Menerba
Menerba, nke a makwaara dị ka Menopause Formula 101 (MF-101), bụ ọgwụ botanical nke na-arụ ọrụ dị ka modulator na-ahọrọ estrogen receptor (SERM) [1] nke a na-amụ maka ikike ya iji belata ọkụ ọkụ metụtara menopause. Menerba, estrogen receptor beta (ERβ) agonist (ERBA), bụ akụkụ nke klas ọhụrụ nke receptor subtype-selective estrogens, [1] bụ nke a na-ahọrọ na nhazi ederede na otu n'ime ụdị abụọ nke estrogen receptor (ER). Menerba nwere mkpuru osisi iri abụọ na abụọ ejirila mee ihe n'akụkọ ihe mere eme na ọgwụ ọdịnala ndị China.[2]
Menerba na-ejikọta ma ERα na ERβ ma nwee nkekọ nhata, mana ọ naghị arụ ọrụ ERα ma kama ọ na-arụ ọrụ naanị ERβ-mediated gene transcription.[3][4]
Ụzọ e si eme ihe
[dezie | dezie ebe o si]A kọọrọ Menerba ka ọ na-ebelata mgbaàmà nke ịhụ nsọ dị ka ọkụ ọkụ, ebe ọ na-enweghị mmetụta na-akpali akpali na endometrium ma ọ bụ anụ ahụ ara.[1]
N'ime ụdị xenograft nke òké, Menerba mepụtara ọdịdị dị iche na estrogen receptor alpha (ERα) site na ERβ ma e jiri ya tụnyere ọdịdị nke estradiol mepụtara. Mgbanwe a kapịrị ọnụ nke Menerba kpatara na-enye ohere ka ERβ jikọta ya na ihe mmeghachi omume estrogen ma nata protein ndị na-achịkwa nke achọrọ maka ịrụ ọrụ nke mkpụrụ ndụ ihe nketa.[5] E gosipụtara na ohere dị ukwuu nke Ọrịa kansa ara na akpa nwa nwere njikọ na ERα na ERβ na-egbochi mmetụta na-akwalite uto na mkpụrụ ndụ kansa ara.[6] Menerba anaghị arụ ọrụ ERα-na-achịkwa proliferative genes, c-myc na cyclin D1, ma ọ bụ na-akpali MCF-7 breast cancer cell proliferation ma ọ bụ mmepụta nke akpụ, na-egosi na ọ nwere ike ịbụ ihe ọzọ dị irè maka Ọgwụgwọ hormone ma e jiri ya tụnyere estrogen nke na-ahọrọghị arụ ọrụ abụọ ER subtypes.[1]
N'afọ 2007, Menerba rụzuru ọtụtụ ụlọ ọrụ Phase 2, nke kpuru ìsì abụọ, nke placebo na-achịkwa na-enyocha ikike ya maka ọgwụgwọ ọkụ ọkụ na ụmụ nwanyị 217 nwere ahụike na US. Onye isi nyocha nke ikpe ahụ bụ Dr. Deborah Grady nke Mahadum California, San Francisco. Menerba gosipụtara ọnụ ọgụgụ dị ịrịba ama ọnụ ọgụgụ nke ọkụ ọkụ na-ekpo ọkụ mgbe izu iri na abụọ nke ọgwụgwọ gasịrị ma nwee mbelata nke ukwuu na edemede abalị site na ọkụ ọkụ (-67%, p=0.05). Enweghị ọdịiche dị na ọbara ọgbụgba nke akpanwa n'etiti otu ọgwụgwọ na placebo, ọ dịghịkwa ihe na-adịghị mma nke akpanwa hụrụ n'oge ọmụmụ ihe. Naanị mmetụta dị n'akụkụ a hụrụ bụ stool dị nro (12% na otu ọgwụgwọ vs. 3% n'ime otu placebo).[1]
Nnyocha ndị ọzọ egosiwo na ihe kachasị arụ ọrụ na Menerba bụ liquiritigenin, nke sitere na mgbọrọgwụ nke Glycyrrhizae uralensis Fisch, otu n'ime ihe iri abụọ na abụọ sitere na osisi a hụrụ na Menerba. N'ime ihe nlereanya nke òké xenograft, liquiritigenin na-arụ ọrụ ọtụtụ ihe nchịkwa ER na mkpụrụ ndụ ihe nketa nke ERβ ma ọ bụghị ERα. Nhọrọ ERβ nke liquiritigenin bụ n'ihi nhọpụta nke coactivator steroid receptor coactivator-2 na-elekwasị anya na mkpụrụ ndụ ihe nketa. Liquiritigenin emeghị ka ogo akpa nwa ma ọ bụ tumorigenesis nke mkpụrụ ndụ kansa ara MCF-7. Nsonaazụ na-egosi na ụfọdụ osisi nwere estrogens nke ukwuu maka ERβ [1] ma na-ahọrọ dị ka ogige sịntetik, ma na-achịkwa mkpụrụ ndụ ihe nketa dị iche iche. (PLOs 1 - Julaị 17) ma na-atụ aro na ogige ERb nke na-emepụta ihe ọkụkụ nwere ike iduga na nchebe ọzọ na-adọrọ adọrọ maka mgbaàmà menopausal.[2][3] N'ọmụmụ ihe ọzọ, e gosipụtara Menerba na-achịkwa ntinye nke calcium, nke metụtara nhazi okpomọkụ.[7]
Menerba nwere ule nchekwa nke Phase 1 na-enyocha nsi ya na 10 g / ụbọchị yana 15 g kwa ụbọchị. Ahụbeghị ihe nsi dị mkpa n'ime ọmụmụ anụmanụ ọ bụla nwere doses sitere na 2000 mg/kg/ụbọchị n'ime nkịta ruo 16,000 mg/kg/ụbọchị n'ime òké. N'ihi nsonaazụ nsi a na-anakwere na nnwale nke Phase 1, FDA kwadoro Menerba ka ọ malite ikpe 3 Phase na ụmụ nwanyị 1200 na-akọ ọkụ ọkụ asaa ma ọ bụ karịa menopausal kwa ụbọchị.
Hụkwa
[dezie | dezie ebe o si]- Nwoke Na-alụ Nwanyị
- Rimostil
Edensibia
[dezie | dezie ebe o si]- ↑ 1.0 1.1 1.2 1.3 Grady (2009). "MF101, a selective estrogen receptor β modulator for the treatment of menopausal hot flushes". Menopause 16 (3): 458–65. DOI:10.1097/gme.0b013e31818e64dd. PMID 19182698.
- ↑ Stovall (2009). "MF-101, an estrogen receptor beta agonist for the treatment of vasomotor symptoms in peri- and postmenopausal women". Current Opinion in Investigational Drugs 10 (4): 365–71. PMID 19337958.
- ↑ Jackson (2011). "Emerging evidence of the health benefits of S-equol, an estrogen receptor β agonist". Nutrition Reviews 69 (8): 432–448. DOI:10.1111/j.1753-4887.2011.00400.x. ISSN 0029-6643. PMID 21790611.
- ↑ Kaunitz (2009). "Effective herbal treatment of vasomotor symptoms-are we any closer?". Menopause 16 (3): 428–429. DOI:10.1097/gme.0b013e31819774e4. ISSN 1072-3714. PMID 19169160.
- ↑ Cvoro (2006). "Selective Activation of Estrogen Receptor- Transcriptional Pathways by an Herbal Extract". Endocrinology 148 (2): 538–47. DOI:10.1210/en.2006-0803. PMID 17095596.
- ↑ King (2009). "Timosaponin AIII is Preferentially Cytotoxic to Tumor Cells through Inhibition of mTOR and Induction of ER Stress". PLOS ONE 4 (9): e7283. DOI:10.1371/journal.pone.0007283. PMID 19789631.
- ↑ Zhang (2010). "Estrogen Receptor β-Selective Agonists Stimulate Calcium Oscillations in Human and Mouse Embryonic Stem Cell-Derived Neurons". PLOS ONE 5 (7): e11791. DOI:10.1371/journal.pone.0011791. PMID 20668547.