK hlwb, feem ntau NKG2D, los ntawm NKG2D ligands (NKG2DLs). Lub ULBP-1, ULBP-2, ULBP-3, MIC-A, thiab MIC-B yog NKG2DLs uas nws cov lus tau maj mam nce- tswj los ntawm kev mob qog noj ntshav ntawm lub cell.
Hloov pauv, cov hlwb ib txwm muaj qhov qhia qis ntawm NKG2DLs. Yog li, NKG2D receptors hauv NK hlwb tuaj yeem siv NKG2DLs kom pom tau yooj yim cov qog nqaij hlav qog nqaij hlav hauv cov ntaub so ntswg ib puag ncig. Kev sib txuas ntawm cov activated NKG2D receptor nyob rau hauv NK hlwb nrog NKG2DLs qhia nyob rau hauv cov qog nqaij hlav cancer ua rau ib txoj kev qhia kom tso cytokine thiab induce cytotoxicity los tua cov qog hlwb. Txawm li cas los xij, NKG2DL qib tau txo qis hauv cov qog nqaij hlav lig, yog li, txo qhov kev xav ntawm cov qog nqaij hlav cancer ntawm NK hlwb uas ua rau muaj kev ua haujlwm cytolysis tsawg. Ntxiv mus, qee cov qog nqaij hlav cancer tau tshaj tawm tias muaj kev qhia qis ntawm NKG2DLs, xws li Ramos, Hep3B, thiab Raji [60,61]. Vim li no, txhim kho ib lossis ob qho kev qhia ntawm NKG2D hauv lub cev tiv thaiv kab mob thiab NKG2DLs hauv cov qog nqaij hlav tuaj yeem hloov kho cov tshuaj tiv thaiv kab mob tiv thaiv kab mob thiab tuaj yeem yog qhov kev cog lus rau kev kho mob qog noj ntshav. Kev siv sesamolin thiab sesamin kom nce NKG2DLs kev qhia los txhim kho NK hlwb-mediated cytolytic kev ua haujlwm tau tshaj tawm los ntawm Kim hauv tib neeg Burkitt's lymphoma cell line (Raji), uas tsis tshua muaj siab rau NK hlwb [58].
Pretreatment ntawm Raji hlwb nrog 40 µM sesamolin rau 72 h tau ua tiav qhov kev nkag siab ntawm NK hlwb, ua rau muaj kev nce hauv cytotoxicity piv rau cov pab pawg tsis kho. Ntxiv mus, nws tau lees paub tias qhov nce hauv cytolysis tau ua raws li qhov nce ntawm NKG2DLs qhia ULBP-1, ULBP-2, thiab MICA/B hauv Raji hlwb. Qhov nce ntawm ERK phosphorylation band nyob rau sab hnub poob blot assay thiab tsis muaj zog cytotoxicity ntawm ERK inhibitor thaiv kev soj ntsuam tau ua pov thawj tias kev txhawb nqa ntawm ERK signaling txoj kev los ntawm sesamolin tau koom nrog hauv kev nce ntawm NKG2DLs qhia. Dhau li ntawm lub hom phiaj ntawm NKG2DLs, NK hlwb-kho cytolytic kev ua kom zoo tuaj yeem ua tiav los ntawm kev txhawb nqa NKG2D receptor qhia hauv NK hlwb. Txhawm rau tshawb xyuas qhov cuam tshuam ncaj qha ntawm sesamolin ntawm NK hlwb, ob leeg NK hlwb (NK-92MI) thiab Raji hlwb tau kho nrog sesamolin. Cov kev ua cytolytic tau nce hauv sesamolin-kho NK-92MI hlwb thiab ntawm sesamolin-kho Raji hlwb piv rau cov pab pawg tsis kho. Yog li ntawd, thaum kho Raji thiab NK-92MI hlwb nrog sesamolin, qhov nce cytolytic kev ua haujlwm ntawm NK hlwb kuj tau pom.
Qhov siab tshaj plaws cytotoxicity ntawm sesamolin tawm tsam Raji thiab NK-92MI hlwb yog nyob ntawm 20 µg/mL, thiab 40 µg/mL, feem. Qhov nthuav qhia ntawm daim nyias nyias nyob rau hauv degranulation ntawm NK hlwb thaum lub sij hawm cytolytic kev ua si (CD107a) tau pom nyob rau hauv sesamolin-kho NK-92MI hlwb nyob rau hauv ib tug concentration thiab lub sij hawm incubation nyob ntawm seb. Ntxiv mus, qhov kev tshawb fawb no tau lees paub tias qhov kev qhia ntawm NKG2D hauv NK hlwb tau nce siab tom qab NK-92MI tau kho nrog 40 µg/mL rau 72 teev. Sesamolin ua rau phosphorylation ntawm p38, ERK1/2, thiab JNK txoj hauv kev hauv NK hlwb los txhim kho cov kev ua cytolytic [59]. Cov nyhuv ntawm sesamolin ntawm kev ua cytolytic los ntawm kev tswj hwm cov lus teb tiv thaiv kab mob qog noj ntshav tau tshawb xyuas ntxiv hauv cov hlwb dendritic (DC) [62]. Txoj kev tshawb no qhia tias sesamolin txhawb DCs los txhawb kev tua thiab tsiv teb tsaws ntawm NK hlwb hauv kev sib koom ua ke ntawm DCs thiab NK hlwb. Cov kev ua haujlwm pharmacological ntawm sesamolin thiab nws cov txheej txheem ntawm kev ua haujlwm tau sau tseg hauv Table 3.
Cov txiaj ntsig ntawm cistanche extracts: anti-aging
6. Pharmacokinetics
Kev tshawb nrhiav ntxiv ntawm cov tshuaj pharmacological hauv cov qauv hauv vivo siv cov sesamolin tus kheej tsis tau tshawb pom dav dav. Ntau qhov kev tshawb fawb tau siv cov qauv tsiaj los kawm txog kev ua tshuaj ntawm sesamolin thiab lwm yam lignans hauv cov noob hnav lossis roj. Txawm li cas los xij, lawv tsis tau tshaj tawm cov tshuaj pharmacokinetic profile ntawm sesamolin tom qab kev tswj hwm [43,63–65]. Ob txoj kev tshawb fawb qhia txog bioavailability ntawm sesamolin hauv vivo qauv. Kev tshawb fawb los ntawm Kang tau tshawb xyuas cov txiaj ntsig ntawm sesamolin ntawm lipid peroxidation siv tus qauv nas uas tau noj nrog 1 feem pua sesamolin. Tsawg dua 25 feem pua ntawm cov tshuaj sesamolin tau nqus, metabolized, thiab tawm ncaj qha. Ib theem siab ntawm sesamolin nyob rau hauv daim ntawv ntawm nws conjugated metabolites tau kuaj pom nyob rau hauv cov hnyuv loj. Tsuas yog cov kab mob tau kuaj pom hauv plasma, plab, siab, ob lub raum, thiab cov hnyuv. Sesamolin tsis cuam tshuam rau lub cev qhov hnyav ntawm cov nas, tab sis daim siab hnyav nce tau pom [42]. Lwm txoj kev tshawb fawb los ntawm Ide tau tshaj tawm tias sesamolin hloov cov noob qhia ntawm cov proteins koom nrog hauv hepatic fatty acid oxidation hauv cov nas kom siab dua cov sesamin tab sis mus rau tib qib li episesamin [66]. Qhov concentration ntawm sesamolin hauv cov ntshav nce sai sai tom qab kev tswj hwm qhov ncauj, nce siab ntawm 7 txog 9 h, thiab txo qis tom qab nrog ib nrab neej ntawm 7.1 ± 0.4 h, uas ntev dua sesamin thiab episesamin (4.7 ± {{16). }}.2 thiab 6.1 ± 0.3, ntsig txog). Sesamolin tau ntau heev hauv cov ntshav thiab daim siab piv rau sesamin thiab episesamin. Txawm li cas los xij, daim siab hnyav kuj tau pom tias nce hauv cov nas uas tau noj nrog sesamolin. Tsis muaj ntawv tshaj tawm hais txog kev tshawb fawb soj ntsuam ntawm sesamolin hauv tib neeg lossis kev tshawb fawb pharmacokinetic hauv cov tsiaj. Txawm li cas los xij, muaj kev tshawb fawb soj ntsuam uas siv cov noob hnav noob hnav thiab roj, uas muaj cov sesamolin los tshawb xyuas cov txiaj ntsig ntawm cov noob hnav lignans (sesamin thiab sesamolin) ntawm qib ntawm tib neeg plasma -tocopherol. Nws tau tshaj tawm tias sesamolin thiab sesamin raug ntaus nqi kom nce ntshav plasma -tocopherol thiab inhibition ntawm vitamin E degradation hauv tib neeg yam tsis muaj kev phiv [67,68].
cistanche extract
7. Cov kev cia siab yav tom ntej
Ib yam li lwm cov sesame lignans tebchaw, sesamolin tau tshaj tawm tias muaj ntau yam tshuaj siv tshuaj feem ntau kuaj hauv cov qauv vitro. Cov kev ua haujlwm pharmacological no tau pom ntawm qee cov kab ntawm tes uas muaj qhov ua tau zoo tsawg (<100 µm).="" this="" matter="" could="" give="" rise="" to="" some="" pros="" and="" cons.="" a="" significant="" effect="" at="" low="" concentration="" represents="" a="" strong="" activity,="" especially="" for="" a="" protective="" activity="" that="" does="" not="" aim="" to="" kill="" the="" cells.="" on="" the="" other="" hand,="" the="" difficulties="" to="" increase="" the="" concentration,="" especially="" in="" the="" in="" vitro="" experiments,="" which="" mostly="" use="" an="" aqueous="" medium,="" are="" causing="" limitations="" in="" evaluating="" the="" activity="" or="" level="" of="" toxicity="" of="">
Sesamolin muaj cytotoxicity tsawg tiv thaiv qee cov qog nqaij hlav cancer, xws li SK-MEL-2 thiab HCT-116 [54,69]. Kev soj ntsuam cytotoxicity ntawm sesamolin piv nrog sesamol thiab sesamin tiv thaiv SK-MEL-2 qhia tias peb cov noob hnav no muaj peev xwm los tiv thaiv melanoma cell loj hlob nyob rau hauv ib qho concentration- thiab lub sij hawm-dependent yam. Txawm li cas los xij, sesamolin pom qhov txo qis hauv melanoma cell viability ntawm qhov concentration ntawm 50 µM txog 100 µM. Tsuas yog sesamol tau muab 50 feem pua inhibitory concentration (IC50) tawm tsam melanoma txawm tias yuav tsum tau muaj kev kho mob siab (1893.1 ± 170.7 µM). Nws tau hais nyob rau hauv txoj kev tshawb no tias sesamolin tsis tuaj yeem yaj tau zoo hauv cov kab lis kev cai xov tooj ntawm tes ntawm qhov concentration siab dua 200 µM ua rau qhov kev tshawb xyuas txwv ntawm qhov siab dua [65]. Cov kev tshawb pom no qhia tias txawm tias sesamolin muaj lub zog los tiv thaiv melanoma cell loj hlob, qhov kev txwv cuam tshuam txog kev solubility cuam tshuam cov nyhuv cytotoxic.
Lwm qhov teeb meem solubility tau pom thaum sesamolin tau sim rau nws cov kev ua hauv vitro extracellular antioxidant. Txawm hais tias sesamolin tau pom muaj peev xwm qis qis ntawm DPPH thiab peroxyl dawb radicals, nws tau pom tias muaj kev ua haujlwm siab dua ntawm superoxide radicals ntawm 100 µM. Kev tshawb nrhiav ntawm qhov ntau dua concentration ntau tsis tuaj yeem ua tiav vim nws cov dej solubility tsawg. Dhau li ntawm qhov tshwm sim los ntawm qhov tseeb tias sesamolin cov qauv molecular tsis muaj phenolic hydroxyl pawg, qhov teeb meem solubility kuj yuav ua rau muaj teeb meem los tshawb xyuas qhov tseeb ntawm cov tshuaj antioxidant. Cov teeb meem solubility kuj yog ib qho ntawm cov laj thawj uas tsis tau tshaj tawm txog IC50 ntawm sesamolin thaum ntsuas rau nws cov cytotoxicity hauv vitro. Kev tshawb nrhiav ntxiv ntawm cov tshuaj ua haujlwm hauv cov qauv hauv vivo siv cov sesamolin ib tus neeg tsis tau tshawb pom dav dav, feem ntau hauv cov extracts uas muaj sesamolin. Ntau lub tswv yim tau tsim los daws qhov teeb meem physicochemical cov cuab yeej uas cuam tshuam cov kev ua haujlwm pharmacological ntawm bioactive compounds.
Piv txwv ntawm kev siv cov tshuaj xa cov tshuab los txhim kho cov solubility ntawm sesamin yog tsim los ntawm micelle, solid dispersion, thiab nano-emulsion carrier delivery systems. Kev txhim kho nyob rau hauv solubility, dissolution profiles, qhov ncauj bioavailability, plab hnyuv permeability ntawm sesamin, thiab thiaj li pharmacological kev ua ub no ntawm sesamin tau tshwm sim [70-72]. Interestingly, tsis muaj kev tshawb fawb txog sesamolin's physicochemical zog li. Qhov teeb meem no yog qhib rau kev tshawb nrhiav ntxiv thiab tau dhau los ua ib qho kev tshawb fawb yav tom ntej. Tsis tas li ntawd, kev tshawb fawb ntawm cov tshuaj pharmacological ntawm cov tshuaj no tseem qhib dav, tshwj xeeb tshaj yog thaum cov teeb meem solubility tuaj yeem daws tau. Cov kev tshawb pom ntawm qhov kev tshawb fawb tam sim no qhia tias sesamolin zoo li cog lus tias yog bioactive compound hauv vivo thiab muaj txiaj ntsig zoo rau kev noj qab haus huv.
Ntawm qhov tod tes, kev tshawb fawb soj ntsuam ntxiv thiab kev tshawb fawb txog kev nyab xeeb yog xav tau. Nws tuaj yeem raug txhais lus kho mob rau qhov zoo tshaj plaws ntawm kev siv tshwj xeeb thiab kev sib txawv ntawm daim tawv nqaij raws li nws cov tshuaj tiv thaiv antioxidant thiab tiv thaiv melanogenesis rau lub hom phiaj kho kom zoo nkauj, thiab pov thawj ntawm kev ua haujlwm antitumor rau kev kho mob qog noj ntshav ntawm daim tawv nqaij. Raws li peb muaj kev txhawj xeeb, cov ntaub ntawv ntawm kev tshawb fawb ntawm sesamolin xws li metabolic profiles, kev ua haujlwm lom neeg hauv vivo, thiab kev tshawb fawb txog kev siv yog tsawg. Peb cia siab tias tsab xov xwm tshuaj xyuas no tuaj yeem ua rau pom cov kev tshawb fawb ntxiv los ua kom muaj qhov sib txawv hauv daim teb no los ntawm kev qhia txog cov kev tshawb fawb tam sim no ntawm sesamolin.
cistanche stems
8. Cov lus xaus
Sesamolin yog ib qho tseem ceeb ntawm lignan tebchaw nyob rau hauv sesame noob thiab roj thiab muaj nyob rau hauv ntau hom noob hnav, dawb, xim av, thiab dub nyob rau hauv ntau feem pua. Sesamolin tuaj yeem raug cais tawm thiab huv si siv cov txheej txheem chromatography, tom qab ntawd qhia cov qauv siv cov txheej txheem spectrophotometric. Pharmacological kev ua ub no ntawm sesamolin muaj xws li antioxidants, daim tawv nqaij melanin inhibition, cell-tiv thaiv cov nyhuv tiv thaiv ntau yam stressed-induced cell tuag, thiab mob qog noj ntshav los ntawm proliferative inhibition thiab tiv thaiv kab mob. Sesamolin, yog li ntawd, tuaj yeem ua tus neeg sawv cev kho mob tiv thaiv ntau yam kab mob thiab tuaj yeem tshawb nrhiav ntxiv. Txij li thaum muaj ob peb tsab ntawv ceeb toom txog qhov ncaj qha cytotoxicity nyhuv ntawm sesamolin tiv thaiv cov qog nqaij hlav cancer, yog li tsis muaj kev tshaj tawm tau tshaj tawm nws cov IC50. Ntxiv mus, nws cov txheej txheem tua neeg tseem tsis meej. Tsis tas li ntawd, sesamolin pharmacological kev ua ub no nyob rau hauv vivo sim thiab lawv cov kev nyab xeeb tsis tau qhia. Tsuas yog cov tawv nqaij ua xua tshwm sim [73]. Lub hauv paus txheej txheem ntawm sesamolin hauv kev pab tib neeg tsis yog qhov tseeb. Qhov teeb meem nrog sesamolin tuaj yeem yog vim nws cov khoom siv physicochemical, uas muaj cov dej solubility tsawg. Yog li ntawd, nws yog ib qho nyuaj rau ua kom cov concentration nyob rau hauv cov kev sim nyob rau hauv vitro sim siv cov qauv ntawm tes thiab yuav muab tsawg bioavailability nyob rau hauv vivo sim. Kev txhim kho solubility yog suav tias yog qhov tseem ceeb rau sesamolin los txhim kho thiab ua kev tshawb fawb ntxiv ntawm cov tshuaj ua haujlwm tshuaj. Tsis tas li ntawd, muaj ob peb tsab ntawv ceeb toom kawm sesamolin's physicochemical zog li; qhov no tuaj yeem tshawb nrhiav ntxiv, dhau los ua qhov kev tshawb fawb yav tom ntej hauv daim teb no.
Cov ntaub ntawv
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